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pH-Responsive Poly(ethylene glycol)/Poly(L-lactide) Supramolecular Micelles Based on Host-Guest Interaction

Zhe Zhang, Qiang Lv, Xiaoye Gao, Li Chen, Yue Cao, Shuangjiang Yu, Chaoliang He, Xuesi Chen

ACS Appl Mater Interfaces. 2015 Apr 29;7(16):8404-11.

PMID: 25856564

Abstract:

pH-responsive supramolecular amphiphilic micelles based on benzimidazole-terminated poly(ethylene glycol) (PEG-BM) and β-cyclodextrin-modified poly(L-lactide) (CD-PLLA) were developed by exploiting the host-guest interaction between benzimidazole (BM) and β-cyclodextrin (β-CD). The dissociation of the supramolecular micelles was triggered in acidic environments. An antineoplastic drug, doxorubicin (DOX), was loaded into the supramolecular micelles as a model drug. The release of DOX from the supramolecular micelles was clearly accelerated as the pH was reduced from 7.4 to 5.5. The DOX-loaded PEG-BM/CD-PLLA supramolecular micelles displayed an enhanced intracellular drug-release rate in HepG2 cells compared to the pH-insensitive DOX-loaded PEG-b-PLLA counterpart. After intravenous injection into nude mice bearing HepG2 xenografts by the tail vein, the DOX-loaded supramolecular micelles exhibited significantly higher tumor inhibition efficacy and reduced systemic toxicity compared to free DOX. Furthermore, the DOX-loaded supramolecular micelles showed a blood clearance rate markedly lower than that of free DOX and comparable to that of the DOX-loaded PEG-b-PLLA micelles after intravenous injection into rats. Therefore, the pH-responsive PEG-BM/CD-PLLA supramolecular micelles hold potential as a smart nanocarrier for anticancer drug delivery.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
LS71131 Poly(L-lactide) N-2-hydroxyethylmaleimide terminated Poly(L-lactide) N-2-hydroxyethylmaleimide terminated Price
LS741177 Poly(ethylene glycol), α-maleimidopropionamide-ω-formyl terminated Poly(ethylene glycol), α-maleimidopropionamide-ω-formyl terminated Price
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