title: Interfacial Cohesion and Assembly of Bioadhesive Molecules for Design of Long-Term Stable Hydrophobic Nanodrugs toward Effective Anticancer Therapy.
abstract: The majority of anticancer drugs are poorly water-soluble and thus suffer from rather low bioavailability. Although a variety of delivery carriers have been developed for bioavailability improvement, they are severely limited by low drug loading and undesired side effects. The optimum delivery vehicle would be a biocompatible and biodegradable drug nanoparticle of uniform size with a thin but stable shell, making it soluble, preventing aggregation and enabling targeting. Here, we present a general strategy for the rational design of hydrophobic drug nanoparticles with high drug loading by means of interfacial cohesion and supramolecular assembly of bioadhesive species. We demonstrate that the pathway is capable of effectively suppressing and retarding Ostwald ripening, providing drug nanoparticles with small and uniform size and long-term colloidal stability. The final complex drug nanoparticles provide higher tumor accumulation, negligible toxicity, and enhanced antitumor activity, superior to commercial formulations. Our findings demonstrate that local, on-demand coating of hydrophobic nanoparticles is achievable through cooperation and compromise of interfacial adhesion and assembly.
authors.affiliation: State Key Laboratory of Biochemical Engineering, Institute of Process Engineering, and ‡Center for Mesoscience, Institute of Process Engineering, Chinese Academy of Sciences , Beijing 100190, China.
authors.forename: Guizhi
authors.initials: G
authors.lastname: Shen
authors.affiliation: State Key Laboratory of Biochemical Engineering, Institute of Process Engineering, and ‡Center for Mesoscience, Institute of Process Engineering, Chinese Academy of Sciences , Beijing 100190, China.
authors.forename: Ruirui
authors.initials: R
authors.lastname: Xing
authors.affiliation: State Key Laboratory of Biochemical Engineering, Institute of Process Engineering, and ‡Center for Mesoscience, Institute of Process Engineering, Chinese Academy of Sciences , Beijing 100190, China.
authors.forename: Ning
authors.initials: N
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Biochemical Engineering, Institute of Process Engineering, and ‡Center for Mesoscience, Institute of Process Engineering, Chinese Academy of Sciences , Beijing 100190, China.
authors.forename: Chengjun
authors.initials: C
authors.lastname: Chen
authors.affiliation: State Key Laboratory of Biochemical Engineering, Institute of Process Engineering, and ‡Center for Mesoscience, Institute of Process Engineering, Chinese Academy of Sciences , Beijing 100190, China.
authors.forename: Guanghui
authors.initials: G
authors.lastname: Ma
authors.affiliation: State Key Laboratory of Biochemical Engineering, Institute of Process Engineering, and ‡Center for Mesoscience, Institute of Process Engineering, Chinese Academy of Sciences , Beijing 100190, China.
authors.forename: Xuehai
authors.initials: X
authors.lastname: Yan
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage*; D004337:Drug Carriers; D004339:Drug Compounding; D016503:Drug Delivery Systems; D057927:Hydrophobic and Hydrophilic Interactions; D053758:Nanoparticles
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers
keywords: Ostwald ripening suppression; drug delivery; hydrophobic drugs; interfacial assembly; nanoengineering