Formulation and Evaluation of Controlled Release Floating Microballoons of Stavudine.

Suryadevara Vidyadhara

doi:10.3797/scipharm.1501-07

Abstract

The aim of this study was to formulate and evaluate stavudine floating microballoons for controlled drug release. Initially, the drug-loaded low-density granular pellets were prepared with hydroxypropyl methylcellulose E5 grade and by using isopropyl alcohol as a granulating fluid. Further, the low-density granular pellets were subjected to microencapsulation by an emulsion evaporation technique using ethyl cellulose 7 cps and Eudragit S 100 as coating polymers and 1% w/v polyethylene glycol 400 as aqueous phase. The prepared microballoons were characterized for their particle size analysis, angle of repose, and compressibility index. The in vitro release studies were performed in 0.1 N HCl as medium. The prepared microballoons were free-flowing and spherical in shape. From all the formulations, F5E and F5F can be considered as promising controlled release floating microballoons of stavudine providing first-order release over a period of 12 hours, with a minimum floating lag time of 1 minute. It was found that the ratio of the drug & polymer, stirring speed, and concentration of surfactant were the most significant variables which influenced the size of the stavudine microballoons under the applied experimental conditions.

Highlights

Drugs that have good absorption in the gastrointestinal tract (GIT) and a short half-life are eliminated quickly from systemic circulation
Among the prepared low-density granular pellets, formulation F5 containing the drug : HPMC E5 in the ratio of 1:5 showed a floating lag time of 15 sec and in vitro drug release up to 2 hr. This formulation was optimized for preparing microballoons employing Eudragit RS 100 & ethyl cellulose 7 cps as coating polymers and 1% w/v PEG 400 as the aqueous phase
Stavudine controlled release floating microballoons were prepared by the solvent evaporation process

Summary

Introduction

Drugs that have good absorption in the gastrointestinal tract (GIT) and a short half-life are eliminated quickly from systemic circulation. These types of drugs require frequent dosing. To overcome these problems, oral controlled release (CR) formulations have been developed. Oral controlled release (CR) formulations have been developed In this regard, controlled drug delivery systems have many benefits, which include improved therapy by increasing the efficacy and gastrointestinal transit time, increased patient compliance through decreased dosing frequency, convenient routes of administration, and improved site-specific delivery to reduce unwanted adverse effects [1, 2].

Objectives

Findings

Discussion

Conclusion