%0 Journal Article
%T Screening of Most Effective Variables for Development of Gastroretentive Mucoadhesive Nanoparticles by Taguchi Design
%A Ankit Anand Kharia
%A Akhlesh Kumar Singhai
%J ISRN Nanomaterials
%D 2013
%R 10.1155/2013/348095
%X The objective of this study was the selection of the most influential variable for the preparation of gastroretentive mucoadhesive nanoparticles of acyclovir. Nanoparticles were prepared by one-step desolvation method; effect of formulation and processing variables on various response variables were studied by a Taguchi standard orthogonal array L8 design. Independent variables studied were the amount of gelatin, amount of glutaraldehyde, amount of Pluronic F-68, acetone addition rate, pH, stirring time, and stirring speed. The dependent variables studied were the particle size, polydispersity index, amount of drug released in 6£¿h, time required to release 60% of drug, entrapment efficiency, loading efficiency, and mucoadhesiveness. The size of all nanoparticulate formulations prepared as per the experimental design (Taguchi screening design) varied between 165 and 1610£¿nm, PDI between 0.360 and 1.00, bioadhesiveness between 3.959 and 11.02£¿g, cumulative percent drug release in 24£¿h between 40.74 and 72.48, entrapment efficiency between 15.70 and 83.12, and loading efficiency between 39.72 and 80.49. Pareto ranking analyses showed that the two most important factors affecting the selected responses were amount of gelatin and amount of Pluronic F-68 ( ). 1. Introduction Acyclovir is a cyclic analogue of the natural nucleoside 2-deoxyguanosine, clinically used in the treatment of Herpes simplex, Varicella zoster, Cytomegalovirus, and Epstein barr virus infections [1]. It is currently marketed as capsules (200£¿mg), tablets (200, 400 and 800£¿mg), and suspension for oral administration, topical ointment, and intravenous injection. Oral acyclovir is mostly used as 200£¿mg tablets, five times a day [2]. Absorption of orally administered acyclovir is slow, variable, and incomplete, with a bioavailability of 15%¨C30% and the elimination half-life of acyclovir is approximately 3£¿h [3]. It has narrow absorption window and is primarily absorbed from stomach and upper part of the small intestine [4¨C6]. Reduced bioavailability of acyclovir may be because of transportation of dosage form from the region of absorption window to site where it is less absorbed. Therefore there was a need to increase the gastroretention time of dosage form so that drug would be available at the site of absorption and results in improved bioavailability. Several attempts are being made to increase the gastric retention of drugs, like intragastric floating systems, hydrodynamically balanced systems, extendable or expandable, microporous compartment system, microballoons, bio/mucoadhesive
%U http://www.hindawi.com/journals/isrn.nanomaterials/2013/348095/