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Article

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

1
College of Pharmacy, Chungbuk National University, Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, Korea
2
Drug Information Research Institute (DIRI), College of Pharmacy, Sookmyung Women’s University, Cheongpa-ro 47-gil 100, Yongsan-gu, Seoul 04310, Korea
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2021, 22(1), 231; https://doi.org/10.3390/ijms22010231
Received: 28 November 2020 / Revised: 23 December 2020 / Accepted: 23 December 2020 / Published: 28 December 2020
(This article belongs to the Special Issue Cell-Biomaterial Interaction 2020)
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. View Full-Text
Keywords: docetaxel; osthol; mPEG-b-PCL polymeric micelles; combination therapy; pharmacokinetics docetaxel; osthol; mPEG-b-PCL polymeric micelles; combination therapy; pharmacokinetics
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MDPI and ACS Style

Jo, M.J.; Lee, Y.J.; Park, C.-W.; Chung, Y.B.; Kim, J.-S.; Lee, M.K.; Shin, D.H. 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. Int. J. Mol. Sci. 2021, 22, 231. https://doi.org/10.3390/ijms22010231

AMA Style

Jo MJ, Lee YJ, Park C-W, Chung YB, Kim J-S, Lee MK, Shin DH. 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. International Journal of Molecular Sciences. 2021; 22(1):231. https://doi.org/10.3390/ijms22010231

Chicago/Turabian Style

Jo, Min J., Yu J. Lee, Chun-Woong Park, Youn B. Chung, Jin-Seok Kim, Mi K. Lee, and Dae H. Shin 2021. "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" International Journal of Molecular Sciences 22, no. 1: 231. https://doi.org/10.3390/ijms22010231

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