Abstract
Formulation and Evaluation of Self-Emulsifying Drug Delivery Systems of Larotaxel for Oral Administration
Department of Pharmaceutics, School of Pharmacy, 1School of Functional Food and Wine, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, PR China
Correspondence Address:
Z. Yu, Department of Pharmaceutics, School of Pharmacy, Shenyang, Liaoning 110016, PR China, E-mail: pharmzy@163.com
The objective of the present study was to develop a self-emulsifying drug delivery system of larotaxel and evaluate its in vitro and in vivo performance. The prepared larotaxel loaded self-emulsifying drug delivery system spontaneously formed microemulsion with a mean particle size of 115.4 nm when mixed with 100-fold water under gentle agitation. In vivo pharmacokinetics study of larotaxel loaded selfemulsifying drug delivery system demonstrated 5.19-fold enhancement in oral bioavailability compared to larotaxel-Sol. Furthermore, intestinal bio-distribution studies revealed that the intestinal residence time of larotaxel loaded self-emulsifying drug delivery system was dramatically extended in comparison to larotaxel-Sol. Lymphatic transport studies showed that cycloheximide, a chylomicron secretion blocker, would impede oral absorption of larotaxel loaded self-emulsifying drug delivery system, which confirmed that lymphatic route was involved in the absorption of larotaxel loaded self-emulsifying drug delivery system. What is more, in vivo antitumor experiment proved that the antitumor activity of oral larotaxel loaded self-emulsifying drug delivery system was significantly superior to oral larotaxel-Sol, which was close to intravenous larotaxel-Sol. In conclusion, self-emulsifying drug delivery system is a promising vehicle for the oral delivery of larotaxel.
