Micellar delivery of dasatinib for the inhibition of pathologic cellular processes of the retinal pigment epithelium
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- 作者：Qingqing Lia ; Ka Lun Laia ; Pui Shan Chana ; Sui Chu Leunga ; Ho Yin Lia ; Yuan Fanga ; Kenneth K.W. Toa ; Chung Hang J. Choib ; Qian Ying Gaoc ; Thomas W.Y. Leea ; thomas.lee@cuhk.edu.hk" class="auth_mail" title="E-mail the corresponding author
- 关键词：Dasatinib ; Polymeric micelles ; Nanoparticles ; Proliferative vitreoretinopathy ; Retinal pigment epithelium
- 刊名：Colloids and Surfaces B: Biointerfaces
- 出版年：2016
- 出版时间：1 April 2016
- 年：2016
- 卷：140
- 期：Complete
- 页码：278-286
- 全文大小：1771 K
文摘
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Physically stable dasatinib-loaded PEG-b-PLC nanomicelles were prepared with an enhanced solubility.
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Both blank and dasatinib-loaded polymeric micelles were non-cytotoxic towards ARPE-19 cells.
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Dasatinib-loaded micelles significantly inhibited PVR-related cellular changes of the retinal pigment epithelium compared to the free drug, the concentration of which was limited due to its poor solubility.
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There is a linear correlation between cellular uptake and the anti-proliferating effect of polymeric micelles.
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Drug loading appears to be a critical parameter for cellular uptake which in turn impacts the in vitro bioactivities of polymeric micelles.