Tumoral acidic pH-responsive MPEG-poly(β-amino ester) polymeric micelles for cancer targeting therapy

Title
Tumoral acidic pH-responsive MPEG-poly(β-amino ester) polymeric micelles for cancer targeting therapy
Authors
민경현김종호배상문김민상박상진이혜정박랑운김인산김광명권익찬정서영이두성
Keywords
Tumoral acidic microenvironment; pH-responsive polymeric micelle; Camptothecin; Cancer targeting drug delivery
Issue Date
2010-06
Publisher
Journal of controlled release
Citation
VOL 144, NO 2, 259-266
Abstract
Herein, we evaluated the tumoral low pH targeting characteristics of pH-responsive polymer micelles in cancer targeting therapy. To design the pH-responsive polymeric micelles, hydrophilic methyl ether poly (ethylene glycol) (MPEG) and pH-responsive/biodegradable poly(β-amino ester) (PAE) were copolymerized using a Michael-type step polymerization, resulting in an MEPG-PAE block copolymer. The amphiphilic MPEG-PAE block copolymer formed polymeric micelles with nano-sized diameter by self-assembly, which showed a sharp pH-dependant micellization/demicellization transition at the tumoral acidic pH value (pH 6.4). For the cancer image and therapy, fluorescence dye, tetramethylrhodamine isothiocyanate (TRITC), or anticancer drug, camptothecin (CPT), was efficiently encapsulated into the pH-responsive polymeric micelles (pH-PMs) by a simple solvent casting method. The TRITC or CPT encapsulated pH-PMs (TRITC-pH-PMs or CPT-pH-PMs) showed rapid release of TRITC or CPT in weakly acidic aqueous (pH 6.4) because they still presented a sharp tumoral acid pH-responsive micellization/demicellization transition. The pH-PMs with 10 wt.% of TRITC could deliver substantially more fluorescence dyes to the target tumor tissue in MDAMB231 human breast tumor-bearing mice, compared to the control polymeric micelles of PEG-poly(L-lactic acid) (PEG-PLLA). Importantly, CPT-pH-PMs exhibited significantly increased therapeutic efficacy with minimum side effects by other tissues in breast tumor-bearing mice, compared to free CPT and CPT encapsulated PEG-PLLA micelles. The tumoral acidic pH-responsive polymeric micelles are highly useful for cancer targeting therapy.
URI
http://pubs.kist.re.kr/handle/201004/38252
ISSN
0168-3659
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KIST Publication > Article
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