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Polymers 2016, 8(11), 379; doi:10.3390/polym8110379

Conjugation of Lectin to Poly(ε-caprolactone)-block-glycopolymer Micelles for In Vitro Intravesical Drug Delivery

1
Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, China
2
National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Patrick van Rijn
Received: 22 August 2016 / Revised: 18 October 2016 / Accepted: 18 October 2016 / Published: 26 October 2016
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Abstract

Amphiphilic poly(ε-caprolactone)-block-poly[2-(α-d-mannopyranosyloxy) ethyl acrylamide] (PCL-b-PManEA) block copolymers were synthesized via a combination of ring-opening polymerization (ROP), reversible addition-fragmentation chain transfer (RAFT) polymerization and reactive ester-amine reaction. The PCL-b-PManEA block copolymers can self-assemble into micelles and encapsulate anticancer drug doxorubicin (DOX). To enhance mucoadhesive property of the resulting DOX-loaded PCL-b-PManEA micelles, Concanavalin A (ConA) lectin was further conjugated with the micelles. Turbidimetric assay using mucin shows that the DOX-loaded PCL-b-PManEA@ConA micelles are mucoadhesive. DOX release from the DOX-loaded PCL-b-PManEA@ConA micelles in artificial urine at 37 °C exhibits an initial burst release, followed by a sustained and slow release over three days. Confocal laser scanning microscope (CLSM) images indicate that the DOX-loaded PCL-b-PManEA@ConA micelles can be effectively internalized by UMUC3 human urothelial carcinoma cells. The DOX-loaded PCL-b-PManEA@ConA micelles exhibit significant cytotoxicity to these cells. View Full-Text
Keywords: lectin; glycopolymer; mucoadhesion; reactive pentafluorophenyl ester; bladder cancer; micelles lectin; glycopolymer; mucoadhesion; reactive pentafluorophenyl ester; bladder cancer; micelles
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Li, N.N.; Cai, X.Y.; Chen, J.C.; Hu, X.F.; Xu, L.Q. Conjugation of Lectin to Poly(ε-caprolactone)-block-glycopolymer Micelles for In Vitro Intravesical Drug Delivery. Polymers 2016, 8, 379.

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