Characterization and hemocompatibility of poly (N-acryloyl-L-tryptophan) nanoparticles as targeting delivery carriers for vinblastine.

Abstract

Favorable biocompatibility is essential to biomaterials, and natural amino acids are recognized as the promising building block of polymers due to their non-toxicity and tunable side chains. We prepared polymeric nanoparticles (NPs) using N-acryloyl-L-tryptophan monomer by precipitation polymerization, and modified with polyethylene glycol and folate (PEG-FA) to improve the solubility and target folate-receptors (FR) overexpressed tumor tissues. Serving as drug carriers for vinblastine (VBL), NPs-PEG-FA with about 212.4 nm had the drug loading of VBL of 6.65 ± 0.41% after co-incubating for 1 h and showed sustained-release in pH 7.4 PBS, in which 99.87 ± 1.00% of VBL was released from NPs-PEG-FA during 72 h. Furthermore, NPs-PEG-FA was more efficiently taken up by FR positive Hela cells compared with NPs-PEG, which signified folate could enhance the internalization of NPs-PEG-FA into FR over-expressed cells. And NPs-PEG-FA began to enter Hela cells in large quantities from 3 h onwards, meanwhile the released drug increased more quickly in the first 3 h, which indicated most of the drugs would be released after entering tumor cells. More importantly, NPs-PEG-FA had good biocompatibility to L929 mouse fibroblast cells and exhibited hemocompatibility via the assays of hemolysis, antithrombogenicity, coagulation activation and platelet activation. NPs-PEG-FA could serve as drug carriers for delivering drugs into FR positive tumor cells.