Synthesis and self-assembly of biodegradable polyethylene glycol-poly (lactic acid) diblock copolymers as polymersomes for preparation of sustained release system of doxorubicin

可生物降解的聚乙二醇-聚乳酸二嵌段共聚物的合成及自组装作为聚合物囊泡用于制备阿霉素缓释系统

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作者:Mona Alibolandi, Fatemeh Sadeghi, Seyed Hossein Sazmand, Seyed Mohammad Shahrokhi, Mahmoud Seifi, Farzin Hadizadeh

Conclusion

In conclusion copolymers of PEG/PLA with f OE ~25% and relatively higher molecular weight are more suitable for encapsulation and providing sustained release of DOX.

Discussion

Results obtained from (1)HNMR and GPC revealed that microwave irradiation is a simple and reliable method for the synthesis of PEG-PLA copolymers. Further analysis indicated the copolymer with relative molecular weight of PLA to PEG ratios of 3 or f Eo ~ 25% produced the smallest size polymersomes. Polymersomes prepared from PEG5000 to PLA15000 were more capable in loading and sustained release of DOX than those prepared from PEG2000 to PLA6000. Conclusion: In conclusion copolymers of PEG/PLA with f OE ~25% and relatively higher molecular weight are more suitable for encapsulation and providing sustained release of DOX.

Methods

Herein, a series of poly (lactic acid) (PLA) and PEG diblock copolymers were synthesized through the ring-opening polymerization. The polymerization reaction and the copolymer structures were evaluated by nuclear magnetic resonance (NMR) and gel permeation chromatography (GPC). The corresponding copolymers were implemented for the formation of polymersome structures using film rehydration method. Impact of methoxy PEG chain length and hydrophobic weight fraction on particle size of polymersomes were studied, and the proper ones were selected for loading of doxorubicin (DOX) via pH gradient method.

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