title: Co-delivery of antineoplastic and protein drugs by chitosan nanocapsules for a collaborative tumor treatment.
abstract: Although combination delivery (co-delivery) shows much superiority in the defect compensation of single-agent therapy, the construction and application of co-delivery systems are still challenging, especially for protein-based joint systems. In this work, a series of chitosan (CS)-amino acid derivatives (Arg-CS, Lys-CS, and Phe-CS) with different degrees of substitution (DS) were synthesized to prepare CS nanocapsules (CNCs) using a simple emulsification method in the presence of linoleic acid (LA). The hydrophobic drug can be loaded in LA droplets, and a positively charged protein stabilized the optimized Arg-CS nanocapsules (Arg-CNCs) on their negative surfaces. The in vitro antitumor efficacy of Arg-CNCs co-delivering paclitaxel and recombinant human caspase-3 was evaluated in HeLa cells. The co-delivery system displayed much lower IC50values and a higher percentage of apoptotic cells compared with the control groups. This system provides a promising and universal strategy for co-delivery, leading to collaborative tumor treatment.
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Dong-Yan
authors.initials: DY
authors.lastname: Wu
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Ma
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Xiao-Shuang
authors.initials: XS
authors.lastname: Hou
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China; Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Wen-Jie
authors.initials: WJ
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China; Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Pei
authors.initials: P
authors.lastname: Wang
authors.affiliation: Department of Biochemistry, School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Huan
authors.initials: H
authors.lastname: Chen
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Bo
authors.initials: B
authors.lastname: Li
authors.affiliation: Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Can
authors.initials: C
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China. Electronic address: ayanju@163.com.
authors.forename: Ya
authors.initials: Y
authors.lastname: Ding
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D048271:Chitosan / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D053769:Nanocapsules / Q000737:chemistry*; D017239:Paclitaxel / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D053769:Nanocapsules; D048271:Chitosan; D017239:Paclitaxel
keywords: Amino acid derivatives; Caspase-3; Chitosan; Co-delivery; Nanocapsules