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Gas‐forming poly(ethylene glycol)‐b‐poly(L‐lactic acid) micelles
Authors:Jung Ok Lee  Dongin Kim  Dong Sup Kwag  Ung Yeol Lee  Kyung Taek Oh  Yu Seok Youn  Young Taik Oh  Jin Woo Park  Eun Seong Lee
Institution:1. Division of Biotechnology, The Catholic University of Korea, , Bucheon‐si, Gyeonggi‐do, 420‐743 Republic of Korea;2. Department of Pharmaceutics and Pharmaceutical Chemistry, University of Utah, , 421 Wakara Way, Suite 318 Salt Lake City, UT, 84108 USA;3. College of Pharmacy, Chung‐Ang University, , Dongjak‐gu, Seoul, 155‐756 Republic of Korea;4. College of Pharmacy, Sungkyunkwan University, , Suwon‐si, Gyeonggi‐do, 440‐746 Republic of Korea;5. Department of Radiology, Severance Hospital, Yonsei University College of Medicine, , Seodaemun‐ku, Seoul, 120‐752 Republic of Korea;6. Amore‐pacific Corporation R&D Center, , Yongin‐si, Gyeonggi‐do, 446‐729 Republic of Korea
Abstract:In this study, a novel drug‐carrying micelle composed of methoxy poly(ethylene glycol) (mPEG)‐b‐poly(L‐lactic acid) (PLLA) with gas‐forming carbonate linkage was fabricated. Here, the gas‐forming carbonate linkage was formed by the chemical coupling of the terminal hydroxyl group of the PLLA block and benzyl chloroformate (BC). mPEG‐b‐PLLA‐BC was self‐organized in aqueous solution: the PEG block on the hydrophilic outer shell and the PLLA‐BC block in the hydrophoboic innor core. The cleavage of carbonate linkage by hydrolysis and formation of carbon dioxide nanobubbles in the micellar core enabled an accelerated release of the encapsulated anticancer drug (doxorubicin: DOX) from the mPEG‐b‐PLLA‐BC micelles. The amount of drug (DOX) released from the mPEG‐b‐PLLA‐BC micelle was higher than that from the conventional mPEG‐b‐PLLA micelle, which allowed for increased in vitro toxicity against KB tumor cells. Copyright © 2013 John Wiley & Sons, Ltd.
Keywords:gas‐forming micelle  poly(ethylene glycol)‐b‐poly(L‐lactic acid)  drug release kinetics  anticancer drug delivery
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