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Gul Majid Khan

Islamia College University Peshawar, VC Secretriat, Vice Chancellor

Quaid-i-Azam University, Islamabad, Pakistan, Pharmacy, Faculty Member

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•>38-years extensive Teaching, Research and Administrative experience with in the Country and abroad in several Western as well as Eastern Countries along with vast experience in the areas of planning
Supervisors: Vice Chancellor, Islamia College University Peshawar

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Papers by Gul Majid Khan

Formulation and evaluation of controlled release matrices of ketoprofen and influence of different co-excipients on the release mechanism

Pharmazie, 2011

GM Khan CV List of Publications 2022

Dr Gul Majid Khan CV List of Publications 2021

Pharmacist-led counselling intervention to improve antiretroviral drug adherence in Pakistan: a randomized controlled trial

BMC Infectious Diseases

Background Pakistan is facing a growing population of people living with human immunodeficiency (... more Background Pakistan is facing a growing population of people living with human immunodeficiency (HIV). In this randomized controlled trial, we investigate if a pharmacist-led intervention can increase adherence to antiretroviral therapy (ART) for people living with HIV (PLWH). Methods Adults with HIV, who have been taking ART for more than 3 months were randomly assigned to receive either a pharmacist-led intervention or their usual care. Measures of adherence were collected at 1) baseline 2) just prior to delivery of intervention and 3) 8 weeks later. The primary outcomes were CD4 cell count and self-reported adherence measured with the AIDS Clinical Trial Group (ACTG) questionnaire. Results Post-intervention, the intervention group showed a statistically significant increase in CD4 cell counts as compared to the usual care group (p = 0.0054). In addition, adherence improved in the intervention group, with participants being 5.96 times more likely to report having not missed their ...

Knowledge, perception and attitude about Crimean Congo Hemorrhagic Fever (CCHF) among medical and pharmacy students of Pakistan

BMC Public Health

Background: Crimean Congo Hemorrhagic (CCHF) is a deadly tick born disease caused by a virus of g... more Background: Crimean Congo Hemorrhagic (CCHF) is a deadly tick born disease caused by a virus of genus Nairovirus and is endemic in the Middle East, Asia, Africa, and Eastern areas of Europe. Pakistan is a CCHF endemic country with a constant threat of sporadic outbreaks. Health care workers are more prone to CCHF, hence, it is a prerequisite for members of the healthcare team to stay abreast with current knowledge and display positive attitude and perception. This study assessed the medical and pharmacy students' preparedness level in terms of CCHF control and management. Methods: A total of 900 consenting students were selected randomly, who completed a predesigned and validated questionnaire which assessed the participant's general knowledge, emergency preparedness control and management of CCHF. Data were analyzed by SPSS (IBM SPSS version 21). For data analysis percentages, P-value, ttest, the independent sample mean, Whitney U test, Kruskal-Wallis test, Logistic regression, and Spearman correlation were utilized. Results: Among 900 study respondents, 68% were females and 32% were males, out of which physicians (MBBS) students were 48.4%, and pharmacists students were 51.6%. Majority of the respondents 39.9% were from age group of 22-25 years. Overall 43% healthcare students demonstrated good knowledge about disease causes, transmission, and treatment options. Additionally, 81% of the study participants showed positive attitude, whereas, 69% students demonstrated positive perceptions. The correlation coefficient showed positive correlation between attitude-perception (r = 0.268, p value = 0.000), knowledge-attitude (r = 0.234, p value = 0.000) and knowledgeperception (r = 0.257, p value = 0.000). Conclusions: Knowledge gaps were observed which is alarming. These gaps were multifactorial and mainly due to lack of knowledge, poor motivation, and old syllabus which needs to be addressed. The study results show that it is crucial to evaluate current curriculum and also showing a dire need of awareness seminars, conferences workshops to highlight and educate about the current endemic disease to future health care professionals.

Nanotechnology: from In Vivo Imaging System to Controlled Drug Delivery

Nanoscale Research Letters

Science and technology have always been the vitals of human's struggle, utilized exclusively for ... more Science and technology have always been the vitals of human's struggle, utilized exclusively for the development of novel tools and products, ranging from micro-to nanosize. Nanotechnology has gained significant attention due to its extensive applications in biomedicine, particularly related to bio imaging and drug delivery. Various nanodevices and nanomaterials have been developed for the diagnosis and treatment of different diseases. Herein, we have described two primary aspects of the nanomedicine, i.e., in vivo imaging and drug delivery, highlighting the recent advancements and future explorations. Tremendous advancements in the nanotechnology tools for the imaging, particularly of the cancer cells, have recently been observed. Nanoparticles offer a suitable medium to carryout molecular level modifications including the site-specific imaging and targeting. Invention of radionuclides, quantum dots, magnetic nanoparticles, and carbon nanotubes and use of gold nanoparticles in biosensors have revolutionized the field of imaging, resulting in easy understanding of the pathophysiology of disease, improved ability to diagnose and enhanced therapeutic delivery. This high specificity and selectivity of the nanomedicine is important, and thus, the recent advancements in this field need to be understood for a better today and a more prosperous future.

Dengue fever again in Pakistan: are we going in the right direction?

Public health, Jan 8, 2017

Carboxylate derivatives of tributyltin (IV) complexes as anticancer and antileishmanial agents

DARU Journal of Pharmaceutical Sciences, 2017

Background: Tributyltin (IV) compounds are promising candidates for drug development. In the curr... more Background: Tributyltin (IV) compounds are promising candidates for drug development. In the current study, we evaluated in-vitro and in-silico profile of carboxylate derivatives of tributyltin (IV) complexes. Methods: ADMET and drug-likeliness properties were predicted using MetaPrint2D React, preADMET, SwissADME and Molsoft tools. SwissTargetPrediction predicted molecular targets for compounds. In-vitro bioactivity was evaluated by quantifying cytotoxicity against HepG2, THP-1 cell lines, isolated lymphocytes and leishmania promastigotes as well as measuring protein kinase (PK) inhibition activity. Results: Results indicate partial compliance of compounds with drug-likeliness rules. Ch-409 complies with WDI and Lipinski rules. ADMET profile prediction shows strong plasma protein binding except for Ch-409, low to high GI absorption and BBB penetration (C brain /C blood = 0.942-11; caco-2 cells permeability 20.13-26.75 nm/sec), potential efflux by P-glycoprotein, metabolism by CYP3A4, medium inhibition of hERG, mutagenicity and capacity to be detoxified by glutathionation and glucuronidation. Molecular targets include proteases, enzymes, membrane receptors, transporters and ion channels where Ch-409 targets membrane receptors only. Compounds are significantly (p < 0.05) cytotoxic against HepG2 cell line and leishmania as compared with normal isolated lymphocytes. Ch-459 indicates highest toxicity against leishmania (mortality 97.9 ± 3.99%; LC50 0.323 ± 0.002 μg/mL) whereas Ch-409 possesses maximum cytotoxicity against HepG2 cell line (IC50 0.08 ± 0.001 μg/mL) as well as 97.5 ± 1.98% (LC50 0.954 ± 0.158 μg/mL) mortality of leishmania promastigotes. It was observed that antileishmanial effect was reduced by 16.38%-34.38% and 15-38.2% in the presence of NaN 3 and mannitol respectively. PK inhibition and reactive oxygen species production are possible mechanisms for cytotoxicity. Conclusions: Selected carboxylate derivatives of tributyltin (IV) complexes possess significant antileishmanial and cytotoxic potential. These are promising compounds for the development of antileishmanial and anticancer drugs.

Appraisal of phytochemical and in vitro biological attributes of an unexplored folklore: Rhus Punjabensis Stewart

BMC complementary and alternative medicine, Jan 9, 2017

The role of plants for discovery of therapeutic potential accentuates the need to know their biol... more The role of plants for discovery of therapeutic potential accentuates the need to know their biological attributes. The present study aims to comprehend the biological attributes of Rhus punjabensis, an unexplored traditional medicinal plant. Leaf and stem extracts of R. punjabensis prepared in 11 different organic solvents are evaluated for multimode antioxidant potential, total phenolic and flavonoid contents were determined through colorimetric assays, HPLC-DAD analysis was carried out for quantification of various polyphenols in extracts. Brine shrimp lethality, SRB and MTT assays were used to elucidate plant's cytotoxic and antileishmanial potentials. Disc diffusion assay was used to elucidate the protein kinase inhibitory, antibacterial and antifungal spectrum. Ethanol + ethyl acetate yielded maximum extract recovery from leaf (6.11 ± 1.09% w/w), total phenolic content (80.5 ± 2.18 μg GAE/mg extract) and reducing power potential (165.4 ± 2.29 μg AAE/mg extract). Maximum fl...

Photocatalytic and antibacterial response of biosynthesized Gold nanoparticles

Journal of Photochemistry and Photobiology B: Biology, 2016

Increase in the bacterial resistance to available antibiotics and water contamination by differen... more Increase in the bacterial resistance to available antibiotics and water contamination by different toxic organic dyes are both severe problems throughout the world. To overcome these concerns, new methodologies including synthesis of nontoxic, human friendly and efficient nanoparticles is required. These nanoparticles not even inhibit the growth of microorganisms but are also effective in the degradation of toxic organics in waste water thus providing a clean and human friendly environment. The use of plants extracts to synthesize and stabilize noble metal nanoparticles have been considered as safe, cost-effective, eco-benign and green approach nowadays. In the present study, Longan fruit juice proficiently reduced ionic gold (Au(+3)) to gold nanoparticles (AuNPs) as well as mediated the stabilization of AuNPs. The antibacterial activity of AuNPs was carried out against both gram positive and gram negative bacteria using agar well diffusion method, followed by the determination of Minimum inhibitory concentration (MIC) values. AuNPs were found to have significant antibacterial activity against Escherichia coli with MIC values of 75μg/ml while outstanding MIC values of 50μg/ml against Staphylococcus areous and Basilus subtilus. AuNPs revealed significant photocatalytic degradation (76%) of methylene blue in time period of 55min, indicating the effective photocatalytic property of biosynthesized AuNPs (K=0.29/min, r(2)=0.95). The considerable antibacterial and photocatalytic activities of the photosynthesized AuNPs can be attributed towards their small size, spherical morphology and uniform dispersion. Our finding suggests the possible therapeutic potential of biogenic AuNPs in the development of new antibacterial agents as well as in the development of effective photocatalysts.

Formulation and in vitro evaluation of ibuprofen-carbopol ® 974P-NF controlled release matrix tablets III: influence of co-excipients on release rate of the drug

J Control Release, 1998

In order to assess the potential of carbopol 974P-NF as matrix material in hydrophilic matrix tab... more In order to assess the potential of carbopol 974P-NF as matrix material in hydrophilic matrix tablets containing a slightly water-soluble drug, ibuprofen (IBF), controlled release matrix tablets of ibuprofen and carbopol 974P-NF, at different drug to polymer ratios, were prepared by the direct compression method. The influence of the concentration of the matrix material (carbopol 974P) and several co-excipients (lactose, microcrystalline cellulose, and starch) on the release rate of the drug was investigated. An in vitro dissolution test in pH 7.2 phosphate buffer solution showed that drug release from all the formulations containing carbopol 974P was considerably prolonged in concentration-dependent manners. Increasing the amount of carbopol 974P in tablets resulted in a reduction in the drug release rate and a linearization of the drug release curve. When the influence of the co-excipients on the release of the drug was examined, all of the co-excipients used in this study enhanced the release rate of IBF. However, lactose demonstrated slower and more linear release behavior as compared in microcrystalline cellulose or starch. The dissolution T50 and T90 values for the three co-excipients were in the order of lactose &amp;amp;amp;amp;gt; microcrystalline cellulose &amp;amp;amp;amp;gt; starch.

Influence of molecular weight & particle size of polymers on drug release mechanism & release kinetics of the drugs

Ramzan GJMS 2(1) 16 (2004) COMPARATIVE STUDY OF VARIOUS GROWTH MEDIA IN

Towards a correlation between drug properties and in vitro transdermal flux variability

International journal of pharmaceutics, Jan 4, 2007

Over recent years, there has been growing evidence that the permeability coefficient variability ... more Over recent years, there has been growing evidence that the permeability coefficient variability describing any specific transdermal drug delivery system is not always normally distributed. However, since different researchers have used different test compounds, methodologies and skin types, it has been difficult to identify any general correlation between drug properties and flux variability. The aim of the present study was to investigate whether there was a relationship between these two variables. To this end, six different compounds (sucrose, adenosine, aldosterone, corticosterone, oestradiol and testosterone) exhibiting a range of partition coefficients but relatively similar molecular weights were screened by taking multiple replicate measurements of their permeation profiles as they penetrated across porcine skin in vitro. It was found that for relatively hydrophilic solutes (log P(o/w)< or = approximately 2.5), physicochemical properties that facilitated slow transdermal...

Comparative evaluation of some new tranexamic acid derivatives and their copper (II) complexes for antitumor, analgesic, bactericidal and fungicidal activities

Pakistan journal of pharmaceutical sciences, 2002

The objective of this series of investigation was the synthesis and comparative evaluation of bio... more The objective of this series of investigation was the synthesis and comparative evaluation of biological and pharmacological activities of some substitutive derivatives of Tranexamic Acid (T.A) and their copper (II) complexes. N-Phthaloyltranexamic Acid (A-1), N-Acetyltranexamic Acid (A-2), Di-Tranexamate Diaquo Copper (II) (C-1) Di-N-Phthaloyltranexamate Diaquo Copper (II) (C-2) and Di-N-Acetyltranexamate Diaquo Copper (II) (C-3) were synthesized, using novel and reproducible procedures. These compounds were characterized by exploiting techniques such as FTIR, Mass Spectroscopy and FT 1H NMR. Bioactivities of the compounds were carried out and it was found that these compounds exhibited excellent anti-tumor, significant analgesic and antifungal activities.

Development of novel diclofenac potassium controlled release tablets by wet granulation technique and the effect of co-excipients on in vitro drug release rates

Pakistan journal of pharmaceutical sciences, 2012

The aim of the present study was the formulation and evaluation of controlled release polymeric t... more The aim of the present study was the formulation and evaluation of controlled release polymeric tablets of Diclofenac Potassium by wet granulation method for the release rate, release pattern and the mechanism involved in drug release. Formulations having three grades of polymer Ethocel (7P; 7FP, 10P, 10FP, 100P, 100FP) in several drugs to polymer ratios (10:3 and 10:1) were compressed into tablets using wet granulation method. Co-excipients were added to some selected formulations to investigate their enhancement effect on in vitro drug release patterns. In vitro drug release studies were performed using USP Method-1 (Rotating Basket method) and Phosphate buffer (pH 7.4) was used as a dissolution medium. The similarities and dissimilarities of release profiles of test formulations with reference standard were checked using f2 similarity factor and f1 dissimilarity factor. Mathematical/Kinetic models were employed to determine the release mechanism and drug release kinetics.

Curcumin: A Natural Product of Biological Importance

Curcumin is a small molecular weight, polyphenolic compound, isolated from the roots of curcuma l... more Curcumin is a small molecular weight, polyphenolic compound, isolated from the roots of curcuma longa L. (family zingiberaceae), has been used traditionally for centuries in Asia for medicinal, culinary and other purposes. A large number of in vitro and in vivo studies in both animals and man have indicated that Curcumin has strong antioxidant, anti-inflammatory, anti-carcinogenic, anti-microbial, anti-parasitic and other activities. The mechanisms of some of these actions have recently been intensively investigated. Safety evaluation studies indicate Curcumin is well tolerated at a very high dose without any toxic effects. Thus, Curcumin has the potential for the development of modern medicine for the treatment of various diseases.

Nigella sativa provides protection against metabolic syndrome

AFRICAN JOURNAL OF BIOTECHNOLOGY, 2012

The seeds of Nigella sativa have been used in folk medicine all over the world. The plant has bee... more The seeds of Nigella sativa have been used in folk medicine all over the world. The plant has been of interest due to its low degree of toxicity and beneficial pharmacological properties like antihypertensive, hypoglycemic, antifungal, anti-inflammatory, antihistaminic, antioxidant, along with significant anti-neuplastic activities. The present clinical study was undertaken to ascertain the adjuvant effect of Nigella seeds on various clinical and biochemical parameters of metabolic syndrome. After final diagnosis and considering inclusion and exclusion criteria, one hundred and fifty nine patients were enrolled in this study. Patients were divided into two groups. In Group I (standard group), patients were advised to take simvastatin 10 mg once a day, metformin 500 mg twice a day, Enalapril 10 mg once a day, Atenolol 50 mg once a day and clopidagrel 75 mg once a day for a period of six weeks. In Group II (Nigella seeds group), patients were advised the above standard medication plus Nigella seeds 250 mg twice daily for a period of six weeks. Blood sugar both fasting and postprandial, fasting lipid profile and different parameters of obesity were recorded before therapy and after completion of therapy. It was found that the addition of Nigella seeds provide beneficial effects in all the clinical and biochemical parameters for the adult's treatment panel-III of metabolic disorders especially in fasting blood sugar, low density lipoproteins and high density lipoproteins. No sign of toxicity of the plant appeared in the Group II. Improvement in all other parameters like blood pressure, circumference of waist and serum triglyceride was also observed. Thus, Nigella seeds were found to be effective as an adjuvant therapy in patients of dyslipidemia and hyperglycemia.

Thiomers and their potential applications in drug delivery

Expert opinion on drug delivery, Jan 22, 2016

Thiomers are the product of the immobilization of sulfhydryl-bearing ligands onto the polymer bac... more Thiomers are the product of the immobilization of sulfhydryl-bearing ligands onto the polymer backbone of a conventional polymer, which results in a significant improvement in mucoadhesion; in situ gelation and efflux inhibition compare with unchanged polymers. Because of thiol groups, thiomers have more reactivity and enhanced protection against oxidation. Since the late 1990s, extensive work has been conducted on these promising polymeric excipients in the pharmaceutical field. This review covers thiomers, their classification and their different properties. Various techniques for the synthesis, purification and characterization of thiomers are described in detail. This review also encompasses their various properties such as mucoadhesion, permeation enhancement, in situ gelation and efflux inhibition, as well as different formulations based on thiomers. In addition to the use of thiomers as multifunctional excipients, this review also encompasses their use as drugs. The synthesis...

Investigating the in vitro drug release kinetics from controlled release diclofenac potassium-ethocel matrix tablets and the influence of co-excipients on drug release patterns

Pakistan journal of pharmaceutical sciences, 2011

The objective of the study was to formulate and evaluate controlled release polymeric tablets of ... more The objective of the study was to formulate and evaluate controlled release polymeric tablets of Diclofenac Potassium for the release rate, release patterns and the mechanism involved in the release process of the drug. Formulations with different types and grades of Ethyl Cellulose Ether derivatives in several drug-to-polymer ratios (D:P) were compressed into tablets using the direct compression method. In vitro drug release studies were performed in phosphate buffer (pH 7.4) as dissolution medium by using USP Method-1 (Rotating Basket Method). Similarity factor f2 and dissimilarity factor f1 were applied for checking the similarities and dissimilarities of the release profiles of different formulations. For the determination of the release mechanism and drug release kinetics various mathematical/kinetic models were employed. It was found that all of the Ethocel polymers could significantly slow down the drug release rate with Ethocel FP polymers being the most efficient, especiall...

Formulation and evaluation of controlled release matrices of ketoprofen and influence of different co-excipients on the release mechanism

Pharmazie, 2011

GM Khan CV List of Publications 2022

Dr Gul Majid Khan CV List of Publications 2021

Pharmacist-led counselling intervention to improve antiretroviral drug adherence in Pakistan: a randomized controlled trial

BMC Infectious Diseases

Background Pakistan is facing a growing population of people living with human immunodeficiency (... more Background Pakistan is facing a growing population of people living with human immunodeficiency (HIV). In this randomized controlled trial, we investigate if a pharmacist-led intervention can increase adherence to antiretroviral therapy (ART) for people living with HIV (PLWH). Methods Adults with HIV, who have been taking ART for more than 3 months were randomly assigned to receive either a pharmacist-led intervention or their usual care. Measures of adherence were collected at 1) baseline 2) just prior to delivery of intervention and 3) 8 weeks later. The primary outcomes were CD4 cell count and self-reported adherence measured with the AIDS Clinical Trial Group (ACTG) questionnaire. Results Post-intervention, the intervention group showed a statistically significant increase in CD4 cell counts as compared to the usual care group (p = 0.0054). In addition, adherence improved in the intervention group, with participants being 5.96 times more likely to report having not missed their ...

Knowledge, perception and attitude about Crimean Congo Hemorrhagic Fever (CCHF) among medical and pharmacy students of Pakistan

BMC Public Health

Background: Crimean Congo Hemorrhagic (CCHF) is a deadly tick born disease caused by a virus of g... more Background: Crimean Congo Hemorrhagic (CCHF) is a deadly tick born disease caused by a virus of genus Nairovirus and is endemic in the Middle East, Asia, Africa, and Eastern areas of Europe. Pakistan is a CCHF endemic country with a constant threat of sporadic outbreaks. Health care workers are more prone to CCHF, hence, it is a prerequisite for members of the healthcare team to stay abreast with current knowledge and display positive attitude and perception. This study assessed the medical and pharmacy students' preparedness level in terms of CCHF control and management. Methods: A total of 900 consenting students were selected randomly, who completed a predesigned and validated questionnaire which assessed the participant's general knowledge, emergency preparedness control and management of CCHF. Data were analyzed by SPSS (IBM SPSS version 21). For data analysis percentages, P-value, ttest, the independent sample mean, Whitney U test, Kruskal-Wallis test, Logistic regression, and Spearman correlation were utilized. Results: Among 900 study respondents, 68% were females and 32% were males, out of which physicians (MBBS) students were 48.4%, and pharmacists students were 51.6%. Majority of the respondents 39.9% were from age group of 22-25 years. Overall 43% healthcare students demonstrated good knowledge about disease causes, transmission, and treatment options. Additionally, 81% of the study participants showed positive attitude, whereas, 69% students demonstrated positive perceptions. The correlation coefficient showed positive correlation between attitude-perception (r = 0.268, p value = 0.000), knowledge-attitude (r = 0.234, p value = 0.000) and knowledgeperception (r = 0.257, p value = 0.000). Conclusions: Knowledge gaps were observed which is alarming. These gaps were multifactorial and mainly due to lack of knowledge, poor motivation, and old syllabus which needs to be addressed. The study results show that it is crucial to evaluate current curriculum and also showing a dire need of awareness seminars, conferences workshops to highlight and educate about the current endemic disease to future health care professionals.

Nanotechnology: from In Vivo Imaging System to Controlled Drug Delivery

Nanoscale Research Letters

Science and technology have always been the vitals of human's struggle, utilized exclusively for ... more Science and technology have always been the vitals of human's struggle, utilized exclusively for the development of novel tools and products, ranging from micro-to nanosize. Nanotechnology has gained significant attention due to its extensive applications in biomedicine, particularly related to bio imaging and drug delivery. Various nanodevices and nanomaterials have been developed for the diagnosis and treatment of different diseases. Herein, we have described two primary aspects of the nanomedicine, i.e., in vivo imaging and drug delivery, highlighting the recent advancements and future explorations. Tremendous advancements in the nanotechnology tools for the imaging, particularly of the cancer cells, have recently been observed. Nanoparticles offer a suitable medium to carryout molecular level modifications including the site-specific imaging and targeting. Invention of radionuclides, quantum dots, magnetic nanoparticles, and carbon nanotubes and use of gold nanoparticles in biosensors have revolutionized the field of imaging, resulting in easy understanding of the pathophysiology of disease, improved ability to diagnose and enhanced therapeutic delivery. This high specificity and selectivity of the nanomedicine is important, and thus, the recent advancements in this field need to be understood for a better today and a more prosperous future.

Dengue fever again in Pakistan: are we going in the right direction?

Public health, Jan 8, 2017

Carboxylate derivatives of tributyltin (IV) complexes as anticancer and antileishmanial agents

DARU Journal of Pharmaceutical Sciences, 2017

Background: Tributyltin (IV) compounds are promising candidates for drug development. In the curr... more Background: Tributyltin (IV) compounds are promising candidates for drug development. In the current study, we evaluated in-vitro and in-silico profile of carboxylate derivatives of tributyltin (IV) complexes. Methods: ADMET and drug-likeliness properties were predicted using MetaPrint2D React, preADMET, SwissADME and Molsoft tools. SwissTargetPrediction predicted molecular targets for compounds. In-vitro bioactivity was evaluated by quantifying cytotoxicity against HepG2, THP-1 cell lines, isolated lymphocytes and leishmania promastigotes as well as measuring protein kinase (PK) inhibition activity. Results: Results indicate partial compliance of compounds with drug-likeliness rules. Ch-409 complies with WDI and Lipinski rules. ADMET profile prediction shows strong plasma protein binding except for Ch-409, low to high GI absorption and BBB penetration (C brain /C blood = 0.942-11; caco-2 cells permeability 20.13-26.75 nm/sec), potential efflux by P-glycoprotein, metabolism by CYP3A4, medium inhibition of hERG, mutagenicity and capacity to be detoxified by glutathionation and glucuronidation. Molecular targets include proteases, enzymes, membrane receptors, transporters and ion channels where Ch-409 targets membrane receptors only. Compounds are significantly (p < 0.05) cytotoxic against HepG2 cell line and leishmania as compared with normal isolated lymphocytes. Ch-459 indicates highest toxicity against leishmania (mortality 97.9 ± 3.99%; LC50 0.323 ± 0.002 μg/mL) whereas Ch-409 possesses maximum cytotoxicity against HepG2 cell line (IC50 0.08 ± 0.001 μg/mL) as well as 97.5 ± 1.98% (LC50 0.954 ± 0.158 μg/mL) mortality of leishmania promastigotes. It was observed that antileishmanial effect was reduced by 16.38%-34.38% and 15-38.2% in the presence of NaN 3 and mannitol respectively. PK inhibition and reactive oxygen species production are possible mechanisms for cytotoxicity. Conclusions: Selected carboxylate derivatives of tributyltin (IV) complexes possess significant antileishmanial and cytotoxic potential. These are promising compounds for the development of antileishmanial and anticancer drugs.

Appraisal of phytochemical and in vitro biological attributes of an unexplored folklore: Rhus Punjabensis Stewart

BMC complementary and alternative medicine, Jan 9, 2017

The role of plants for discovery of therapeutic potential accentuates the need to know their biol... more The role of plants for discovery of therapeutic potential accentuates the need to know their biological attributes. The present study aims to comprehend the biological attributes of Rhus punjabensis, an unexplored traditional medicinal plant. Leaf and stem extracts of R. punjabensis prepared in 11 different organic solvents are evaluated for multimode antioxidant potential, total phenolic and flavonoid contents were determined through colorimetric assays, HPLC-DAD analysis was carried out for quantification of various polyphenols in extracts. Brine shrimp lethality, SRB and MTT assays were used to elucidate plant's cytotoxic and antileishmanial potentials. Disc diffusion assay was used to elucidate the protein kinase inhibitory, antibacterial and antifungal spectrum. Ethanol + ethyl acetate yielded maximum extract recovery from leaf (6.11 ± 1.09% w/w), total phenolic content (80.5 ± 2.18 μg GAE/mg extract) and reducing power potential (165.4 ± 2.29 μg AAE/mg extract). Maximum fl...

Photocatalytic and antibacterial response of biosynthesized Gold nanoparticles

Journal of Photochemistry and Photobiology B: Biology, 2016

Increase in the bacterial resistance to available antibiotics and water contamination by differen... more Increase in the bacterial resistance to available antibiotics and water contamination by different toxic organic dyes are both severe problems throughout the world. To overcome these concerns, new methodologies including synthesis of nontoxic, human friendly and efficient nanoparticles is required. These nanoparticles not even inhibit the growth of microorganisms but are also effective in the degradation of toxic organics in waste water thus providing a clean and human friendly environment. The use of plants extracts to synthesize and stabilize noble metal nanoparticles have been considered as safe, cost-effective, eco-benign and green approach nowadays. In the present study, Longan fruit juice proficiently reduced ionic gold (Au(+3)) to gold nanoparticles (AuNPs) as well as mediated the stabilization of AuNPs. The antibacterial activity of AuNPs was carried out against both gram positive and gram negative bacteria using agar well diffusion method, followed by the determination of Minimum inhibitory concentration (MIC) values. AuNPs were found to have significant antibacterial activity against Escherichia coli with MIC values of 75μg/ml while outstanding MIC values of 50μg/ml against Staphylococcus areous and Basilus subtilus. AuNPs revealed significant photocatalytic degradation (76%) of methylene blue in time period of 55min, indicating the effective photocatalytic property of biosynthesized AuNPs (K=0.29/min, r(2)=0.95). The considerable antibacterial and photocatalytic activities of the photosynthesized AuNPs can be attributed towards their small size, spherical morphology and uniform dispersion. Our finding suggests the possible therapeutic potential of biogenic AuNPs in the development of new antibacterial agents as well as in the development of effective photocatalysts.

Formulation and in vitro evaluation of ibuprofen-carbopol ® 974P-NF controlled release matrix tablets III: influence of co-excipients on release rate of the drug

J Control Release, 1998

In order to assess the potential of carbopol 974P-NF as matrix material in hydrophilic matrix tab... more In order to assess the potential of carbopol 974P-NF as matrix material in hydrophilic matrix tablets containing a slightly water-soluble drug, ibuprofen (IBF), controlled release matrix tablets of ibuprofen and carbopol 974P-NF, at different drug to polymer ratios, were prepared by the direct compression method. The influence of the concentration of the matrix material (carbopol 974P) and several co-excipients (lactose, microcrystalline cellulose, and starch) on the release rate of the drug was investigated. An in vitro dissolution test in pH 7.2 phosphate buffer solution showed that drug release from all the formulations containing carbopol 974P was considerably prolonged in concentration-dependent manners. Increasing the amount of carbopol 974P in tablets resulted in a reduction in the drug release rate and a linearization of the drug release curve. When the influence of the co-excipients on the release of the drug was examined, all of the co-excipients used in this study enhanced the release rate of IBF. However, lactose demonstrated slower and more linear release behavior as compared in microcrystalline cellulose or starch. The dissolution T50 and T90 values for the three co-excipients were in the order of lactose &amp;amp;amp;amp;gt; microcrystalline cellulose &amp;amp;amp;amp;gt; starch.

Influence of molecular weight & particle size of polymers on drug release mechanism & release kinetics of the drugs

Ramzan GJMS 2(1) 16 (2004) COMPARATIVE STUDY OF VARIOUS GROWTH MEDIA IN

Towards a correlation between drug properties and in vitro transdermal flux variability

International journal of pharmaceutics, Jan 4, 2007

Over recent years, there has been growing evidence that the permeability coefficient variability ... more Over recent years, there has been growing evidence that the permeability coefficient variability describing any specific transdermal drug delivery system is not always normally distributed. However, since different researchers have used different test compounds, methodologies and skin types, it has been difficult to identify any general correlation between drug properties and flux variability. The aim of the present study was to investigate whether there was a relationship between these two variables. To this end, six different compounds (sucrose, adenosine, aldosterone, corticosterone, oestradiol and testosterone) exhibiting a range of partition coefficients but relatively similar molecular weights were screened by taking multiple replicate measurements of their permeation profiles as they penetrated across porcine skin in vitro. It was found that for relatively hydrophilic solutes (log P(o/w)< or = approximately 2.5), physicochemical properties that facilitated slow transdermal...

Comparative evaluation of some new tranexamic acid derivatives and their copper (II) complexes for antitumor, analgesic, bactericidal and fungicidal activities

Pakistan journal of pharmaceutical sciences, 2002

The objective of this series of investigation was the synthesis and comparative evaluation of bio... more The objective of this series of investigation was the synthesis and comparative evaluation of biological and pharmacological activities of some substitutive derivatives of Tranexamic Acid (T.A) and their copper (II) complexes. N-Phthaloyltranexamic Acid (A-1), N-Acetyltranexamic Acid (A-2), Di-Tranexamate Diaquo Copper (II) (C-1) Di-N-Phthaloyltranexamate Diaquo Copper (II) (C-2) and Di-N-Acetyltranexamate Diaquo Copper (II) (C-3) were synthesized, using novel and reproducible procedures. These compounds were characterized by exploiting techniques such as FTIR, Mass Spectroscopy and FT 1H NMR. Bioactivities of the compounds were carried out and it was found that these compounds exhibited excellent anti-tumor, significant analgesic and antifungal activities.

Development of novel diclofenac potassium controlled release tablets by wet granulation technique and the effect of co-excipients on in vitro drug release rates

Pakistan journal of pharmaceutical sciences, 2012

The aim of the present study was the formulation and evaluation of controlled release polymeric t... more The aim of the present study was the formulation and evaluation of controlled release polymeric tablets of Diclofenac Potassium by wet granulation method for the release rate, release pattern and the mechanism involved in drug release. Formulations having three grades of polymer Ethocel (7P; 7FP, 10P, 10FP, 100P, 100FP) in several drugs to polymer ratios (10:3 and 10:1) were compressed into tablets using wet granulation method. Co-excipients were added to some selected formulations to investigate their enhancement effect on in vitro drug release patterns. In vitro drug release studies were performed using USP Method-1 (Rotating Basket method) and Phosphate buffer (pH 7.4) was used as a dissolution medium. The similarities and dissimilarities of release profiles of test formulations with reference standard were checked using f2 similarity factor and f1 dissimilarity factor. Mathematical/Kinetic models were employed to determine the release mechanism and drug release kinetics.

Curcumin: A Natural Product of Biological Importance

Curcumin is a small molecular weight, polyphenolic compound, isolated from the roots of curcuma l... more Curcumin is a small molecular weight, polyphenolic compound, isolated from the roots of curcuma longa L. (family zingiberaceae), has been used traditionally for centuries in Asia for medicinal, culinary and other purposes. A large number of in vitro and in vivo studies in both animals and man have indicated that Curcumin has strong antioxidant, anti-inflammatory, anti-carcinogenic, anti-microbial, anti-parasitic and other activities. The mechanisms of some of these actions have recently been intensively investigated. Safety evaluation studies indicate Curcumin is well tolerated at a very high dose without any toxic effects. Thus, Curcumin has the potential for the development of modern medicine for the treatment of various diseases.

Nigella sativa provides protection against metabolic syndrome

AFRICAN JOURNAL OF BIOTECHNOLOGY, 2012

The seeds of Nigella sativa have been used in folk medicine all over the world. The plant has bee... more The seeds of Nigella sativa have been used in folk medicine all over the world. The plant has been of interest due to its low degree of toxicity and beneficial pharmacological properties like antihypertensive, hypoglycemic, antifungal, anti-inflammatory, antihistaminic, antioxidant, along with significant anti-neuplastic activities. The present clinical study was undertaken to ascertain the adjuvant effect of Nigella seeds on various clinical and biochemical parameters of metabolic syndrome. After final diagnosis and considering inclusion and exclusion criteria, one hundred and fifty nine patients were enrolled in this study. Patients were divided into two groups. In Group I (standard group), patients were advised to take simvastatin 10 mg once a day, metformin 500 mg twice a day, Enalapril 10 mg once a day, Atenolol 50 mg once a day and clopidagrel 75 mg once a day for a period of six weeks. In Group II (Nigella seeds group), patients were advised the above standard medication plus Nigella seeds 250 mg twice daily for a period of six weeks. Blood sugar both fasting and postprandial, fasting lipid profile and different parameters of obesity were recorded before therapy and after completion of therapy. It was found that the addition of Nigella seeds provide beneficial effects in all the clinical and biochemical parameters for the adult's treatment panel-III of metabolic disorders especially in fasting blood sugar, low density lipoproteins and high density lipoproteins. No sign of toxicity of the plant appeared in the Group II. Improvement in all other parameters like blood pressure, circumference of waist and serum triglyceride was also observed. Thus, Nigella seeds were found to be effective as an adjuvant therapy in patients of dyslipidemia and hyperglycemia.

Thiomers and their potential applications in drug delivery

Expert opinion on drug delivery, Jan 22, 2016

Thiomers are the product of the immobilization of sulfhydryl-bearing ligands onto the polymer bac... more Thiomers are the product of the immobilization of sulfhydryl-bearing ligands onto the polymer backbone of a conventional polymer, which results in a significant improvement in mucoadhesion; in situ gelation and efflux inhibition compare with unchanged polymers. Because of thiol groups, thiomers have more reactivity and enhanced protection against oxidation. Since the late 1990s, extensive work has been conducted on these promising polymeric excipients in the pharmaceutical field. This review covers thiomers, their classification and their different properties. Various techniques for the synthesis, purification and characterization of thiomers are described in detail. This review also encompasses their various properties such as mucoadhesion, permeation enhancement, in situ gelation and efflux inhibition, as well as different formulations based on thiomers. In addition to the use of thiomers as multifunctional excipients, this review also encompasses their use as drugs. The synthesis...

Investigating the in vitro drug release kinetics from controlled release diclofenac potassium-ethocel matrix tablets and the influence of co-excipients on drug release patterns

Pakistan journal of pharmaceutical sciences, 2011

The objective of the study was to formulate and evaluate controlled release polymeric tablets of ... more The objective of the study was to formulate and evaluate controlled release polymeric tablets of Diclofenac Potassium for the release rate, release patterns and the mechanism involved in the release process of the drug. Formulations with different types and grades of Ethyl Cellulose Ether derivatives in several drug-to-polymer ratios (D:P) were compressed into tablets using the direct compression method. In vitro drug release studies were performed in phosphate buffer (pH 7.4) as dissolution medium by using USP Method-1 (Rotating Basket Method). Similarity factor f2 and dissimilarity factor f1 were applied for checking the similarities and dissimilarities of the release profiles of different formulations. For the determination of the release mechanism and drug release kinetics various mathematical/kinetic models were employed. It was found that all of the Ethocel polymers could significantly slow down the drug release rate with Ethocel FP polymers being the most efficient, especiall...

GM Khan's CURRICULUM VITAE

CURRICULUM VITAE, 2023

 >38-years extensive Teaching, Research experience with in the Country and abroad in several Wes... more  >38-years extensive Teaching, Research experience with in the Country and abroad in several Western as well as Eastern Countries along with vast experience in the areas of planning & development, project management and academic administration (including experience as Seniormost Dean & as Vice Chancellor).

GM Khan CV & List of Publications

GM Khan CV & List of Publications, 2022

 >38-years extensive Teaching, Research experience with in the Country and abroad in several Wes... more  >38-years extensive Teaching, Research experience with in the Country and abroad in several Western as well as Eastern Countries along with vast experience in the areas of planning & development, project management and academic administration (including experience as Seniormost Dean & as Vice Chancellor).