

FOLLOWUS
a.National University of Singapore Environmental Research Institute(NERI), National University of Singapore, Singapore 117576, Singapore
b.Beijing Advanced Innovation Center for Soft Matter Science and Engineering, State Key Laboratory of Organic-inorganic Composite Materials, College of Life Science and Technology, Beijing University of Chemical Technology, Beijing 100029, China
c.Department of Urology, China-Japan Friendship Hospital, Beijing 100029, China
E-mail yuqs@mail.buct.edu.cn (Q.S.Y)
E-mail zhgan@mail.buct.edu.cn (Z.H.G)
Received:28 June 2017,
Accepted:12 July 2017,
Online First:20 December 2018,
Published:05 April 2018
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Dan-Hua Zhou, Guan Zhang, Qing-Song Yu, et al. Folic Acid Modified Polymeric Micelles for Intravesical Instilled Chemotherapy[J]. Chinese Journal of Polymer Science, 2018, 36(4): 479-487.
Dan-Hua Zhou, Guan Zhang, Qing-Song Yu, et al. Folic Acid Modified Polymeric Micelles for Intravesical Instilled Chemotherapy[J]. Chinese Journal of Polymer Science, 2018, 36(4): 479-487. DOI: 10.1007/s10118-018-2009-y.
In this study
a targeting micellar drug delivery system was developed for intravesical instilled chemotherapy of bladder cancer. The amphiphilic diblock copolymer poly(
ε
-caprolactone)-block-poly(ethylene glycol) (PCL-
b
-PEO) with functional amino group (NH
2
) at the end of PEO block was synthesized. Then the copolymer was conjugated with folic acid (FA) and fluorescein isothiocyannate (FITC)
via
the PEO-NH
2
terminus
and then assembled into micelles with the target moiety and fluorescence labeling. In addition
drug loaded micelles were also fabricated with anticancer drug doxorubicin (DOX) encapsulated in the hydrophobic core. The micelles were characterized in terms of size
drug loaded efficiency and critical micellization concentration (CMC) by means of DLS
UV and fluorescence spectra.
In vitro
cellular uptake and cytotoxicity studies showed that FA modified PCL-
b
-PEO-FA micelles have a greater targeting efficiency to human bladder cancer cell (T-24 cell) compared to PCL-
b
-PEO-NH
2
micelles due to the conjugation of FA on the surface
while no targeting effect to normal tissue originated human embryonic kidney 293 (HEK-293) cells was observed
enabling the micelles a promising drug carrier for intravesical instilled chemotherapy of bladder cancer.
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