화학공학소재연구정보센터
학회 한국고분자학회
학술대회 2004년 가을 (10/08 ~ 10/09, 경북대학교)
권호 29권 2호, p.118
발표분야 생체적합성 유ㆍ무기 입자소재
제목 Hydrotropic Polymer Micelles for Solubilization of Poorly Water-Soluble Drugs
초록 The clinical utilities of a large number of drugs are limited by their poor water-solubilities. A large number of drug candidates are also abandoned due to their extremely low water-solubilities. Paclitaxel is one of the poorly soluble drugs of which bioavailability can be improved significantly by increasing the water-solubility. Several approaches have been used for increasing water solubilities of poorly soluble drugs including paclitaxel, but only with limited successes.
During the last few years, we have developed hydrotropic solubilization system as a new and alternative approach to increase water-solubility of poorly soluble drugs. We have identified low molecular weight hydrotropic agents effective for paclitaxel solibilization, and synthesized various polymeric forms of the hydrotropes.1 The polymers, dendrimers, and hydrogels with hydrotropic properties produced paclitaxel formulations with very high stability as well as high solubilization capacity.2
The objective of this study is to develop hydrotropic polymer micelles for paclitaxel delivery so that the bioavailability of orally delivered paclitaxel is high enough for clinical applications. The presence of hydrotropic polymer segment in the micelle core provided unique properties which were not accomplished with currently available polymeric micelles. Combining hydrotropic property and polymeric micelle systems produced a unique delivery system with the following advantages. The hydrotropic polymeric micelles showed substantially increased paclitaxel loading capacity (up to 40 wt%) and physical stability for more than 2 months.3 Our in vitro studies using hydrotropic polymer micelles showed that hydrotropic polymer micelles were highly effective against human tumor cell lines. The time course of paclitaxel in serum after intravenous, portal venous, and duodenal catheter administration clearly indicated the absorption of paclitaxel from the oral administration of the hydrotropic polymer micelle formulations.

참고문헌
1. S. C. Lee, G. Acharya, J. Lee, and K. Park, Macromolecules, 36, 2248 (2003).
2. J. Lee, S. C. Lee, G. Acharya, and K. Park, Pharm. Res, 20, 1022 (2003).
3. K. M. Huh, S. C. Lee, Y. W. Cho, J. Lee, J. H. Jeong, and K. Park, Journal of Controlled Release in press.


Acknowledgment. This study was supported in part by National Institute of Health through grant GM 65284 and Samyang Corporation.
저자 이상천1, 김경자1, 허강무2, 조용우2, 이재휘2, 박기남2
소속 1요업(세라믹)기술원 생체재료팀, 2Purdue Univ. Dept. of Pharmaceutics and Biomedical Eng.
키워드 hydrotropic; micelles; copolymer; paclitaxel
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