Evaluation of the Physicochemical Properties, Pharmacokinetics, and In Vitro Anticancer Effects of Docetaxel and Osthol Encapsulated in Methoxy Poly(ethylene glycol)-b-Poly(caprolactone) Polymeric Micelles
- Jo, Min Jeong; Lee, Yu Jin; Park, Chun-Woong; Chung, Youn Bok; Kim, Jin-Seok; Lee, Mi Kyeong; Shin, Dae Hwan
- Issue Date
- docetaxel; osthol; mPEG-b-PCL polymeric micelles; combination therapy; pharmacokinetics
- INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, v.22, no.1, pp.1 - 16
- Journal Title
- INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
- Start Page
- End Page
- Docetaxel (DTX), a taxane-based anticancer drug, and osthol (OTH), a coumarin-derivative compound, have shown anticancer effects against different types of cancers through various mechanisms. However, these drugs have low solubility in water and low oral bioavailability, and thus their clinical application is difficult. To overcome these problems, we encapsulated DTX and OTH in methoxy poly(ethylene glycol)-b-poly(caprolactone) (mPEG-b-PCL) and conducted studies in vitro and in vivo. We selected a 1:4 ratio as the optimal ratio of DTX and OTH, through combination index analysis in A549 cancer cells, and prepared micelles to evaluate the encapsulation efficiency, drug loading, particle size, and zeta potential. The in vitro drug-release profile showed that DTX/OTH-loaded mPEG-b-PCL micelles could slowly release DTX and OTH. In the clonogenic assay, DTX/OTH-loaded mPEG-b-PCL micelles showed 3.7 times higher inhibitory effect than the DTX/OTH solution. Pharmacokinetic studies demonstrated that micelles in combination with DTX and OTH exhibited increased area under curve and decreased clearance values, as compared with single micelles.
- Files in This Item
Go to Link
- Appears in
- 약학대학 > 약학부 > 1. Journal Articles
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.