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Characterization and Compatibility Studies of Different Rate Retardant Polymer Loaded Microspheres by Solvent Evaporation Technique: In Vitro-In Vivo Study of Vildagliptin as a Model Drug.

Dewan I, Islam S, Rana MS - J Drug Deliv (2015)

Bottom Line: The SEM, DSC, and FTIR studies have been done to confirm good spheres and smooth surface as well as interaction along with drug and polymer.In this experiment, it is difficult to explain the exact mechanism of drug release.At last it can be concluded that all in vitro and in vivo experiments exhibited promising result to treat type II diabetes mellitus with Vildagliptin microspheres.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, Jahangirnagar University, Savar 1342, Dhaka, Bangladesh ; Department of Pharmacy, University of Asia Pacific, Dhanmondi, Dhaka 1209, Bangladesh.

ABSTRACT
The present study has been performed to microencapsulate the antidiabetic drug of Vildagliptin to get sustained release of drug. The attempt of this study was to formulate and evaluate the Vildagliptin loaded microspheres by emulsion solvent evaporation technique using different polymers like Eudragit RL100, Eudragit RS100, Ethyl cellulose, and Methocel K100M. In vitro dissolution studies were carried out in 0.1 N HCl for 8 hours according to USP paddle method. The maximum and minimum drug release were observed as 92.5% and 68.5% from microspheres, respectively, after 8 hours. Release kinetics were studied in different mathematical release models to find out the linear relationship and release rate of drug. The SEM, DSC, and FTIR studies have been done to confirm good spheres and smooth surface as well as interaction along with drug and polymer. In this experiment, it is difficult to explain the exact mechanism of drug release. But the drug might be released by both diffusion and erosion as the correlation coefficient (R (2)) best fitted with Korsmeyer model and release exponent (n) was 0.45-0.89. At last it can be concluded that all in vitro and in vivo experiments exhibited promising result to treat type II diabetes mellitus with Vildagliptin microspheres.

No MeSH data available.


Related in: MedlinePlus

Effect of drug on lipid profile of control and experimental groups.
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Related In: Results  -  Collection


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fig11: Effect of drug on lipid profile of control and experimental groups.

Mentions: STZ diabetic rats were found to have significantly elevated serum creatinine and urea levels as compared to nondiabetic control rats. This is because STZ diabetic rats have diminished ability to filter urea and creatinine from blood and excrete them in urine. This is another characteristic change in diabetes. Whereas after treatment both the values were comparable to those which received Vildagliptin treatment, there was no significant difference in values obtained for group I and group IV shown in Figure 10. Various parameters of blood lipid profiles were tested in the normal and diabetic rats. The levels of TC and TG were significantly elevated and level of serum HDL was decreased in diabetic control group as compared to normal control rats. In case of insulin deficiency, there is increased lipolysis leading to hyperlipidemia. In insulin deficient diabetes, the concentration of free fatty acids is elevated as a result of free fatty acid outflow from fat depots, where the balance of free fatty acid esterification-triglyceride lipolysis cycle is displaced in favor of lipolysis. It has been shown from Figure 11 that, after being treated with formulation VF13, the alteration in lipid metabolism was partially attenuated as evidenced by decreased serum TG and TC levels in diabetic rats.


Characterization and Compatibility Studies of Different Rate Retardant Polymer Loaded Microspheres by Solvent Evaporation Technique: In Vitro-In Vivo Study of Vildagliptin as a Model Drug.

Dewan I, Islam S, Rana MS - J Drug Deliv (2015)

Effect of drug on lipid profile of control and experimental groups.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4660022&req=5

fig11: Effect of drug on lipid profile of control and experimental groups.
Mentions: STZ diabetic rats were found to have significantly elevated serum creatinine and urea levels as compared to nondiabetic control rats. This is because STZ diabetic rats have diminished ability to filter urea and creatinine from blood and excrete them in urine. This is another characteristic change in diabetes. Whereas after treatment both the values were comparable to those which received Vildagliptin treatment, there was no significant difference in values obtained for group I and group IV shown in Figure 10. Various parameters of blood lipid profiles were tested in the normal and diabetic rats. The levels of TC and TG were significantly elevated and level of serum HDL was decreased in diabetic control group as compared to normal control rats. In case of insulin deficiency, there is increased lipolysis leading to hyperlipidemia. In insulin deficient diabetes, the concentration of free fatty acids is elevated as a result of free fatty acid outflow from fat depots, where the balance of free fatty acid esterification-triglyceride lipolysis cycle is displaced in favor of lipolysis. It has been shown from Figure 11 that, after being treated with formulation VF13, the alteration in lipid metabolism was partially attenuated as evidenced by decreased serum TG and TC levels in diabetic rats.

Bottom Line: The SEM, DSC, and FTIR studies have been done to confirm good spheres and smooth surface as well as interaction along with drug and polymer.In this experiment, it is difficult to explain the exact mechanism of drug release.At last it can be concluded that all in vitro and in vivo experiments exhibited promising result to treat type II diabetes mellitus with Vildagliptin microspheres.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, Jahangirnagar University, Savar 1342, Dhaka, Bangladesh ; Department of Pharmacy, University of Asia Pacific, Dhanmondi, Dhaka 1209, Bangladesh.

ABSTRACT
The present study has been performed to microencapsulate the antidiabetic drug of Vildagliptin to get sustained release of drug. The attempt of this study was to formulate and evaluate the Vildagliptin loaded microspheres by emulsion solvent evaporation technique using different polymers like Eudragit RL100, Eudragit RS100, Ethyl cellulose, and Methocel K100M. In vitro dissolution studies were carried out in 0.1 N HCl for 8 hours according to USP paddle method. The maximum and minimum drug release were observed as 92.5% and 68.5% from microspheres, respectively, after 8 hours. Release kinetics were studied in different mathematical release models to find out the linear relationship and release rate of drug. The SEM, DSC, and FTIR studies have been done to confirm good spheres and smooth surface as well as interaction along with drug and polymer. In this experiment, it is difficult to explain the exact mechanism of drug release. But the drug might be released by both diffusion and erosion as the correlation coefficient (R (2)) best fitted with Korsmeyer model and release exponent (n) was 0.45-0.89. At last it can be concluded that all in vitro and in vivo experiments exhibited promising result to treat type II diabetes mellitus with Vildagliptin microspheres.

No MeSH data available.


Related in: MedlinePlus