Nanoparticle based drug/gene delivery holds great promise in cancer therapeutics. However, site-specificity, efficacy, stability and toxicity of the carriers remain the major hurdle for the clinic application of nanoparticles in therapeutics. Here, we discuss synthesis of two types of vesicular, pH sensitive nanoparticles for drug/gene delivery. The polymeric nanoparticles (diameter of 20 nm to 500 nm) were assembled from amphiphilic random copolymers of acryloyl chloride, followed by functionalization with poly(ethyleneimines) (PEI). Hybrid nanoparticles (diameter of 25-50 nm) was prepared from calcium hydrophosphate (CaHPO4) as core for drug loading, followed by surface functionalization with PEGlated octadecyl-quaternized poly(?-glutamic acid) as shell, providing stealthiness and steric stability of the nanocomplex. PEI nanoparticles showed highly efficient in vitro delivery of anticancer drug, doxorubicin hydrochloride (Dox), and mRNA to HEK 293T cells at a relatively low cytotoxicity level.  Meanwhile, the use of hybrid core-shell nanocomplex could potentially enhance endosome escape efficiency while reducing cytotoxicity.

Design of polymeric and hybrid nanoparticles as drug and mRNA carriers for safe and efficient cancer therapeutics

244th National Meeting (2012)

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