Due to the tunable structures and properties of polymers, polymer-based drug and gene delivery systems hold promise for treating a wide range of diseases in a more accurate and disease-specific manner. In this study, well-defined poly(ethylene glycol)-b-poly(ε-caprolactone) (PEG-b-PCL) based biomaterials were investigated for drug and gene delivery applications (Figure 1). Specifically, the polymeric biomaterials for individual delivery of: (1) doxorubicin (DOX) as an anticancer drug, and (2) plasmid DNA (pDNA) were successfully achieved through the synthesis of functionalized ε-caprolactone monomers, the subsequent preparation of functional PEG-b-PCL diblock copolymers, followed by post-polymerization click modifications. The DOX-containing polymer-drug conjugate (PDC) was obtained by using alkyne-functionalized ε-caprolactone as the starting monomer to prepare the corresponding functional PEG-b-PCL for DOX conjugation. Cytotoxicity study using MCF-7 cells showed that the PDC micelles led to improved anticancer efficacy as compared to free DOX. The PEGylated cationic PCL (CPCL) for pDNA delivery was prepared by using allyl-functionalized ε-caprolactone as the starting monomer to synthesize the corresponding functional PEG-b-PCL for modification with tertiary amine groups. CPCL can readily form nanocomplexes with pDNA via spontaneous electrostatic interactions. At optimal weight ratio of CPCL to pDNA, these nanocomplexes resulted in significant transfection efficiency.

Well-defined poly(ethylene glycol)-b-poly(ε-caprolactone) based diblock polymeric biomaterials for drug and gene delivery

2019 Spring National Meeting

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