Phosphorylcholine-based stealthy nanocapsules enabling tumor microenvironment-responsive doxorubicin release for tumor suppression.

Abstract	The efficient delivery of anticancer drugs into tumor tissues to improve therapeutic efficacy remains an urgent demand. To satisfy this demand, a drug delivery system based on a stealthy nanocapsule was developed. This nanocapsule was fabricated by encapsulating stealthy cross-linked poly(2-methacryloyloxyethyl phosphorylcholine) (PMPC) and benzaldehyde groups around the protein bovine serum albumin (BSA) followed by conjugation of doxorubicin (Dox) through a pH-responsive benzoic-imine bond. The in vitro results show that the Dox-conjugated nanocapsule (nBSA-Dox) released the drug under an acidic tumor microenvironment (pH ~6.5) and killed HepG2 human liver cancer cells. The half-life of Dox conjugated to nBSA in mice was significantly prolonged, and the area-under-curve of plasma Dox of the mice treated with nBSA-Dox was as much as 242 fold of free Dox. The in vivo results confirmed that this nanocapsule efficiently accumulated in tumor tissue and significantly suppressed the tumor growth.
Authors	Gan Liu, Hsiang-I Tsai, Xiaowei Zeng, Yixiong Zuo, Wei Tao, Jun Han, Lin Mei
Journal	Theranostics (Theranostics) Vol. 7 Issue 5 Pg. 1192-1203 ( 2017) ISSN: 1838-7640 [Electronic] Australia
PMID	28435458 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Antibiotics, Antineoplastic Drug Carriers Nanocapsules Phosphorylcholine Doxorubicin
Topics	Animals Antibiotics, Antineoplastic (pharmacokinetics, therapeutic use) Cell Survival (drug effects) Disease Models, Animal Doxorubicin (pharmacokinetics, therapeutic use) Drug Carriers (administration & dosage) Half-Life Hep G2 Cells Hepatoblastoma (drug therapy) Hepatocytes (drug effects, physiology) Heterografts Humans Hydrogen-Ion Concentration Mice Nanocapsules (administration & dosage) Phosphorylcholine (administration & dosage) Treatment Outcome Tumor Microenvironment

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