Naser Tavakoli

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Kerman University of Medical Sciences

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Prof. Dr. Abu Shara Shamsur Rouf

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Papers by Naser Tavakoli

Preparation of Diltiazem Topical Gel for the Treatment of Anal Fissure and In-Vitro, Ex-Vivo Drug Release Evaluations

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Drug Release Evaluation of Ibuprofen Sugar Coated and Film Coated Tablets Marketed in Iran

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Gastric Floating Matrix Tablets of Metformin Hcl : Design and Optimization Using Combination of Polymers

The objective of this study was to develop a floating drug delivery system (FDDS) from metformin ... more The objective of this study was to develop a floating drug delivery system (FDDS) from metformin hydrochloride to enhance gastro residence time (GRT), with floating properties which remain in the stomach more than gastric empting time (GET). Eight batches were prepared using hydrophilic polymers as release-retarding, and sodium bicarbonate as a gas former by direct compression technique. The effects of effervescent agent (sodium bicarbonate) and a binary combination of hydroxypropyl methylcellulose (HPMC) K4M with polyvinylpyrrolidone (PVP) or carbopol934 on floating properties and drug release profile were investigated. Drug release study was evaluated for 12 hours using USP paddle-type dissolution apparatus using 0.1N HCl in 37±0.5 ̊C as dissolution medium. The swelling index, floating behavior and kinetic parameter were found to be regulated by polymers and CO2 generating agent content. The results of powder ingredients and compressed tablets showed acceptable physicochemical pro...

Simvastatin nanosuspensions prepared using a combination of pH-sensitive and timed-release approaches for potential treatment of colorectal cancer

Pharmaceutical Development and Technology, 2021

Abstract A dual pH- and time-dependent polymeric coated capsule was developed to achieve the site... more Abstract A dual pH- and time-dependent polymeric coated capsule was developed to achieve the site specificity of simvastatin (SIM) release in the colon. To improve the SIM solubility, soluplus-based nanosuspension of the drug were prepared by applying the anti-solvent crystallization technique; this was then followed by lyophilization. Particle size, polydispersity index, and saturation solubility were evaluated. The optimized nanosuspension was combined with SLS and freeze-dried before filling into hard gelatin capsules. Drug release characteristics of the coated capsules were studied in HCl 0.1 N, the phosphate buffers 6.8 and 7.4, and the simulated colonic fluid (pH 6.8). The in-vitro cytotoxic effects of SIM nanoparticles against HT29 cells were then evaluated using the MTT assay. The prepared nanoparticles were spherical with a mean size of 261.66 nm, the zeta potential of −18.20 and the dissolution efficiency of 59.71%. X-ray diffraction and differential scanning calorimetry studies showed that the nanosizing technique transformed the crystalline drug into the more soluble amorphous form. The coated capsules had no release in the gastric media, providing the specific delivery of SIM in the colon. The cytotoxic effect of the SIM nanoparticles was significantly increased, as compared to the free SIM. The findings, therefore, showed that the coated capsules using the two polymers of ethyl cellulose and Eudragit S100 could be suitable for the colon target delivery of SIM. Graphical Abstract

An injectable carboxymethyl chitosan-methylcellulose-pluronic hydrogel for the encapsulation of meloxicam loaded nanoparticles

International Journal of Biological Macromolecules, 2020

et al., An injectable carboxymethyl chitosan-methylcellulose-pluronic hydrogel for the encapsulat... more

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Alginate hydrogel enriched with Ambystoma mexicanum epidermal lipoxygenase-loaded pectin nanoparticles for enhanced wound healing

Journal of Biomaterials Applications, 2019

Epidermal lipoxygenase enzyme extracted from Ambystoma mexicanum (AmbLOXe) is known to accelerate... more Epidermal lipoxygenase enzyme extracted from Ambystoma mexicanum (AmbLOXe) is known to accelerate the wound-healing process. AmbLOXe as a protein suffers from inactivation and losing its activity during formulation. Therefore, a delivery system that protects AmbLOXe from inactivation and preserves its activity is needed. We prepared AmbLOXe-loaded pectin nanoparticles (AmbLOXe Pec-NPs) and placed them into an alginate hydrogel. AmbLOXe Pec-NPs incorporation into the alginate hydrogel provides a means for controlled and sustained delivery of AmbLOXe to the wound site. Furthermore, the suitable swelling behavior and mechanical properties of AmbLOXe Pec-NPs alginate hydrogel make it feasible for clinical use. AmbLOXe Pec-NPs alginate hydrogel significantly enhanced the wound-healing process on the rat full-thickness excisional wounds, increased the rate of wound closure, enhanced the re-epithelialization and decreased the incidence of abnormal scarring. AmbLOXe Pec-NPs alginate hydroge...

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Formulation and evaluation of licorice shampoo in comparison with commercial shampoo

Journal of Pharmacy And Bioallied Sciences, 2018

Aim: Glycyrrhiza glabra (G. glabra) or licorice with isoflavonoid, flavonoids, and triterpenoid g... more Aim: Glycyrrhiza glabra (G. glabra) or licorice with isoflavonoid, flavonoids, and triterpenoid glycosides (saponins) components are highly regarded in the cosmetic industry. This study has been planned as the first project for formulating a new herbal shampoo by utilizing the aqueous extracts of G. glabra. Materials and Methods: The dried powdered root of G. glabra was extracted with boiled water through percolation method, and the pH was set by ammonia; then it was used with other constituents to formulate the herbal shampoo. The desirability of licorice shampoo was evaluated by physicochemical tests including visual inspection, detergency evaluation, pH assessment, percentage of solid contents, viscosity, foaming volume, and wetting time and compared with a commercial shampoo. Also, the product was checked for microbial control and consumers were asked about the quality of the licorice shampoo. Results: The licorice shampoo has excellent cleansing ability, acceptable clarity, and viscosity. The volume of created foam and the wetting time were similar to the commercial shampoo. No microbial contamination was observed during the microbial control assessment tests. The licorice shampoo scored well on consumer’s poll and was free from complication and also able to obviate hair and scalp problems. Discussion and Conclusion: The results indicated that the consumers were satisfied with using the formulated licorice shampoo. Licorice shampoo seems to be helpful in obviation of hair problems, but specific investigations are required to prove this claim. The shampoo was safe from microbial contamination and showed acceptable results in physicochemical evaluations. Licorice shampoo could be useful in the treatment of many hair diseases, so further research is needed for discovering the potential of licorice shampoo.

Transdermal iontophoretic delivery of celecoxib from gel formulation

Research in pharmaceutical sciences

Celecoxib is used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, joint inf... more Celecoxib is used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, joint inflammation and sport injuries. Long term administration of the drug results in such complications as gastrointestinaland renal disturbances and cardio-vascular complications. The main objective of the present study was to investigate the feasibility of delivering celecoxib incorporated in gel formulations by iontophoresis. Sodium alginate, sodium carboxymethyl cellulose, hydroxypropyl methylcellulose (HPMC) and carbopol 934P were used to develop topical gel formulations of celecoxib. The gel formulations were evaluated for macroscopic and microscopic properties, pH determination, spreadability, rheological behaviour, and drug release characteristics both in vitro and ex vivo. Drug release was evaluated in the presence of iontophoresis field (0.1 to 0.5 mA/cm(2)) or without electrical current (passive diffusion) and celecoxib was measured spectrophotometrically at 252 nm. Most gel formulat...

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Formulation of sustained - release lithium carbonate matrix tablets: influence of hydrophilic materials on the release rate and in vitro-in vivo evaluation

Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Société canadienne des sciences pharmaceutiques, Jan 15, 2004

Conventional lithium carbonate (LC) tablets not only produce rapid and relatively high peak blood... more Conventional lithium carbonate (LC) tablets not only produce rapid and relatively high peak blood levels resulting in adverse effects but also should be administered 3 to 4 times daily. These drawbacks can be overcome by designing a suitable sustained-release LC preparation. Sustained-release matrix tablets containing 450 mg LC were developed using different types and ratios of polymers including carbopol (CP), Na carboxymethylcellulose (Na CMC) and hydroxypropylmethylcellulose (HPMC). The tablets were prepared by either direct compression or wet granulation. In vitro and in vivo, newly formulated sustained-release LC tablets were compared with sustained-release commercial tablet (Eskalith CR). In vivo studies were conducted in nine healthy subjects in a cross over design, with a 3 3 Latin square sequence. Pharmacokinetic parameters were estimated using classical methods. The matrix tablets containing 15% CP exhibited suitable release kinetics and uniform absorption characteristics ...

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Evaluating the effect of magnesium and magnesium plus vitamin B6 supplement on the severity of premenstrual syndrome

Iranian journal of nursing and midwifery research, 2010

Since premenstrual syndrome (PMS) can cause suicide, dissociation of familial relationships, abno... more Since premenstrual syndrome (PMS) can cause suicide, dissociation of familial relationships, abnormalities in the daily work and inter-personal relationships in the patients, and bring about direct and indirect economic burden for the society, it is important to resolve the problems of the patients. The objective of the current study is to determine the effect of magnesium (Mg), combination of vitamin B6 and Mg, and the placebo on the severity of PMS in the patients affected by the disease referred to the health centers of Isfahan University of Medical Sciences during 2009-2010. The participants were randomly assigned to two intervention groups and one control group. The study was carried out for four months in ten selected health centers in Isfahan. To confirm the PMS diagnosis in patients, they were asked to fill out the PMS daily symptom record form for two months and then, when the diagnosis was confirmed, the participants were randomly assigned to one of the three groups of the...

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Calorimetric Investigations of Non-Viral DNA Transfection Systems

Thermodynamics - Kinetics of Dynamic Systems, 2011

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Application of Taguchi Method to Investigate the Drug Release Behavior of Poly(Acrylamide-co-Maleic Acid)/Montmorillonite Nanocomposite Hydrogels

Advances in Polymer Technology, 2014

The pH-sensitive poly(acrylamide-co-maleic acid)/montmorillonite (P(AAm-MA)/MMT) nanocomposite hy... more The pH-sensitive poly(acrylamide-co-maleic acid)/montmorillonite (P(AAm-MA)/MMT) nanocomposite hydrogels were synthesized through in situ polymerization. The chemical structure and morphology of nanocomposites were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, and transmission electron microscopy. The resulted disks were then loaded by caffeine, a moderately soluble model drug, using soaking method. The swelling and the drug release experiments were carried out in enzyme-free simulated gastric and intestinal fluids. The release experiments showed that with the addition of MMT, the burst effect is well controlled, and the barrier property of nanocomposite hydrogels is improved. The effects of some compositional parameters including maleic acid to acrylamide (MA/AAm) molar ratio (MA R), weight percent of MMT (MMT%), cross-linker/AAm molar ratio (C R), and also the influence of pH of medium on the equilibrium swelling ratio (Q) as well as caffeine release behavior of disks were studied by Taguchi method. The results indicated that shifting the pH value from 1.2 to 7.4 leads to a greater Q. The Q value and the release percentage (P%) increased with increasing the MA R in the structure of disks at pH 7.4. The amounts of P% and Q in both external media decreased with increasing both MMT% and C R. Mathematical behavior of release process was well represented by Peppas Power law model (at short times) and a two-dimensional Fickian mass transfer model (at long times). The caffeine release behavior in both media was corresponded to the non-Fickian transport mechanism.

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Development and Evaluation of a Novel Pellet-Based Tablet System for Potential Colon Delivery of Budesonide

Journal of Drug Delivery, 2012

Budesonide, a potent glucocorticoid, is used for the treatment of inflammatory bowel diseases. Cu... more Budesonide, a potent glucocorticoid, is used for the treatment of inflammatory bowel diseases. Current available oral formulations of budesonide have low efficacy against ulcerative colitis because of the premature drug release in the upper part of the gastrointestinal tract. In this paper a pH- and time-controlled colon-targeted pellet-based tablet of budesonide was established. Pellet cores were prepared by extrusion-spheronization method and further coated with xanthan gum (barrier layer), Eudragit NE30D and L30D55 combination (inner layer), and Eudragit FS30 (as enteric layer) sequentially to achieve the required release profile. The coated pellets then compressed into tablets using inert tabletting granules of Cellactose or Pearlitol. Release studies, performed in simulated gastric, intestinal, and colon pH were used in sequence to mimic the gastrointestinal transit. The influence of formulation variables like barrier layer thickness, inner layer composition, and enteric coat t...

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Enhancement of follicular delivery of finasteride by liposomes and niosomes

International Journal of Pharmaceutics, 2006

Finasteride is indicated orally in the treatment of androgenetic alopecia and some other piloseba... more Finasteride is indicated orally in the treatment of androgenetic alopecia and some other pilosebaceous unit (PSU) disorders. We wished to investigate whether topical application of finasteride-containing vesicles (liposomes and niosomes) could enhance drug concentration at the PSU, as compared to finasteride hydroalcoholic solution (HA). Liposomes consisted of phospholipid (dimyristoyl phosphatidylcholine (DMPC) or egg lecithin):cholesterol:dicetylphosphate (8:2:1, mole ratio). Niosomes were comprising non-ionic surfactant (polyoxyethylene alkyl ethers (Brij series) or sorbitan monopalmitate):cholesterol:dicetylphosphate (7:3:1, mole ratio). Vesicles were prepared by the film hydration technique and characterized with regard to the size, drug entrapment efficiency and gel-liquid transition temperature (T(c)). In vitro permeation of (3)H-finasteride through hamster flank skin was faster from hydroalcoholic solution (0.13 microg/cm(2)h) compared to vesicles (0.025-0.058 microg/cm(2)h). In vivo deposition of (3)H-finasteride vesicles in hamster ear showed that liquid-state vesicle, i.e. those made of DMPC or Brij97:Brij76 (1:1), were able to deposit 2.1 or 2.3% of the applied dose to the PSU, respectively. This was significantly higher than drug deposition by gel-state vesicles (0.35-0.51%) or HA (0.76%). Both in vitro permeation and in vivo deposition studies, demonstrated the potentials of liquid-state liposomes and niosomes for successful delivery of finasteride to the PSU.

Transfection and structural properties of phytanyl substituted gemini surfactant-based vectors for gene delivery

Physical Chemistry Chemical Physics, 2013

In this study, the transfection ability and cytotoxicity of a series of phytanyl substituted gemi... more In this study, the transfection ability and cytotoxicity of a series of phytanyl substituted gemini surfactants, rationally designed and synthesized in an attempt to create cationic surfactants that will improve transfection efficiencies of non-viral vectors was evaluated in OVCAR-3 cells at the charge ratios (N(+)/P(-)) of 2:1, 5:1, and 10:1. Particle sizes, zeta potentials, and small angle X-ray scattering (SAXS) profiles were also determined. For each gemini surfactant complex, the transfection efficiency and cytotoxicity are observed to go through a more or less well-evidenced maximum, occurring at different values of the charge ratio (N(+)/P(-)), depending on the surfactant structure. Considering both results of in vitro transfection efficiency and cytotoxicity, the optimal charge ratio to formulate the complexes containing phy-3-m was found to be 5:1. The particle size decreased, while zeta potential increased with increasing N(+)/P(-). Comparing particle size and zeta potential with transfection efficiency, no correlation between size/zeta potential and transfection ability was observed. Analysis of SAXS profiles indicates that the ability of phy-3-m delivery system to adopt multiple phases correlated well with their higher transfection efficiency in OVCAR-3 cells.

Enhanced dissolution rate of simvastatin using spherical crystallization technique

Pharmaceutical Development and Technology, 2010

Simvastatin is a hypocholestrolemic drug that is insoluble in water. Its low water solubility rat... more Simvastatin is a hypocholestrolemic drug that is insoluble in water. Its low water solubility rate limits the pharmacological effects. The aim of this study was to improve the dissolution rate of simvastatin using spherical crystallization method. The drug was dissolved in boiling dichloromethane as the good solvent. This solution was added to 5°C water as the non-solvent. After sedimentation, isopropyl acetate was added as the bridging solvent. At the end the crystals were collected and dried for 12 h in a 50°C oven. The FTIR and DSC results showed no change in the drug after crystallization process. XRPD studies showed the sharp peaks are present in the diffractograms of spherical crystals with minor reduction in height of the peaks. The particle size of spherical aggregates was about 37 μm and the dissolution efficiency of simvastatin up to 60 min increased to about 2-fold in phosphate buffer solution containing 0.5% sodium dodecyl sulfate (pH 7) using the rotating paddle method. Spherical crystals showed enhanced solubility than untreated powder possibly due to partial conversion to amorphous form. Their dissolution rate at 60 min was still 4-fold of untreated powder when stored at 25°C and 84% relative humidity for one month.

Volatile Constituents of the Leaves ofZiziphus spina-christi(L.) Willd. from Bushehr, Iran

Journal of Essential Oil Research, 2003

... from Bushehr, Iran. by Ghannadi, Alireza, Tavakoli, Naser, Mehri-Ardestani, Mozhgan. ... 11. ... more

Preparation of budesonide–dextran conjugates using glutarate spacer as a colon-targeted drug delivery system:in vitro/in vivoevaluation in induced ulcerative colitis

Journal of Drug Targeting, 2010

An oral colon-targeted formulation of budesonide was developed for treatment of ulcerative coliti... more An oral colon-targeted formulation of budesonide was developed for treatment of ulcerative colitis. Budesonide conjugates were prepared using glutarate spacer and different molecular weights (MW) of dextran and their degree of substitution (DS), solubility, and stability were examined. Drug release in the presence of rat colonic contents was studied. In vivo efficacy was studied against acetic-acid induced colitis in rat. DS was dependent on polymer MW and was 7.40 ± 0.18, 5.20 ± 0.35, and 13.80 ± 0.48 mg/100 mg conjugate for MW 10,000, 70,000, and 500,000, respectively. Solubility of drug in conjugates of MW 10,000 and 70,000 was increased and was dependent on DS. The conjugates were stable in HCl 0.1 N, phosphate buffer solutions pH 6.8, and 7.4 incubated at 37°C within 6 h and degradation rate constants were &amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;lt;0.009 h(-1). Less than 10% of budesonide was released in contents of stomach and small intestine and it was increased significantly after incubating with colonic contents. The conjugate prepared using dextran 70,000 was selected for in vivo studies that could decrease the macroscopic and microscopic scores of induced colitis compared with mesalasine and budesonide suspension.

Effectiveness of budesonide-succinate-dextran conjugate as a novel prodrug of budesonide against acetic acid-induced colitis in rats

International Journal of Colorectal Disease, 2010

Anti-inflammatory drugs with high potency and low systemic adverse effects, such as budesonide, a... more Anti-inflammatory drugs with high potency and low systemic adverse effects, such as budesonide, are drugs of choice for the treatment of ulcerative colitis (UC). Budesonide controlled-release formulations are now being used to induce and maintain clinical remission of Crohn&amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;#39;s disease. Budesonide-dextran conjugates were synthesized as novel prodrugs of budesonide for oral controlled delivery of the major part of the drug to the colon without needing to coat the pellets of the drug. The aim of this study was to evaluate the in vivo efficacy of this conjugate against acetic acid-induced colitis in rats. Experimental UC was induced by rectal instillation of 4% solution of acetic acid to rats. After induction of colitis, rats were treated with vehicle (dextran solution), mesalasine (120 mg/kg), budesonide suspension (300 microg/kg) and BSD-70 (equivalent to 300 microg/kg of budesonide), prednisolon (4 mg/kg), hydrocortisone acetate enema (20 mg/kg), and 5-ASA enema (Asacol) (400 mg/kg) for 5 days and then colon macroscopic and microscopic sections were examined for inflammatory response. Vehicle-treated rats presented bloody diarrhoea and gross lesions. The effective formulations for attenuating the damage were BSD-70, oral prednisolon and hydrocortisone acetate enema. Rats treated with BSD-70 showed huge improvement in macroscopic and histological scores of colitis compared to the negative control group and mesalasine and budesonide suspension. Data indicated that budesonide-dextran conjugate is effective in improving signs of inflammation in experimental model of colitis through selective delivery of the drug to the inflamed area.

Preparation and in vitro/in vivo evaluation of dextran matrix tablets of budesonide in experimental ulcerative colitis in rats

Drug Delivery, 2010

Budesonide is an anti-inflammatory drug of choice for treatment of ulcerative colitis which affec... more Budesonide is an anti-inflammatory drug of choice for treatment of ulcerative colitis which affects the rectum and a part of or the entire colon. Delivery of budesonide specifically to the colon would increase the efficacy of the drug and reduce the side-effects. The aim of this study was to develop an oral matrix system formulation for budesonide to deliver the major part of the drug to the colon for treatment of ulcerative colitis that has not been reported before. Directly compressed matrix tablets were prepared using different molecular weights of dextran and three ratios of drug-to-polymer. The physical properties of the tablets including weight variation, hardness, content uniformity, and release profile in HCl 0.1 N, phosphate buffer pH 7.4 and 6.8 containing 4% rat caecal and colonic contents were studied. The efficacy of the desired formulation was also evaluated against acetic acid-induced colitis in rats. Physical properties of the tablets were in the ranges recommended by official references. More than 10% of the drug was released in HCl 0.1 N and pH 7.4, while a very drastic increase was observed after exposure to pH 6.8 containing rat caecal contents. The efficacy of the selected formulation against rat-induced colitis was also increased in comparison to the non-targeted formulation of budesonide. In conclusion, matrix tablets with a 1:10 drug-to-dextran ratio with high molecular weight could deliver the drug specifically to the colon and are promising for treatment of ulcerative colitis.

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Preparation of Diltiazem Topical Gel for the Treatment of Anal Fissure and In-Vitro, Ex-Vivo Drug Release Evaluations

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Drug Release Evaluation of Ibuprofen Sugar Coated and Film Coated Tablets Marketed in Iran

Download

Gastric Floating Matrix Tablets of Metformin Hcl : Design and Optimization Using Combination of Polymers

Simvastatin nanosuspensions prepared using a combination of pH-sensitive and timed-release approaches for potential treatment of colorectal cancer

Pharmaceutical Development and Technology, 2021

An injectable carboxymethyl chitosan-methylcellulose-pluronic hydrogel for the encapsulation of meloxicam loaded nanoparticles

International Journal of Biological Macromolecules, 2020

et al., An injectable carboxymethyl chitosan-methylcellulose-pluronic hydrogel for the encapsulat... more

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Alginate hydrogel enriched with Ambystoma mexicanum epidermal lipoxygenase-loaded pectin nanoparticles for enhanced wound healing

Journal of Biomaterials Applications, 2019

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Formulation and evaluation of licorice shampoo in comparison with commercial shampoo

Journal of Pharmacy And Bioallied Sciences, 2018

Transdermal iontophoretic delivery of celecoxib from gel formulation

Research in pharmaceutical sciences

Download

Formulation of sustained - release lithium carbonate matrix tablets: influence of hydrophilic materials on the release rate and in vitro-in vivo evaluation

Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Société canadienne des sciences pharmaceutiques, Jan 15, 2004

Download

Evaluating the effect of magnesium and magnesium plus vitamin B6 supplement on the severity of premenstrual syndrome

Iranian journal of nursing and midwifery research, 2010

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Calorimetric Investigations of Non-Viral DNA Transfection Systems

Thermodynamics - Kinetics of Dynamic Systems, 2011

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Application of Taguchi Method to Investigate the Drug Release Behavior of Poly(Acrylamide-co-Maleic Acid)/Montmorillonite Nanocomposite Hydrogels

Advances in Polymer Technology, 2014

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Development and Evaluation of a Novel Pellet-Based Tablet System for Potential Colon Delivery of Budesonide

Journal of Drug Delivery, 2012