Preparation and Characterization of Nanoparticles Composed of Methylated N-(4-N,N-Dimethyl Aminobenzyl) Chitosan for Oral Delivery of Cyclosporine A Publisher



Mahjub R³ ; Allahyar R¹ ; Rafieetehrani M¹ ; Dorkoosh FA^{1, 2} Show Affiliations
Source: European Journal of Nanomedicine Published:2016

Abstract

Cyclosporine is considered a highly lypophilic compound meaning low bioavailability through oral administration. In this study, cyclosporine was entrapped in a novel aromatic, quaternized derivative of chitosan (i.e. methylated N-(4-N,N-dimethyl aminobenzyl) chitosan) in order to improve solubility and bioavailability. Methylated N-(4,N,N-dimethyl aminobenzyl) chitosan was synthesized by the Schiff base reaction method. Polymeric nanoparticles containing cyclosporine was prepared and the physico-chemical properties of prepared nanoparticles were determined. The nanoparticles were studied morphologically using transmission electron microscopy (TEM). Finally, the release of cyclosporine from nanoparticles was studied in vitro using simulated intestinal fluid adjusted to pH of 6.8. For the preparation of nanoparticles, different formulations were studied and it was found that proper nanoparticles were prepared in equal concentration (1 mg/mL) of polymer and sodium tri-poly phosphate (TPP). The size, zeta potential, PdI, EE% and LE% of the prepared nanoparticles were reported as 173±36 nm, 23.1±4.18 mV, 0.243±0.05, 97.1±4.38% and 3.2±0.21%, respectively. The TEM images of nanoparticles revealed spherical to sub-spherical nanoparticles with no sign of agglomeration. This study suggests that preparations of nanoparticles composed of methylated N-(4,N,N-dimethyl aminobenzyl) chitosan can be a good candidate for improving the oral bioavailability of cyclosporine. © 2016 by De Gruyter.