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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

Release of Vildagliptin from microspheres prepared by emulsion solvent evaporation technique, respectively, where (a) zero order is from VF1 to VF3, (b) first order is from VF4 to VF6, (c) Higuchi model is from VF10 to VF12, and (d) Korsmeyer model is from VF13 to VF5.
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fig4: Release of Vildagliptin from microspheres prepared by emulsion solvent evaporation technique, respectively, where (a) zero order is from VF1 to VF3, (b) first order is from VF4 to VF6, (c) Higuchi model is from VF10 to VF12, and (d) Korsmeyer model is from VF13 to VF5.

Mentions: Vildagliptin microspheres were prepared by polymeric concentration variation to study the effect of combination of polymers on the release of drug from microspheres. Formulations VF1 to VF3 were prepared by using Eudragit RS100 and Ethyl cellulose. After the end of 8 hours of dissolution, the release drug from microspheres was 87.5%, 85.7%, and 84.5%, respectively, which is shown in Figure 4(a). Formulations VF4 to VF6 were prepared by using Eudragit RL100 and Ethyl cellulose. After the end of 8 hours of dissolution, the release drug from microspheres was 86.6%, 88.2%, and 90.2%, respectively, which is shown in Figure 4(b). Formulations VF10 to VF12 were prepared by using Eudragit RS100 and Methocel K100M. After the end of 8 hours of dissolution, the release drug from microspheres was 88.0%, 81.1%, and 68.5%, respectively, which is shown in Figure 4(c). Formulations VF13 to VF15 were prepared by using Eudragit RL100 and Methocel K100M. After the end of 8 hours of dissolution, the release drug from microspheres was 92.4%, 85.5%, and 81.23%, respectively, which is shown in Figure 4(d).


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)

Release of Vildagliptin from microspheres prepared by emulsion solvent evaporation technique, respectively, where (a) zero order is from VF1 to VF3, (b) first order is from VF4 to VF6, (c) Higuchi model is from VF10 to VF12, and (d) Korsmeyer model is from VF13 to VF5.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig4: Release of Vildagliptin from microspheres prepared by emulsion solvent evaporation technique, respectively, where (a) zero order is from VF1 to VF3, (b) first order is from VF4 to VF6, (c) Higuchi model is from VF10 to VF12, and (d) Korsmeyer model is from VF13 to VF5.
Mentions: Vildagliptin microspheres were prepared by polymeric concentration variation to study the effect of combination of polymers on the release of drug from microspheres. Formulations VF1 to VF3 were prepared by using Eudragit RS100 and Ethyl cellulose. After the end of 8 hours of dissolution, the release drug from microspheres was 87.5%, 85.7%, and 84.5%, respectively, which is shown in Figure 4(a). Formulations VF4 to VF6 were prepared by using Eudragit RL100 and Ethyl cellulose. After the end of 8 hours of dissolution, the release drug from microspheres was 86.6%, 88.2%, and 90.2%, respectively, which is shown in Figure 4(b). Formulations VF10 to VF12 were prepared by using Eudragit RS100 and Methocel K100M. After the end of 8 hours of dissolution, the release drug from microspheres was 88.0%, 81.1%, and 68.5%, respectively, which is shown in Figure 4(c). Formulations VF13 to VF15 were prepared by using Eudragit RL100 and Methocel K100M. After the end of 8 hours of dissolution, the release drug from microspheres was 92.4%, 85.5%, and 81.23%, respectively, which is shown in Figure 4(d).

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