Development of mucoadhesive nanoparticulate system of ebastine for nasal drug delivery

Abstract

Purpose: To prepare and evaluate mucoadhesive nanoparticulate system of ebastine for nasal drug delivery. Methods: The nanoparticles were prepared by ionic gelation method using drug-chitosan weight ratios 1:1, 1:2 and 1:3, and incorporating 0.5 or 0.7% w/v sodium tripolyphosphate (STPP) and poloxamer 407. The mucoadhesive nanoparticles were characterized by scanning electron microscope (SEM), transmission electron microscope (TEM), differential scanning colorimetry(DSC) and Fourier transform i nfrared spectroscopy (FTIR) and evaluated for drug loading, entrapment efficiency, in vitro mucoadhesion, in vitro drug release and ex-vivo permeation. Results: FTIR and DSC studies indicate that no chemical interaction occurred between the drug and polymer. Nanoparticle size ranged from 169 to 500 nm. Drug loading and entrapment efficiency increased with increase in chitosan concentration and decreased with increase in poloxamer 407 concentration. The highest drug loading obtained for the nanoparticles was 19.5%. With increase in polymer (chitosan) concentration (1:1 to 1:3), production yield was unchanged (73.2 to 74.4% (F6)). Mucoadhesion increased with increase in the concentration of chitosan. In vitro drug release from all the formulations was biphasic, being characterized by a slight 'burst' followed by slow release. At the end of 8 h F6 (1:3) showed drug release of only 86.9%, indicating sustained release. Ex-vivo permeation of pure ebastine was more rapid than from F6, thus indicating the capability of chitosan to control drug permeation rate through sheep nasal mucosa. Conclusion: The results indicate that a mucoadhesive nanoparticulate system can be used effectively for the nasal delivery of the antihistamine, ebastine. © Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria. All rights reserved.