Fabrication and Characterization of Gliclazide Loaded Microcapsules

Asad, Muhammad Usman; Bashir, Sajid; Mahmood, Tariq; Imran, Muhammad; Karim, Sabiha; Hassnain, Fakhar ul

doi:10.1590/s1516-8913201402505

Cited by 4 publications

(3 citation statements)

References 10 publications

(10 reference statements)

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“…The data indicate more linearity when plotted by the zero-order kinetic model. Hence, it can be concluded that the major mechanism of drug release follows zero-order kinetics [21].…”

Section: Resultsmentioning

confidence: 98%

Formulation and Evaluation of Gliclazide Nanosponges

Solunke¹,

Borge²,

Murthy³

et al. 2019

Int J App Pharm

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Objective: The objective of the present study was to develop and characterize an optimal stable nanosponges of Gliclazide (GLZ) by using the emulsion solvent diffusion method and aimed to increase its bioavailability and release the drug in sustained and controlled manner. Methods: The GLZ nanosponge was prepared by emulsion solvent diffusion method using different drug-polymer ratios (1:1 to 1:5) Eudragit S100 is used as a polymer. Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) estimated the compatibility of GLZ with polymer. All formulations evaluated for production yield, entrapment efficiency, in vitro drug release, scanning electron microscopy (SEM) and stability studies. Results: The DSC and FTIR Studies revealed that no interaction between drug and polymer. The Production yield of all batches in the range of 73.8±0.30 to 85.6±0.32. Batch F3 showed the highest production yield, the entrapment efficiency of batch F3 70.6±0.77. The average particle size ranges from 303±2.36 to 680±2.50 nm. By the end of 10th hour F3 formulation shown highest drug release was found to be 94.40±1.12%. The release kinetics of the optimized formulation shows zero-order drug release. The stability study indicates no significant change in the in vitro dissolution profile of optimized formulation. Conclusion: The results of various evaluation parameters, revealed that GLZ nanosponges would be possible alternative delivery systems to conventional formulation to improve its bioavailability, the emulsion solvent diffusion method is best method for preparation of nanosponges and release the drug in sustained and controlled manner.

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“…The data indicate more linearity when plotted by the zero-order kinetic model. Hence, it can be concluded that the major mechanism of drug release follows zero-order kinetics [21].…”

Section: Resultsmentioning

confidence: 98%

Formulation and Evaluation of Gliclazide Nanosponges

Solunke¹,

Borge²,

Murthy³

et al. 2019

Int J App Pharm

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“…All analysis was done in triplicate, then the average ± SD was calculated using Microsoft office, 2010. 14…”

Section: Evaluation Of the Entrapment Efficiency (Ee)mentioning

confidence: 99%

Effect of Ethyl Cellulose Content on Release Profile and Pharmacodynamics of Fenoprofen Microparticles

Aboueisha¹,

Gad²,

Khalil³

et al. 2019

IJPER

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Introduction: Fenoprofen calcium (FC) is a non-steroidal anti-inflammatory drug and due to its short half-life, high absorption, extensive metabolism and adverse effect, sustained release formulation of FC is desired. Objective: this study was to develop sustained release microcapsules of FC to obtain better drug delivery. Material and Methods: Different formulae of FC microcapsules were prepared by o/w emulsion solvent evaporation method using Ethyl cellulose (EC) in three different ratios. The processed microcapsules were evaluated in-vitro for production yield, entrapment efficiency, micromeritic properties and thermal characteristics and in-vivo for its pharmacodynamics. Results: In-vitro release studies of formulae H1 and H3 showed regression coefficient (r) value in the Higuchi diffusion model of 0.967 and 0.946 respectively, suggesting diffusion mechanism release from these forms. While marketed capsules and H2 microcapsules showed regression coefficient value in the zero-order model (0.985 and 0.985 respectively), suggesting non-linear release. In-vivo, the carrageenan-induced hind paw edema was induced in rats; the area under the inhibition of inflammation percentage-time curve (AUC0-24) showed that formula H3 possesses the highest therapeutic efficiency comparing with marketed capsules followed by formula H1 and finally H2. Moreover, in hot plate test in mice, there were highly significant increases in the mean reaction time in groups H2 and H3 over the marketed capsule at 12h interval (p<0.001). Conclusion: FC loaded EC microcapsule H3 produced a sustained and effective drug release over a prolonged timeframe that led to greater therapeutic efficacy.

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“…Gliclazide is a member of second-generation sulfonylureas ( Figure 1) and is primarily used as an oral hypoglycemic drug in NIDDM (non-insulin-dependent diabetes mellitus). İt produces an antidiabetic effect through selectively inhibiting pancreatic K + ATP channels [8].…”

Section: Introductionmentioning

confidence: 99%

Influence of Ocimum sanctum (L.) Extract on the Activity of Gliclazide in Alloxan-induced Diabetes in Rats

Ramzan¹,

Aslam²,

Muhammad³

et al. 2020

Rev. Chim.

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Ocimum sanctum L. is widely used as traditional remedy to manage hyperglycemia. This study was aimed to evaluate the effect of aqueous-methanolic extract of O. sanctum leaves (OSE) on the anti-diabetic activity of gliclazide in alloxan-induced diabetes in Wistar rats. Diabetes was induced by intraperitoneally injecting alloxan (120 mg/kg b.w.) in rats. Treatments including OSE (100 mg/kg b.w.), gliclazide (100 mg/kg b.w.), and in combination were given daily to diabetic rats till the 21st day of study. Body weight and fasting blood glucose levels were determined at regular intervals, while blood and organ samples were taken at the end of the study for biochemical and histopathological studies. Results showed that treatments exhibited anti-hyperglycemic activity through significantly (p [ 0.05) restoring body weight, fasting blood glucose level, and serum levels of glucose, insulin and HbA1c. The anti-lipidemic activity was noticed as total cholesterol (TC), triglyceride (TG), high-/low density-lipoproteins (HDL-C, LDL-C) levels were restored in treated diabetic rats. Ameliorative effects of treatments were observed as significant (p [ 0.05) reduction in serum levels of liver function biomarkers (alanine aminotransferase; ALT, aspartate aminotransferase; AST, alkaline phosphatase; ALP and bilirubin; BIL) and restoration of oxidative stress biomarkers (catalase; CAT, superoxide dismutase; SOD and malondialdehyde; MDA) in liver tissue. Histopathological findings supported these results as an increase in pancreatic islets size and protective effects on liver tissue was observed in diabetic rats treated with gliclazide and OSE alone and their combination. Conclusively, the combination of OSE and gliclazide produced a synergistic anti-diabetic effect as compared to that of alone treatment.

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Fabrication and Characterization of Gliclazide Loaded Microcapsules

Abstract: ABSTRACT

Cited by 4 publications

References 10 publications

Formulation and Evaluation of Gliclazide Nanosponges

Formulation and Evaluation of Gliclazide Nanosponges

Effect of Ethyl Cellulose Content on Release Profile and Pharmacodynamics of Fenoprofen Microparticles

Influence of Ocimum sanctum (L.) Extract on the Activity of Gliclazide in Alloxan-induced Diabetes in Rats

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