Charge‐conversional poly(amino acid)s derivatives as a drug delivery carrier in response to the tumor environment

Abstract A charge‐converting and pH‐dependent nanocarrier was achieved by conjugating 2,3‐dimethylmaleic anhydride (DMMA) to the amino group of an octadecyl grafted poly (2‐hydroxyethyl aspartamide) (PHEA‐g‐C₁₈‐NH₂) backbone, thereby forming a spherical micelle. PHEA, a poly(amino acid)s derivative, was derived from poly(succinimide), which is biocompatible and biodegradable. DMMA, a detachable component at the tumor site, was added, preventing aggregation with negative blood serum and enhancing the nanocarrier's cellular uptake. The polymeric micelle was comprehensively characterized and doxorubicin was encapsulated successively. The cellular uptake and anticancer therapeutic effect were evaluated by flow cytometry, confocal laser scanning microscopy, and a MTT assay. The properties of the nanocarrier can further be exploited to develop an early detection module for cancer. The present work is also expected to advance the study of designing smart carriers for drug and gene delivery. © 2012 Wiley Periodicals, Inc. J Biomed Mater Res Part A, 2012.