%0 Journal Article
%T Formulation of a Novel Nanoemulsion System for Enhanced Solubility of a Sparingly Water Soluble Antibiotic, Clarithromycin
%A Stuti Vatsraj
%A Kishor Chauhan
%A Hilor Pathak
%J Journal of Nanoscience
%D 2014
%R 10.1155/2014/268293
%X The sparingly water soluble property of majority of medicinally significant drugs acts as a potential barrier towards its utilization for therapeutic purpose. The present study was thus aimed at development of a novel oil-in-water (o/w) nanoemulsion (NE) system having ability to function as carrier for poorly soluble drugs with clarithromycin as a model antibiotic. The therapeutically effective concentration of clarithromycin, 5£¿mg/mL, was achieved using polysorbate 80 combined with olive oil as lipophilic counterion. A three-level three-factorial central composite experimental design was utilized to conduct the experiments. The effects of selected variables, polysorbate 80 and olive oil content and concentration of polyvinyl alcohol, were investigated. The particle size of clarithromycin for the optimized formulation was observed to be 30£¿nm. The morphology of the nanoemulsion was explored using transmission electron microscopy (TEM). The emulsions prepared with the optimized formula demonstrated good physical stability during storage at room temperature. Antibacterial activity was conducted with the optimized nanoemulsion NESH 01 and compared with free clarithromycin. Zone of inhibition was larger for NESH 01 as compared to that with free clarithromycin. This implies that the solubility and hence the bioavailability of clarithromycin has increased in the formulated nanoemulsion system. 1. Introduction The increasing frequency of poorly soluble new chemical entities exhibiting therapeutic activity is of major concern to the pharmaceutical industry [1]. These drugs are difficult to process or administer to patients due to poor dissolution. This is the major hurdle that prevents the commercialization of poorly water soluble drugs. There are various techniques available to improve the solubility of such drugs. One of them includes formulation of emulsions using a biocompatible emulsifier to disperse oil in an aqueous phase and is widely used for drug delivery [2¨C6]. The emulsions are usually biocompatible, biodegradable, physically stable (particularly nanoemulsions and microemulsions), and relatively easy to produce on a large scale [7]. Nanoemulsions (NEs) can be defined as nonequilibrium, heterogeneous systems consisting of two immiscible liquids in which one liquid is dispersed in another liquid as droplets with diameters of tens to a few hundred nanometers [8]. The major advantages of nanoemulsions as drug delivery carriers include ease of fabrication, increased drug loading, enhanced drug solubility and bioavailability, reduced patient variability,
%U http://www.hindawi.com/journals/jns/2014/268293/