Formulation and Evaluation as Sustain Released Nanoparticles for Zolmitriptan Hydrochloride for the enhanced Bioavailability and Better Therapeutic Action by using Chitosan as a Permeation Enhancer

Abstract

Chitosan was hydrophobically modified as N-Butyryl chitosan (NBC), N-Lauroyl chitosan (NLC) were synthesized and characterized by FTIR, NMR, XRD, modified chitosan were having about 14 % degree of substitution and varying solubility. Further evaluation of synthesized N-acyl chitosan to loaded Zolmitriptan HCl as nanoparticle by ionotropic method with cross linking by TPP. Average particle size, drug loading, entrapment efficiency and in-vitro mucoadhesion of Zolmitriptan HCl loaded nanoparticle was 150.7±3.3nm, 24.80±1.1% and 54.96±3.8% respectively, with positive zeta potential which were directly correlated with increases bulkiness of the acyl substitution in the modified chitosan except zeta potential was found inversely correlated. TEM and SEM imaging relieved spherical structure of nanoparticle. In vitro release of Zolmitriptan HCl in 1.2 pH HCl buffer and pH 7.4 phosphate buffer solutions showed biphasic release pattern best fitted with Korsmeyer’s-Peppas kinetics with fickian transport mechanism. Acylated chitosan showed sustained release reducing with increasing length of acyl group. Result of the present study showed that hydrophobically modified acylated chitosan can be useful for achieving sustained release controlled by acylation modification.