Abstract

Aims: The aim of this work is the formulation of Eudragit RL100 polymeric microsponges. The Microsponge Delivery System is a patented technique in which there is a polymeric system consisting of porous particles.
 Methodology: The ratio of Diclofenac sodium and eudragit RL100 varied from 1:1 to 13: 1 to formulate microsponge. Dichloromethane was used as internal phase and polyvinylalcohol was used as an external phase. The formed microsponges were characterized for particle size, entrapment efficiency, drug content, in vitro drug release and SEM.
 Results: With increase in drug: polymer ratio there is increase in production yield from 20.04% to 72.14%, and entrapment efficiency from 20.11% to 70.77%. Drug content of formed microsponge varied between 50.18% to 91.09% whereas particle size ranged from 1.41 µm to 17.66 µm. Microsponge formulations F3, F4 and F5 showed desired particle size hence studied for further evaluation. Formulation F3, F4 and F5 showed controlled release of 89.54%, 98.5% and 98.76% respectively up to 6 hr. F3 showed more controlled release at the end of 6 hr. The drug release from microsponges was best fitted to Higuchi’s diffusion kinetics for all microsponge formulations with non-Fickian diffusion mechanism. The formed microsponge particles have spherical porous structure.
 Conclusion: Study showed significance of Microsponge Delivery System for ophthalmic administration.

Highlights

  • The Microsponge Delivery System (MDS) is a patented technique in which there is a polymeric system consisting of porous particles

  • This study aims at formulation of Diclofenac sodium containing microsponges for ophthalmic use

  • Diclofenac sodium containing microsponges were prepared by the quasi emulsion solvent diffusion method using Eudragit RL 100 polymer

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Summary

INTRODUCTION

The Microsponge Delivery System (MDS) is a patented technique in which there is a polymeric system consisting of porous particles. They have tiny sponge like rounded particles, having a countless interconnecting voids. Ocular drug delivery is a challenge for pharmaceutical researchers due to the complex nature and structure of the eye. Most drugs are formulated as simple eye drops and ointments for ophthalmic use. More than 90% of ocular preparations are formulated as Eye drops. At physiologic conditions eudragit RL 100 is insoluble It is capable of mucoadhesion at ocular site for prolong period of time [8,9]. This study aims at formulation of Diclofenac sodium containing microsponges for ophthalmic use.

Materials
Preparation of Diclofenac sodium Loaded Microsponges
Determination of percentage yield
In Vitro Drug Release from Diclofenac Sodium Loaded Microsponges
Drug content
Particle size
F2 F3 F4 F5 F6 F7
CONCLUSION
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