Sneha Shome, (2019) Formulation and Evaluation of Gliclazide Microsponge Drug Delivery System. Masters thesis, C.L.Baid Metha College of Pharmacy, Chennai..
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Abstract
Oral drug delivery via polymer systems has been proposed to be prevailing in the type of controlled drug delivery devices both in present and future. For scientific as well as economic reasons, such delivery systems have potential advantage which include enhanced therapeutic response, predictable rate of release, less side effects and extent of absorption and better patience compliance. In the present work an oral delivery microsponge formulation of a very stable and potent antidiabetic drug, Gliclazide has been developed. The study includes formulation and evaluation of Gliclazide microsponges. The idea behind developing an oral polymeric microsponge delivery system of Gliclazide was to deliver Gliclazide in a controlled release pattern for a long period of time up to 12 hours in order to reduce dose frequency and improve patience compliance. Box-Behnken statistical design with 3 factors, 3 levels and 17 runs were employed for the optimization study using design-expert software version 7.0. The variables stirring speed, polymer Ethyl cellulose and eudragit RS 100 were main factors that impacted the particle size, entrapment efficiency and production yield in our microsponge formulation in our preliminary experiments. To investigate the impact of stirring speed(A), Ethyl cellulose in mg (B) and eudragit RS 100 in mg (C) were selected as independent variables and they were set at high, medium and low level on the basis of the results of initial trials. In accordance with the design ,17 microsponge formulations were prepared and characterized for particle size (R1, entrapment efficiency (R2) and production yield (R3). However, five set of formulations were selected from given 17 runs of formulations since those five showed better response. The ratio of polymer:polymer for the formulation of Gliclazide microsponge was varied in formulation and then the microsponges were evaluated for drug content, encapsulation efficiency, particle size, x -ray diffraction study, morphological study by SEM, and invitro release study. Further, the analysis of release mechanisms was carried out by fitting the release data to various kinetic equations like, zero order, first order Korsmeyer-Peppas, Higuchi(matrix) and Hixson crowell equations and the best fit model describing the release pattern was determined. It shows that the release of drug from the microsponges follow Higuchi order diffusion model with non-fickian transport mechanism. The results obtained from the optimization technique was incorporated in our experimental value and signified that stirring speed of 1300 rpm, Ethyl cellulose of 20mg and eudragit RS 100 of 80mg was found to produce microsponges with good physical and morphological characters. Therefore, our optimized formulation F3 was significantly in accordance with the formulation derived from the optimization technique, values varying little, and stirring speed was not inputted in the formulation code in the end because this independent variable could be easily controlled practically. The release rate of drug from varying concentrations of polymeric microsponges shows that the release of drug increase with increasing concentration of polymers. By considering all the results obtained, F3 was found to be best formulation amongst all the other. However, in invitro study, F4 too showed a better result. The results of swelling study revealed that the swelling index of all the formulations from F1 – F5 increased with higher concentration of eudragit RS 100 since it being a hydrophilic polymer. F3 showed an adequate % of swelling index thus making it an appropriate option. However, in vivo experiments are essential to establish the actual usefulness of these microsponges. CONCLUSION: An oral delivery microsponge formulation of Gliclazide was formulated using two types of polymers Ethyl cellulose and eudragit RS 100. From the study the following conclusion can be drawn. ❖ The amount of internal phase that is Dichloromethane was selected at 15ml depending on the previous researches suitable for the preparation of microsponges and the external phase was found to be distilled water oaf 100ml. ❖ The concentrations of the polymers required to produce microsponges with good physical and morphological characteristics was found to be 20mg of Ethyl cellulose and 80mg of eudragit RS 100 in accordance the optimum amount derived from the optimization technique with little variation in the main formulation. ❖ The stirring speed was found out to be 1300rpm for 1 hour from the optimization technique to check how it affects the particle size, however it was not inputted in the main formulation as it can controlled while in the experiments. ❖ The ratio of polymer:polymer required to produce microsponges with good encapsulation efficiency was found to be at 1:3 below this ratio, microsponges formed had low capacity encapsulation efficiency of drug and low production yield and above thus range, there was also further increase in the encapsulation efficiency but the particle size increased. Hence, it was concluded that at 1:3 polymer: polymer ratio, was an optimum ratio of polymer ratio to produce good microsponges. ❖ By the drug release studies of formulation F1 to F5, it was concluded that the release profile of F3 and F4 was in controlled fashion. ❖ By model fitting of the date obtained by drug release profile, we can conclude that the mechanism of drug release from microsponge showed Higuchi order kinetic drug release model, was non fickian transport mechanism. ❖ Finally, we may conclude that formulation F3 was best formulation in the class of Ethyl cellulose of 20mg and eudragit RS 100 of 80mg as retarding polymers.
| Item Type: | Thesis (Masters) |
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| Additional Information: | 261710011 |
| Uncontrolled Keywords: | Formulation, Evaluation, Gliclazide Microsponge, Drug Delivery System. |
| Subjects: | PHARMACY > Pharmaceutics |
| Depositing User: | Ramakrishnan J |
| Date Deposited: | 04 Dec 2021 06:06 |
| Last Modified: | 22 Mar 2022 07:38 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/18809 |
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