Eudragit S-100 entrapped chitosan microspheres of valdecoxib for colon cancer |
| |
Authors: | Naveen K Thakral Alok R Ray Dipak K Majumdar |
| |
Affiliation: | (1) Centre for Biomedical Engineering, Indian Institute of Technology Delhi, Hauz Khas, New Delhi, 110016, India;(2) Biomedical Engineering Unit, All India Institute of Medical Science, New Delhi, 110029, India;(3) Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences and Research, Formerly College of Pharmacy, University of Delhi, Pushp Vihar, Sector III, New Delhi, 110017, India; |
| |
Abstract: | COX-2 inhibitors have demonstrated beneficial effects in colorectal cancer. The purpose of this study was to prepare and evaluate
the colon specific microspheres of COX-2 inhibitors using valdecoxib as a model drug. Mucoadhesive core microspheres were
prepared using chitosan as polymer and entrapped within Eudragit S 100 for colon targeting. FTIR spectrum of selected, coated
microspheres showed peaks of valdecoxib at 3377, 3250, 1334 and 1155 cm−1. XRD showed amorphous character and DSC showed depressed broad endotherm of valdecoxib at 169.07°C, which may be attributed
to dilution effect by the amorphous polymer. The coated microspheres were spherical with an average size of 90 μm. Storage
of the microspheres at 40°C/75% relative humidity for 6 months indicated no significant drug degradation. The coated microspheres
did neither release the drug in acidic pH of stomach (pH 1.2) nor in small intestinal pH between 5 to 6.8, and the release
started at pH 7.4, indicting perfect colonic delivery. The coated microspheres pretreated with phosphate buffer pH 7.4 for
30 min, when applied to mucosal surface of freshly excised goat colon, showed good mucoadhesion. The drug release at pH 7.4
and good mucoadhesive property of the microspheres make the system ideal for colonic delivery. |
| |
Keywords: | |
本文献已被 SpringerLink 等数据库收录! |
|