Abstract

The aim of the present study was to develop an optimized niosome formulation for the encapsulation of a poorly water-soluble drug by the ecological probe sonication method. Pluronic L121 and Span 60 were used as surface active agents and the optimization of the composition was made with the aid of Design of Experiment (DoE) concept. Rifampicin was used as a model drug. Concentration levels of charge inducing agent, dicetylphosphate (DCP), and Pluronic L121 were studied as variables. Prepared niosomes with varying concentrations of DCP and Pluronic L121 resulted in small sized niosomes with sizes ranging from 190 nm to 893 nm. During the four weeks stability testing, the particle sizes were reduced slightly. The formulation containing 2 mg of DCP resulted in most stable niosomes with 75.37% entrapment efficiency. All the niosomal formulations showed higher in vitro drug release rates as compared to bulk drug formulation. As a conclusion, rifampicin loaded niosomes prepared with Pluronic L121 and Span 60 resulted in stable, small sized niosomes with improved drug release profile.

Highlights

  • Niosomes are self-organizing non-ionic surfactant vesicles, which encapsulate aqueous volume of drug(s) with or without the addition of cholesterol and other lipid contents [1,2]

  • Preparation of rifampicin niosomes For production of niosomes by probe sonication method [19], rifampicin was first mixed with 15 mL of water with the help of magnetic stirrer, after which cholesterol, Span 60, Pluronic L121 and DCP were added

  • Rifampicin loaded niosomes were prepared with the combination of surfactants Span 60 and Pluronic L121

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Summary

Introduction

Niosomes are self-organizing non-ionic surfactant vesicles, which encapsulate aqueous volume of drug(s) with or without the addition of cholesterol and other lipid contents [1,2]. Niosomes have the capability to encapsulate both lipophilic and hydrophilic drugs [3]. They are alternative to liposomes, and their main benefits as compared to liposomes are their lower price, higher stability and better biodegradability [4]. Poloxamers are widely utilized pharmaceutical excipients, though they are less studied in formulating niosomes They are well known to improve the solubility of poorly soluble drugs via solubilization effect [14,15] and they are functioning as permeation enhancers [16], and good candidates for excipients in niosomal formulations

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