The present study aimed to investigate the brain targeting efficacy of Lamotrigine (LTG) loaded P... more The present study aimed to investigate the brain targeting efficacy of Lamotrigine (LTG) loaded PLGA nanoparticles (LTG-PNPs) upon intranasal administration. LTG-PNPs were fabricated through the emulsification-solvent evaporation technique and evaluated for % Entrapment efficiency, particle size, in-vitro release, surface morphology, crystallinity, ex-vivo permeation & thermal behaviour. Biodistribution, gamma scintigraphy, and pharmacodynamic studies were performed in BALB/c mice, New Zealand rabbits, and Wistar rats respectively. LTG-PNPs exhibited % EE 71%; particle size 170.0 nm; Polydispersity index 0.191; zeta potential -16.60 mV. LTG-PNPs exhibited a biphasic release pattern. Biodistribution and gamma scintigraphy studies proved a greater amount of LTG in the brain following intranasal delivery of LTG-PNPs in comparison to LTG-SOL. Pharmacodynamic studies demonstrated delayed seizure onset time with LTG-PNPs in comparison to LTG-SOL. Intranasal administration of LTG-PNPs provided prolonged release, higher bioavailability, and better brain targeting bypassing the BBB. The developed formulation could be administered as a once-a-day formulation that would reduce the dosing frequency; dose; dose-related side effects; cost of the therapy and would be beneficial in the management of epilepsy as compared to the LTG-SOL. However, the proof of concept generated through these studies needs to be further validated in higher animals and human volunteers.
High-dose methotrexate (HDMTX) is gaining importance in the management of acute lymphoblastic leu... more High-dose methotrexate (HDMTX) is gaining importance in the management of acute lymphoblastic leukemia (ALL). Its efficacy and toxicity depends on dose strength, route of administration, and infusion time. HDMTX toxicities can be controlled by continuous monitoring of urine pH and adequate supportive care (hyper-hydration, alkalinizing agents, and leucovorin rescue). A patient suffering from B cell Ph + ALL was kept on Berlin-Frankfurt-Munster-90 protocol and administered methotrexate 8 g/cycle by intravenous infusion with normal saline over 6 h. He developed leucopenia and severe anemia after receiving the first cycle of chemotherapy, which was treated with subcutaneous filgrastim 300 mcg OD for 5 days and 1 pint red blood cell. After the third cycle, patient developed mucositis and treated with leucovorin and local anesthetics; and continued the chemotherapy. In conclusion, the patient was continuously monitored for urine pH and tolerated the HDMTX well when provided adequate supp...
Standardization of herbal formulations is essential in order to assess the quality of drugs, base... more Standardization of herbal formulations is essential in order to assess the quality of drugs, base on the concentration of their active principles, physical and chemical standards. Standardization of the poly herbal formulation is possible by following modern scientific quality control procedure both for raw material and the finished product. The phytochemical constituents found to be present in the raw material used for the preparation of “RIPARE” possibly facilitate the desirable therapeutic efficacy of standardized medicinal formulation as a whole, and also could help in knowing the underlying mechanisms of the pharmacological action. The article reports on standardization of polyherbal formulation used to heal the arthritis. Specific plant extracts are used in the preparation of “RIPARE” polyherbal formulation. “RIPARE” Capsule has a good amount of herbal ingredients that possess antiarthritic activity. They were also screened for the evaluation of phytochemical parameters, prese...
5-Fluorouracil (5-FU) is the most preferred chemotherapeutic agent in the management of colon can... more 5-Fluorouracil (5-FU) is the most preferred chemotherapeutic agent in the management of colon cancer but is associated with poor therapeutic efficacy and lack of site specificity. Hence, it was aimed to employ Eudragit S100 surface engineered 5-FU nanostructured lipid carriers for the spatial and temporal release of the drug for the treatment of colon cancer. Hot high-pressure homogenization (HPH) technique was employed in the preparation of 5-FU-NLCs. The optimization of 5-FU-NLCs was performed using a Quality by Design (QbD) approach. A 32 factorial design was employed wherein the relationship between independent variables [amount of oleic acid (X1) and concentration of Tween®80 (X2)] and dependent variables [particle size (Y1) and % entrapment efficiency (Y2)] was studied. Optimized 5-FU-NLCs were surface treated to obtain Eudragit S100-coated 5-FU-NLCs (EU-5-FU-NLCs). The evaluation parameters for 5-FU-NLCs and EU-5-FU-NLCs included surface morphology, particle size, PDI, and ze...
Standardization of herbal formulations is the quality of drugs, based on the concentration princi... more Standardization of herbal formulations is the quality of drugs, based on the concentration principles, physical and chemical standards. herbal formulation is possible by following modern scientific quality control procedure both for raw material and the finished product. The phytochemical constituents found to be present in the raw material used for the preparation of RENOLITH possibly facilitate the desirable therapeutic efficacy of standardized medicinal formulation as a whole, and also could help in knowing the underlying mechanisms of the pharmacological action. The article reports on standardization of poly heal the renal stone. Specific plant extracts are used in the preparation of RENOLITH polyherbal formulation. RENOLITH herbal ingredients that possess antiurolithiatic activity. They were also screene d for the evaluation of phytochemical parameters, presence of pathogens, heavy metals and their Quality Control Parameters.
Background: The pharmacists can contribute to positive therapeutic outcomes by educating patients... more Background: The pharmacists can contribute to positive therapeutic outcomes by educating patients for rational use of medications. A chronic obstructive pulmonary disease (COPD) is one the most prevalent chronic respiratory diseases which requires continuous medication therapy. The clinical pharmacist can play an effective role through providing patient counselling to improve medication adherence and therapeutic outcomes. Aims and Objectives: The present study aims to assess the baseline levels of knowledge, attitude and practice of COPD patients and to study the impact of patient counselling on level of knowledge, attitude and practice with COPD patients. Materials and Methods: A total 90 patients (45 in the test group and 45 in control group) were enrolled in the study. A validated Knowledge, Attitude and Practice (KAP) Questionnaire was administered to both test and control group of patients at base line and at follow up (after 15 days) to assess the awareness regarding disease m...
Background and aim The present study evaluates the antidiabetic effects of aqueous (CPAQ) and met... more Background and aim The present study evaluates the antidiabetic effects of aqueous (CPAQ) and methanolic (CPME) extract of Costus pictus D. Don singly and/or in combination with metformin in alloxan-induced diabetic rats. Experimental procedure CPAQ and CPME (400 mg/kg dose), metformin (120 mg/kg) and two different combinations of plant extracts and metformin (200 + 60 mg/kg and 400 mg/kg + 60 mg/kg) were orally given to alloxan-induced diabetic rats for 21 days. At 0, 7, 14, and 21 days, body weight and blood glucose levels were measured. Results and conclusion After 21 days of treatment, biochemical profiling and histopathology analysis were carried out. CPAQ and CPME, when administrated separately, could decrease blood glucose levels (P ≤ 0.05). CPME showed more promising results (P ≤ 0.05) compared to the diabetic control group. Extracts co-administrated with metformin showed dose-dependent significant recovery of hypoglycemic activity of metformin. Fasting blood glucose levels,...
The objective of the present study was to evaluate the potential of solid dispersion adsorbate to... more The objective of the present study was to evaluate the potential of solid dispersion adsorbate to improve the solubility and bioavailability of rivaroxaban (RXN). Solid dispersion adsorbate (SDA) of RXN was developed by fusion method using PEG 4000 as carrier and Neusilin as adsorbent. A 32 full factorial design was utilized to formulate various SDAs. The selected independent variables were amount of carrier (X1) and amount of adsorbate (X2). The responses measured were time required for 85% drug release (Y1) and saturated solubility (Y2). MTT assay was employed for cytotoxicity studies on Caco-2 cells. In vivo pharmacokinetics and pharmacodynamic evaluations were carried out to assess the prepared SDA. Pre-compression evaluation of SDA suggests the prepared batches (B1-B9) possess adequate flow properties and could be used for compression of tablets. Differential scanning calorimetry and X-ray diffraction data signified the conversion of crystalline form of drug to amorphous form, ...
Ticagrelor (TG) suffers from low peroral bioabsorption (36%) due to P-gp efflux and poor solubili... more Ticagrelor (TG) suffers from low peroral bioabsorption (36%) due to P-gp efflux and poor solubility (10 µg/mL). TG solid dispersion adsorbates (TG-SDAs) were formulated using an amalgamation of solid dispersion and melt adsorption techniques which were simple, economic, scalable, and solvent-free. FTIR indicated no incompatibility between drug and excipients. DSC, XRD, and SEM suggested a reduction in TG crystallinity. Q30min from TG-SUSP and TG-conventional tablets was only 2.30% and 6.59% respectively whereas TG-SDA-based tablets exhibited a significantly higher drug release of 86.47%. Caco-2 permeability studies showed 3.83-fold higher permeability of TG from TG-SDAs. TG-SDA-based tablets exhibited relative bioavailability of 748.53% and 153.43% compared to TG-SUSP and TG-conventional tablets respectively in rats. TG-SDA-based tablets were devoid of any cytotoxicity as indicated by MTT assay and exhibited better antiplatelet activity in rats. Enhanced oral bioavailability of TG-SDAs can be attributed to inhibition of P-gp efflux by PEG 4000, increased wettability, and reduced crystallinity of drug leading to improved drug solubility and dissolution. Improved bioabsorption results in a reduction of dose, cost of therapy as well as dose-related side effects. Thus, SDAs can be considered a promising and scalable approach for the improvement of dissolution rate and solubility of TG. TG-SDAs can be translated to an effective and safe dosage form, whereby its rapid onset of action promotes the prevention of heart attack, stroke, and related ill events in individuals with the acute coronary syndrome. However, scale-up, validation, and clinical-studies are necessary for confirmation of the proof-of-concept.
Objective This study aims to investigate the change in quality adjusted life-years (QALYs) after ... more Objective This study aims to investigate the change in quality adjusted life-years (QALYs) after providing oncology pharmacist services to assess its impact on humanistic outcome. Methods It was a prospective, single-centered study conducted for a period of two years at Bharat cancer Hospital and Nirali memorial radiation center, Surat. Patients were recruited into the control group (CG) and the intervention group (IG). The oncology pharmacist services (OPS) were provided only to the IG. The humanistic outcome was measured by incorporating the EQ-5D-5L instrument to calculate quality-adjusted life-years (QALYs) in both the groups. Patients have been provided with the EQ-5D-5L questionnaire at the pre-determined intervals i.e. before the commencement of chemotherapy and then after every chemotherapy cycle till the completion of treatment. The analysis was carried out using descriptive analysis (frequency distribution for categorical variables and measures of central tendency (median ...
The prevalence of cardiometabolic disorders (CMDs) is increasing all around the world especially ... more The prevalence of cardiometabolic disorders (CMDs) is increasing all around the world especially in India. The CMDs are a cluster of abnormalities linked to insulin resistance and high risk for cardiovascular diseases (CVDs). To estimate cardiometabolic risk prediction profile without known CVDs and metabolic disorders in a southern Gujarat population, a prospective cross-sectional study conducted in the rural areas of south Gujarat for 6 months. Undiagnosed subjects with age 20–80 years were included in the study, and the information regarding anthropometric measurements, sociodemographic details, socioeconomic status, blood pressure and fasting blood glucose was collected to estimate cardiometabolic risk using the Indian Diabetes Risk Score (IDRS) and WHO CVDs risk chart. Multivariate regression analysis was performed to assess cardiometabolic risk factors. For diabetes risk, amongst 200 respondents, 103 (51.5%) subjects were having moderate risk followed by 61 (30.5%) and 36 (18%) having high and low risk respectively. For CVD risk, as per SBP vs. BMI, the majority of the subjects (151, 75.5%) were found with low risk followed by moderate risk (33, 16.5%) and high risk (16, 8%) whereas for CVD risk, as per SBP vs. blood glucose, the highest number of subjects was found with low risk (172, 86%), followed by moderate risk (16, 8%) and high risk (12, 6%). Our study suggests that the IDRS and WHO CVD prediction charts are a convenient and affordable screening tool for the assessment of diabetes and CVD mortality risk, respectively, in the settings where limited resources are available.
Linagliptin (LGP), a novel anti-diabetic drug, is a DPP-4 inhibitor used in the treatment of type... more Linagliptin (LGP), a novel anti-diabetic drug, is a DPP-4 inhibitor used in the treatment of type II diabetes. One of the major disadvantages of LGP is its low oral bioavailability (29.5%) due to first-pass metabolism and P-gp efflux. In an attempt to increase the oral bioavailability, LGP solid lipid nanoparticles (LGP-SLNs) were developed with poloxamer 188 and Tween 80 as P-gp inhibitors. LGP-SLNs were formulated using palmitic acid, poloxamer 188 and Tween 80 as lipid, surfactant and co-surfactant, respectively, by hot homogenization ultrasonication method and optimized using 3 2 full factorial designs. Particle size, entrapment efficiency (%EE) and drug release at 24 h were evaluated as responses. An optimized batch of LGP-SLNs (L12) was evaluated for intestinal transport of LGP by conducting in situ single-pass intestinal perfusion (SPIP), everted gut sac and Caco-2 permeability study. The pharmacokinetic and pharmacodynamic evaluation of L12 was carried out in albino Wistar rats. The mean particle size, polydispersity index, zeta potential and %EE of L12 were found to be 225.96 ± 2.8 nm, 0.180 ± 0.034, − 5.4 ± 1.07 mV and 73.8 ± 1.73%, respectively. %CDR of 80.96 ± 3.13% was observed in 24 h. The permeability values of LGP-SLNs in the absorptive direction were 1.82-, 1.76- and 1.74-folds higher than LGP-solution (LGP-SOL) in SPIP, everted gut sac and Caco-2 permeability studies, respectively. LGP-SLNs exhibited relative bioavailability of 300% and better reduction in glucose levels in comparison with LGP-SOL in rats. The enhanced oral bioavailability exhibited by LGP-SLNs bioavailability may be due to P-gp efflux inhibition and lymphatic targeting. Improved bioabsorption can cause reduction in dose, dose-related side effects and frequency of administration. Thus, LGP-SLNs can be considered promising carriers for oral delivery but clinical studies are required to confirm the proof of concept. Graphical abstract
Background: Intranasal administration of biodegradable nanoparticles has been extensively studied... more Background: Intranasal administration of biodegradable nanoparticles has been extensively studied for targeting the drug directly to CNS through olfactory or trigeminal route bypassing blood brain barrier. Objective: The objective of the present study was to optimize Clonazepam loaded PLGA nanoparticles (CLO-PNPs) by investigating the effect of process variables on the responses using 32 full factorial design. Methods: Effect of two independent factors-amount of PLGA and concentration of Poloxamer 188, were studied at low, medium and high levels on three dependent responses-%Entrapment efficiency, Particle size (nm) and %cumulative drug release at 24hr. Results: %EE, Particle size and %CDR at 24hr of optimized batch was 63.7%, 165.1 nm and 86.96% respectively. Nanoparticles were radiolabeled with 99mTc and biodistribution was investigated in BALB/c mice after intranasal & intravenous administrations. Significantly higher brain/blood uptake ratios and AUC values in brain following in...
International Journal of Pharmacy and Pharmaceutical Sciences
Objective: To develop a rapid, simple and sensitive ultra-performance liquid chromatography and t... more Objective: To develop a rapid, simple and sensitive ultra-performance liquid chromatography and tandem mass spectrometry (UPLC-MS/MS) method for quantitative estimation of atenolol (ATN) in rat plasma and its application to pharmacokinetic drug-herb interaction study.Methods: Simple precipitation method was used for the extraction of plasma samples with an aliquot of 25 μl plasma samples extracted using acetonitrile precipitation technique containing internal standard. Chromatographic separation was performed using Phenomenex, Kinetex, C18, 50 x 2.1 mm, 1.7µ by a gradient mixture of 0.1 % formic acid in acetonitrile and 10 mmol Ammonium formate as a mobile phase at the flow rate of 0.7 ml/min. The analyte was protonated in the positive electrospray ionization (ESI) interface and detected in multiple reactions monitoring (MRM) modes using the transition m/z 145.0-267.2.Results: The developed method had an advantage of fast chromatography run time of 1.8 min with improved sensitivity ...
Contact lenses are ideally suited for extended drug delivery to the ocular tissues, but incorpora... more Contact lenses are ideally suited for extended drug delivery to the ocular tissues, but incorporation of any particulate system affects the critical properties of the contact lens. Timolol loading by the conventional soaking method does not significantly alter the critical properties of the contact lens. However, there are challenges of low drug loading and high burst release. This research work aimed to investigate the effect of gold nanoparticles (GNPs) on loading and its release kinetics from the contact lens using the soaking method. In one approach, GNPs were loaded into the timolol soaking solution (GNPs-SS), and in another approach, GNPs were incorporated into the contact lenses (GNPs-CL) during fabrication. The contact lenses were soaked at two different concentrations of timolol (i.e., 2 mg/ml and 4 mg/ml). Swelling and optical transmittance were not significantly affected by the presence of GNPs in the contact lenses. A significant uptake/loading of timolol using the GNPs in both the approaches was observed. The in vitro flux data showed no significant improvement in the release rate profiles of timolol when using both approaches. However, the in vivo study in the rabbit tear fluid showed high timolol concentration with the GNPs-laden contact lens at all timepoints in comparison to the soaked contact lenses without GNPs. The in vivo pharmacodynamic study in rabbits showed a 2 mmHg average fall in intraocular pressure (72 h) using the GNPs-laden contact lenses, while the soaked contact lenses without GNPs and eye drops solution (0.5 %w/v) showed 2 mmHg. The drug distribution study in the ocular tissue showed a significant improvement in the drug deposition with the GNPs-laden contact lenses in the ciliary muscle and conjunctiva. This study successfully demonstrated the potential of GNPs to enhance the uptake of drug from the drug soaking solution to treat glaucoma without compromising the critical properties of contact lens. STATEMENT OF SIGNIFICANCE: In this study, we have overcome the limitation of the conventional soaking method of low drug loading and high burst release from the contact lenses. We have investigated the effect of gold nanoparticles (GNPs) on the timolol loading and its release kinetics from the contact lenses. The study revealed the potential of GNPs to enhance the uptake of timolol from the timolol soaking solution to treat glaucoma without compromising the critical lens properties.
The present study aimed to investigate the brain targeting efficacy of Lamotrigine (LTG) loaded P... more The present study aimed to investigate the brain targeting efficacy of Lamotrigine (LTG) loaded PLGA nanoparticles (LTG-PNPs) upon intranasal administration. LTG-PNPs were fabricated through the emulsification-solvent evaporation technique and evaluated for % Entrapment efficiency, particle size, in-vitro release, surface morphology, crystallinity, ex-vivo permeation & thermal behaviour. Biodistribution, gamma scintigraphy, and pharmacodynamic studies were performed in BALB/c mice, New Zealand rabbits, and Wistar rats respectively. LTG-PNPs exhibited % EE 71%; particle size 170.0 nm; Polydispersity index 0.191; zeta potential -16.60 mV. LTG-PNPs exhibited a biphasic release pattern. Biodistribution and gamma scintigraphy studies proved a greater amount of LTG in the brain following intranasal delivery of LTG-PNPs in comparison to LTG-SOL. Pharmacodynamic studies demonstrated delayed seizure onset time with LTG-PNPs in comparison to LTG-SOL. Intranasal administration of LTG-PNPs provided prolonged release, higher bioavailability, and better brain targeting bypassing the BBB. The developed formulation could be administered as a once-a-day formulation that would reduce the dosing frequency; dose; dose-related side effects; cost of the therapy and would be beneficial in the management of epilepsy as compared to the LTG-SOL. However, the proof of concept generated through these studies needs to be further validated in higher animals and human volunteers.
High-dose methotrexate (HDMTX) is gaining importance in the management of acute lymphoblastic leu... more High-dose methotrexate (HDMTX) is gaining importance in the management of acute lymphoblastic leukemia (ALL). Its efficacy and toxicity depends on dose strength, route of administration, and infusion time. HDMTX toxicities can be controlled by continuous monitoring of urine pH and adequate supportive care (hyper-hydration, alkalinizing agents, and leucovorin rescue). A patient suffering from B cell Ph + ALL was kept on Berlin-Frankfurt-Munster-90 protocol and administered methotrexate 8 g/cycle by intravenous infusion with normal saline over 6 h. He developed leucopenia and severe anemia after receiving the first cycle of chemotherapy, which was treated with subcutaneous filgrastim 300 mcg OD for 5 days and 1 pint red blood cell. After the third cycle, patient developed mucositis and treated with leucovorin and local anesthetics; and continued the chemotherapy. In conclusion, the patient was continuously monitored for urine pH and tolerated the HDMTX well when provided adequate supp...
Standardization of herbal formulations is essential in order to assess the quality of drugs, base... more Standardization of herbal formulations is essential in order to assess the quality of drugs, base on the concentration of their active principles, physical and chemical standards. Standardization of the poly herbal formulation is possible by following modern scientific quality control procedure both for raw material and the finished product. The phytochemical constituents found to be present in the raw material used for the preparation of “RIPARE” possibly facilitate the desirable therapeutic efficacy of standardized medicinal formulation as a whole, and also could help in knowing the underlying mechanisms of the pharmacological action. The article reports on standardization of polyherbal formulation used to heal the arthritis. Specific plant extracts are used in the preparation of “RIPARE” polyherbal formulation. “RIPARE” Capsule has a good amount of herbal ingredients that possess antiarthritic activity. They were also screened for the evaluation of phytochemical parameters, prese...
5-Fluorouracil (5-FU) is the most preferred chemotherapeutic agent in the management of colon can... more 5-Fluorouracil (5-FU) is the most preferred chemotherapeutic agent in the management of colon cancer but is associated with poor therapeutic efficacy and lack of site specificity. Hence, it was aimed to employ Eudragit S100 surface engineered 5-FU nanostructured lipid carriers for the spatial and temporal release of the drug for the treatment of colon cancer. Hot high-pressure homogenization (HPH) technique was employed in the preparation of 5-FU-NLCs. The optimization of 5-FU-NLCs was performed using a Quality by Design (QbD) approach. A 32 factorial design was employed wherein the relationship between independent variables [amount of oleic acid (X1) and concentration of Tween®80 (X2)] and dependent variables [particle size (Y1) and % entrapment efficiency (Y2)] was studied. Optimized 5-FU-NLCs were surface treated to obtain Eudragit S100-coated 5-FU-NLCs (EU-5-FU-NLCs). The evaluation parameters for 5-FU-NLCs and EU-5-FU-NLCs included surface morphology, particle size, PDI, and ze...
Standardization of herbal formulations is the quality of drugs, based on the concentration princi... more Standardization of herbal formulations is the quality of drugs, based on the concentration principles, physical and chemical standards. herbal formulation is possible by following modern scientific quality control procedure both for raw material and the finished product. The phytochemical constituents found to be present in the raw material used for the preparation of RENOLITH possibly facilitate the desirable therapeutic efficacy of standardized medicinal formulation as a whole, and also could help in knowing the underlying mechanisms of the pharmacological action. The article reports on standardization of poly heal the renal stone. Specific plant extracts are used in the preparation of RENOLITH polyherbal formulation. RENOLITH herbal ingredients that possess antiurolithiatic activity. They were also screene d for the evaluation of phytochemical parameters, presence of pathogens, heavy metals and their Quality Control Parameters.
Background: The pharmacists can contribute to positive therapeutic outcomes by educating patients... more Background: The pharmacists can contribute to positive therapeutic outcomes by educating patients for rational use of medications. A chronic obstructive pulmonary disease (COPD) is one the most prevalent chronic respiratory diseases which requires continuous medication therapy. The clinical pharmacist can play an effective role through providing patient counselling to improve medication adherence and therapeutic outcomes. Aims and Objectives: The present study aims to assess the baseline levels of knowledge, attitude and practice of COPD patients and to study the impact of patient counselling on level of knowledge, attitude and practice with COPD patients. Materials and Methods: A total 90 patients (45 in the test group and 45 in control group) were enrolled in the study. A validated Knowledge, Attitude and Practice (KAP) Questionnaire was administered to both test and control group of patients at base line and at follow up (after 15 days) to assess the awareness regarding disease m...
Background and aim The present study evaluates the antidiabetic effects of aqueous (CPAQ) and met... more Background and aim The present study evaluates the antidiabetic effects of aqueous (CPAQ) and methanolic (CPME) extract of Costus pictus D. Don singly and/or in combination with metformin in alloxan-induced diabetic rats. Experimental procedure CPAQ and CPME (400 mg/kg dose), metformin (120 mg/kg) and two different combinations of plant extracts and metformin (200 + 60 mg/kg and 400 mg/kg + 60 mg/kg) were orally given to alloxan-induced diabetic rats for 21 days. At 0, 7, 14, and 21 days, body weight and blood glucose levels were measured. Results and conclusion After 21 days of treatment, biochemical profiling and histopathology analysis were carried out. CPAQ and CPME, when administrated separately, could decrease blood glucose levels (P ≤ 0.05). CPME showed more promising results (P ≤ 0.05) compared to the diabetic control group. Extracts co-administrated with metformin showed dose-dependent significant recovery of hypoglycemic activity of metformin. Fasting blood glucose levels,...
The objective of the present study was to evaluate the potential of solid dispersion adsorbate to... more The objective of the present study was to evaluate the potential of solid dispersion adsorbate to improve the solubility and bioavailability of rivaroxaban (RXN). Solid dispersion adsorbate (SDA) of RXN was developed by fusion method using PEG 4000 as carrier and Neusilin as adsorbent. A 32 full factorial design was utilized to formulate various SDAs. The selected independent variables were amount of carrier (X1) and amount of adsorbate (X2). The responses measured were time required for 85% drug release (Y1) and saturated solubility (Y2). MTT assay was employed for cytotoxicity studies on Caco-2 cells. In vivo pharmacokinetics and pharmacodynamic evaluations were carried out to assess the prepared SDA. Pre-compression evaluation of SDA suggests the prepared batches (B1-B9) possess adequate flow properties and could be used for compression of tablets. Differential scanning calorimetry and X-ray diffraction data signified the conversion of crystalline form of drug to amorphous form, ...
Ticagrelor (TG) suffers from low peroral bioabsorption (36%) due to P-gp efflux and poor solubili... more Ticagrelor (TG) suffers from low peroral bioabsorption (36%) due to P-gp efflux and poor solubility (10 µg/mL). TG solid dispersion adsorbates (TG-SDAs) were formulated using an amalgamation of solid dispersion and melt adsorption techniques which were simple, economic, scalable, and solvent-free. FTIR indicated no incompatibility between drug and excipients. DSC, XRD, and SEM suggested a reduction in TG crystallinity. Q30min from TG-SUSP and TG-conventional tablets was only 2.30% and 6.59% respectively whereas TG-SDA-based tablets exhibited a significantly higher drug release of 86.47%. Caco-2 permeability studies showed 3.83-fold higher permeability of TG from TG-SDAs. TG-SDA-based tablets exhibited relative bioavailability of 748.53% and 153.43% compared to TG-SUSP and TG-conventional tablets respectively in rats. TG-SDA-based tablets were devoid of any cytotoxicity as indicated by MTT assay and exhibited better antiplatelet activity in rats. Enhanced oral bioavailability of TG-SDAs can be attributed to inhibition of P-gp efflux by PEG 4000, increased wettability, and reduced crystallinity of drug leading to improved drug solubility and dissolution. Improved bioabsorption results in a reduction of dose, cost of therapy as well as dose-related side effects. Thus, SDAs can be considered a promising and scalable approach for the improvement of dissolution rate and solubility of TG. TG-SDAs can be translated to an effective and safe dosage form, whereby its rapid onset of action promotes the prevention of heart attack, stroke, and related ill events in individuals with the acute coronary syndrome. However, scale-up, validation, and clinical-studies are necessary for confirmation of the proof-of-concept.
Objective This study aims to investigate the change in quality adjusted life-years (QALYs) after ... more Objective This study aims to investigate the change in quality adjusted life-years (QALYs) after providing oncology pharmacist services to assess its impact on humanistic outcome. Methods It was a prospective, single-centered study conducted for a period of two years at Bharat cancer Hospital and Nirali memorial radiation center, Surat. Patients were recruited into the control group (CG) and the intervention group (IG). The oncology pharmacist services (OPS) were provided only to the IG. The humanistic outcome was measured by incorporating the EQ-5D-5L instrument to calculate quality-adjusted life-years (QALYs) in both the groups. Patients have been provided with the EQ-5D-5L questionnaire at the pre-determined intervals i.e. before the commencement of chemotherapy and then after every chemotherapy cycle till the completion of treatment. The analysis was carried out using descriptive analysis (frequency distribution for categorical variables and measures of central tendency (median ...
The prevalence of cardiometabolic disorders (CMDs) is increasing all around the world especially ... more The prevalence of cardiometabolic disorders (CMDs) is increasing all around the world especially in India. The CMDs are a cluster of abnormalities linked to insulin resistance and high risk for cardiovascular diseases (CVDs). To estimate cardiometabolic risk prediction profile without known CVDs and metabolic disorders in a southern Gujarat population, a prospective cross-sectional study conducted in the rural areas of south Gujarat for 6 months. Undiagnosed subjects with age 20–80 years were included in the study, and the information regarding anthropometric measurements, sociodemographic details, socioeconomic status, blood pressure and fasting blood glucose was collected to estimate cardiometabolic risk using the Indian Diabetes Risk Score (IDRS) and WHO CVDs risk chart. Multivariate regression analysis was performed to assess cardiometabolic risk factors. For diabetes risk, amongst 200 respondents, 103 (51.5%) subjects were having moderate risk followed by 61 (30.5%) and 36 (18%) having high and low risk respectively. For CVD risk, as per SBP vs. BMI, the majority of the subjects (151, 75.5%) were found with low risk followed by moderate risk (33, 16.5%) and high risk (16, 8%) whereas for CVD risk, as per SBP vs. blood glucose, the highest number of subjects was found with low risk (172, 86%), followed by moderate risk (16, 8%) and high risk (12, 6%). Our study suggests that the IDRS and WHO CVD prediction charts are a convenient and affordable screening tool for the assessment of diabetes and CVD mortality risk, respectively, in the settings where limited resources are available.
Linagliptin (LGP), a novel anti-diabetic drug, is a DPP-4 inhibitor used in the treatment of type... more Linagliptin (LGP), a novel anti-diabetic drug, is a DPP-4 inhibitor used in the treatment of type II diabetes. One of the major disadvantages of LGP is its low oral bioavailability (29.5%) due to first-pass metabolism and P-gp efflux. In an attempt to increase the oral bioavailability, LGP solid lipid nanoparticles (LGP-SLNs) were developed with poloxamer 188 and Tween 80 as P-gp inhibitors. LGP-SLNs were formulated using palmitic acid, poloxamer 188 and Tween 80 as lipid, surfactant and co-surfactant, respectively, by hot homogenization ultrasonication method and optimized using 3 2 full factorial designs. Particle size, entrapment efficiency (%EE) and drug release at 24 h were evaluated as responses. An optimized batch of LGP-SLNs (L12) was evaluated for intestinal transport of LGP by conducting in situ single-pass intestinal perfusion (SPIP), everted gut sac and Caco-2 permeability study. The pharmacokinetic and pharmacodynamic evaluation of L12 was carried out in albino Wistar rats. The mean particle size, polydispersity index, zeta potential and %EE of L12 were found to be 225.96 ± 2.8 nm, 0.180 ± 0.034, − 5.4 ± 1.07 mV and 73.8 ± 1.73%, respectively. %CDR of 80.96 ± 3.13% was observed in 24 h. The permeability values of LGP-SLNs in the absorptive direction were 1.82-, 1.76- and 1.74-folds higher than LGP-solution (LGP-SOL) in SPIP, everted gut sac and Caco-2 permeability studies, respectively. LGP-SLNs exhibited relative bioavailability of 300% and better reduction in glucose levels in comparison with LGP-SOL in rats. The enhanced oral bioavailability exhibited by LGP-SLNs bioavailability may be due to P-gp efflux inhibition and lymphatic targeting. Improved bioabsorption can cause reduction in dose, dose-related side effects and frequency of administration. Thus, LGP-SLNs can be considered promising carriers for oral delivery but clinical studies are required to confirm the proof of concept. Graphical abstract
Background: Intranasal administration of biodegradable nanoparticles has been extensively studied... more Background: Intranasal administration of biodegradable nanoparticles has been extensively studied for targeting the drug directly to CNS through olfactory or trigeminal route bypassing blood brain barrier. Objective: The objective of the present study was to optimize Clonazepam loaded PLGA nanoparticles (CLO-PNPs) by investigating the effect of process variables on the responses using 32 full factorial design. Methods: Effect of two independent factors-amount of PLGA and concentration of Poloxamer 188, were studied at low, medium and high levels on three dependent responses-%Entrapment efficiency, Particle size (nm) and %cumulative drug release at 24hr. Results: %EE, Particle size and %CDR at 24hr of optimized batch was 63.7%, 165.1 nm and 86.96% respectively. Nanoparticles were radiolabeled with 99mTc and biodistribution was investigated in BALB/c mice after intranasal & intravenous administrations. Significantly higher brain/blood uptake ratios and AUC values in brain following in...
International Journal of Pharmacy and Pharmaceutical Sciences
Objective: To develop a rapid, simple and sensitive ultra-performance liquid chromatography and t... more Objective: To develop a rapid, simple and sensitive ultra-performance liquid chromatography and tandem mass spectrometry (UPLC-MS/MS) method for quantitative estimation of atenolol (ATN) in rat plasma and its application to pharmacokinetic drug-herb interaction study.Methods: Simple precipitation method was used for the extraction of plasma samples with an aliquot of 25 μl plasma samples extracted using acetonitrile precipitation technique containing internal standard. Chromatographic separation was performed using Phenomenex, Kinetex, C18, 50 x 2.1 mm, 1.7µ by a gradient mixture of 0.1 % formic acid in acetonitrile and 10 mmol Ammonium formate as a mobile phase at the flow rate of 0.7 ml/min. The analyte was protonated in the positive electrospray ionization (ESI) interface and detected in multiple reactions monitoring (MRM) modes using the transition m/z 145.0-267.2.Results: The developed method had an advantage of fast chromatography run time of 1.8 min with improved sensitivity ...
Contact lenses are ideally suited for extended drug delivery to the ocular tissues, but incorpora... more Contact lenses are ideally suited for extended drug delivery to the ocular tissues, but incorporation of any particulate system affects the critical properties of the contact lens. Timolol loading by the conventional soaking method does not significantly alter the critical properties of the contact lens. However, there are challenges of low drug loading and high burst release. This research work aimed to investigate the effect of gold nanoparticles (GNPs) on loading and its release kinetics from the contact lens using the soaking method. In one approach, GNPs were loaded into the timolol soaking solution (GNPs-SS), and in another approach, GNPs were incorporated into the contact lenses (GNPs-CL) during fabrication. The contact lenses were soaked at two different concentrations of timolol (i.e., 2 mg/ml and 4 mg/ml). Swelling and optical transmittance were not significantly affected by the presence of GNPs in the contact lenses. A significant uptake/loading of timolol using the GNPs in both the approaches was observed. The in vitro flux data showed no significant improvement in the release rate profiles of timolol when using both approaches. However, the in vivo study in the rabbit tear fluid showed high timolol concentration with the GNPs-laden contact lens at all timepoints in comparison to the soaked contact lenses without GNPs. The in vivo pharmacodynamic study in rabbits showed a 2 mmHg average fall in intraocular pressure (72 h) using the GNPs-laden contact lenses, while the soaked contact lenses without GNPs and eye drops solution (0.5 %w/v) showed 2 mmHg. The drug distribution study in the ocular tissue showed a significant improvement in the drug deposition with the GNPs-laden contact lenses in the ciliary muscle and conjunctiva. This study successfully demonstrated the potential of GNPs to enhance the uptake of drug from the drug soaking solution to treat glaucoma without compromising the critical properties of contact lens. STATEMENT OF SIGNIFICANCE: In this study, we have overcome the limitation of the conventional soaking method of low drug loading and high burst release from the contact lenses. We have investigated the effect of gold nanoparticles (GNPs) on the timolol loading and its release kinetics from the contact lenses. The study revealed the potential of GNPs to enhance the uptake of timolol from the timolol soaking solution to treat glaucoma without compromising the critical lens properties.
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