Doxorubicin-loaded poly(lactic-co-glycolic acid) hollow microcapsules for targeted drug delivery to cancer cells

Abstract

We report here the fabrication, characterization and use of poly(lactic-co-glycolic acid) (PLGA) hollow microcapsules (HMs) loaded with the anticancer drug doxorubicin (DOX) for targeted drug delivery to cancer cells. In this study, PLGA HMs loaded with DOX (PLGA–DOX HMs) were prepared by a double emulsion method, followed by electrostatic assembly of positively charged polyethyleneimine (PEI) pre-modified with polyethylene glycol–folic acid segments (PEI–PEG–FA). The formed multifunctional PLGA–DOX–PEI–PEG–FA HMs were characterized via different techniques. We show that the HMs having a size of 2.5 μm are stable, and are able to release DOX in a sustained manner with a higher release rate under acidic pH conditions than that under the physiological pH conditions. Importantly, the PLGA–DOX–PEI–PEG–FA HMs displayed an effective therapeutic efficacy, comparable to that of free DOX, and were able to target cancer cells overexpressing high-affinity folic acid receptors and effectively inhibit the growth of the cancer cells. The fabricated PLGA–DOX–PEI–PEG–FA HMs may hold great promise to be used as a versatile carrier system for targeted drug delivery to different types of cancer cells.