Development of docetaxel-loaded solid self-nanoemulsifying drug delivery system (SNEDDS) for enhanced chemotherapeutic effect

作者：Seo Youn Gee; Kim Dae Hwan; Ramasamy Thiruganesh; Kim Jeong Hwan; Marasini Nirmal; Oh Yu Kyoung; Kim Dong Wuk; Kim Jin Ki; Yong Chul Soon; Kim Jong Oh; Choi Han Gon^*

来源：International Journal of Pharmaceutics, 2013, 452(1-2): 412-420.

DOI：10.1016/j.ijpharm.2013.05.034

• Anti-tumor efficacy
• Bioavailability
• Docetaxel
• Self-nanoemulsifying drug delivery systems
• Toxicity

The main purpose of this study was to investigate the potential of self-nano-emulsifying drug delivery system (SNEDDS) in improving the bioavailability of docetaxel (DCT) and its chemotherapeutic effect. The DCT-loaded SNEDDS was prepared by employing rational blends of capryol 90, labrasol, and transcutol HP using ternary phase diagram. The liquid nano-emulsion was spray-dried into solid SNEDDS (D-SNEDDS) using an inert porous carrier, colloidal silica. The optimized formulation was characterized in terms of physico-chemical and pharmacokinetic parameters. Furthermore, anti-tumor efficacy of D-SNEDDS was compared with commercial marketed product, Taxotere (R). The various compositions of SNEDDS were screened and found optimal at a volume ratio of 10/75/15 for capryol 90, labrasol, and transcutol HP, respectively. We observed a high oral bioavailability of 17% DCT for D-SNEDDS than compared to only 2.6% for pure DCT solution. Notably, D-SNEDDS exhibited an augmented anti-tumor efficacy with a reduced toxicity profile when compared with intravenously administered Taxotere (R), the commercialized formulation of DCT. Taken together, D-SNEDDS could be a potential candidate for an oral dosage form of DCT with enhanced antitumor activity and reduced toxicity.

• 出版日期2013-8-16