Li Gan and Yi-Ping Gao contributed equally to this work.
Novel pH-sensitive lipid–polymer composite microspheres of 10-hydroxycamptothecin exhibiting colon-specific biodistribution and reduced systemic absorption
Article first published online: 18 APR 2013
Copyright © 2013 Wiley Periodicals, Inc.
Journal of Pharmaceutical Sciences
Volume 102, Issue 6, pages 1752–1759, June 2013
How to Cite
Gan, L., Gao, Y.-P., Zhu, C.-L., Zhang, X.-X. and Gan, Y. (2013), Novel pH-sensitive lipid–polymer composite microspheres of 10-hydroxycamptothecin exhibiting colon-specific biodistribution and reduced systemic absorption. J. Pharm. Sci., 102: 1752–1759. doi: 10.1002/jps.23499
- Issue published online: 16 MAY 2013
- Article first published online: 18 APR 2013
- Manuscript Accepted: 4 FEB 2013
- Manuscript Revised: 17 JAN 2013
- Manuscript Received: 5 DEC 2012
- colonic drug delivery;
Novel lipid–polymer composite microspheres (LP-MS) were prepared by combining pH-sensitive polymer Eudragit S100 with solid lipid Compritol 888 ATO for colonic delivery of 10-hydroxycamptothecin (HCPT), and pH-dependent controlled drug release has been achieved. The colon-specific biodistribution and uptake by the mucosal tissue were examined using coumarin-6-marked LP-MS. It is proved that good in vitro–in vivo relationship has been achieved, with more drugs being delivered to colon and a higher drug level was maintained for a long period. Moreover, in vivo bioavailability of LP-MS was evaluated with conventional enteric microspheres (enteric MS) as reference. After administration of LP-MS, systemic absorption of HCPT was greatly reduced, with area under the curve from 0 to 24h (AUC0–24 h, 2.186 ± 0.27) being significantly lower than that of enteric MS group (6.352 ± 0.696). In conclusion, the novel pH-sensitive LP-MS has potential for colon-specific drug delivery. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:1752–1759, 2013