PLGA nanoparticles with folate-conjugation and co-encapsulation of doxorubicin, quantum dots and SPIONS for cancer drug delivery and dual-modality imaging

Shen, Xue, Yan, Jie, Zhang, Chengchen, Yang, Hong, Wu, Chunhui and Liu, Yiyao (2016) PLGA nanoparticles with folate-conjugation and co-encapsulation of doxorubicin, quantum dots and SPIONS for cancer drug delivery and dual-modality imaging. Nanomedicine: Nanotechnology, Biology, and Medicine, 12 (2), 539-539. (doi:10.1016/J.NANO.2015.12.257).

Abstract

Doxorubicin (Dox) is a traditional chemotherapy drug, which has significant side effects, such as cardiotoxicity, mucositis, and myelosuppression. Meanwhile, many tumor cells also have a multi-drug resistant (MDR), which results in lower drug concentration in the tumor cells, and reduces its therapeutic effect. So, it is an important work for us to improve the selective delivery of DOX. Recently, using various nanocarriers encapsulated with anticancer drugs or inorganic nanoparticles which possessing special imaging effects for targeted delivery to tumor cells, gradually become a focus in the field of the nano-biotechnology research.

In this study, CdSe/ZnS quantum dots, superparamagetic iron oxide nanocrystals (SPIONs) and doxorubicin (Dox) are co-encapsulated into PLGA [poly(d,l-lactic-co-glycolic acid)]-based polymeric nanoparticles using a double emulsion solvent evaporation method (W/O/W), followed by coupled to the amine group of the polyethyleneimine (PEI) pre-modified with polyethylene glycol–folic acid segments (PEI–PEG–FA), the FA-targeted PEGylated PLGA NPs (QDs/DOX/Fe3O4@PLGA/PEI–PEG–FA) were formed for tumor specific targeting drug delivery and dual-modality imaging. SEM, TEM, EDX, ξ-potential analysis, fluorescence spectroscopy, ultraviolet and visible spectrophotometer were carried out to characterize the morphology, composition, and properties of the as-prepared composite nanoparticles. The mean diameter of the QDs/DOX/Fe3O4@PLGA/PEI–PEG–FA is 317 nm, which is dispersive and sable in water. When the weight ratio of DOX to PLGA was 100 (mg DOX/g PLGA), the encapsulation efficiency and the drug loading can be reached approximately 77.81% and 7.75% respectively. And the drug release was higher in an acid pH environment (pH 4.0) than in the physiological pH environment (pH 7.0). QDs/DOX/Fe3O4@PLGA/PEI–PEG–FA nanocomposite can be targeted to tumor cells with high expression of the folate receptor, reducing the side effects of Dox on normal tissues. It may be great promising for this nanocomposite to become an effective drug delivery system for tumor-targeted drug delivery and MR/optical dual-modality imaging.

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Contributors

Author: Chengchen Zhang

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