Abstract
Rifampicin biodegradable microcapsules were prepared by feasible emulsification-ionic gelation method for a novel controlled release product. Sodium alginate and Carbopol 974P were used as coating polymers in different ratios 1:1, 1:2, 1:3 and 1:4 to obtain elegant microcapsules. The formulations were characterized for encapsulation efficiency, drug loading, sieve analysis, scanning electron microscopy and in vitro release studies. The microcapsules were discrete, large, almost spherical and free flowing with encapsulation efficiency in the range of 75% to 89%, drug loading 75% to 86% and size 440 μm to 500 μm. Rifampicin release from these microcapsules was slow and extended over longer periods of time depending on the polymer coat. Drug release was diffusion controlled and followed first order kinetics. The formulation MC1 with a coating ratio of 1:1 (Sodium alginate: Carbopol 974P) was found to be suitable for oral controlled release.
Highlights
Controlled release dosage forms are becoming increasingly important, either to achieve the desired level of therapeutic activity required for a new drug entity or to extend life cycle of an existing drug through improved performance or patient compliance
Rifampicin, a semi synthetic hydrazine derivative of rifampicin B was chosen for the study because it is one of the established first-line drugs used to treat tuberculosis and its biological half-life varies from 1.5 to 5 h
The soluble sodium alginate was cross-linked with calcium chloride, resulting in the formation of the insoluble calcium alginate
Summary
Sodium alginate and Carbopol 974P were used as coating polymers in different ratios 1:1, 1:2, 1:3 and 1:4 to obtain elegant microcapsules. The microcapsules were discrete, large, almost spherical and free flowing with encapsulation efficiency in the range of 75% to 89%, drug loading 75% to 86% and size 440 μm to 500 μm Rifampicin release from these microcapsules was slow and extended over longer periods of time depending on the polymer coat. The soluble sodium alginate was cross-linked with calcium chloride, resulting in the formation of the insoluble calcium alginate This strong thermo stable gel has properties that largely depend on the characteristics of the polymer and the preparation method[7,8,9]. The results obtained were fitted according to the TABLE 1: CHRACTERISTICS OF THE PREPARED MICROCAPSULES
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