Construction of Enzyme-Sensitive Polypeptide Micelles and Feasibility of Drug Delivery to T Cells
HAN Zhi-min1, LI Guo-rui1, LI Juan-juan1, TAI Zong-guang2, GONG Chun-ai3, GAO Shen1*
1. Department of Pharmacy, Changhai Hospital, Second Military Medical University, Shanghai 200433, China; 2. Department of Pharmacy,Shanghai Dermatology Hospital, Shanghai 200443, China; 3. Department of Pharmacy, Ninth People's Hospital of Shanghai, Shanghai Jiao Tong University School of Medicine, Shanghai 200011, China
Abstract：OBJECTIVE To construct and characterize an enzyme-sensitive poly-peptide micelles which carrying the aromatic hydrocarbon receptor inhibitor CH223191, and preliminary evaluate its feasibility of delivering drugs to T cells. METHODS The peptide monomer SHRP was synthesized by solid-phase synthesis and the drug-loaded micelle SHRP-CH was prepared. Its particle size, drug loading, critical micelle concentration, cytotoxicity and immunogenicity etc. were measured. Flow cytometry and laser confocal were used to investigate the uptake efficiency of micelles into CD8+T cells. RESULTS The particle size of SHRP-CH was (133.8±7.4) nm, the particle size reduced to (92±5.8) nm after enzyme treatment; drug loading and encapsulation rate were (7.1±1.2)% and (67.7±2.3)%, micelles before and after enzymatic hydrolysis both have low cytotoxicity; CD8+T cell uptake experiments confirmed the feasibility of this micelle system to deliver drugs to T cells. CONCLUSION SHRP peptide micelle system has good drug-carrying capacity and low cytotoxicity, and is expected to be a potential carrier for T-cell drug delivery.
韩治敏, 李国瑞, 李鹃鹃, 台宗光, 宫春爱, 高申. 酶敏感多肽胶束的构建及其向T细胞递送药物的可行性研究[J]. 中国药学杂志, 2020, 55(23): 1955-1961.
HAN Zhi-min, LI Guo-rui, LI Juan-juan, TAI Zong-guang, GONG Chun-ai, GAO Shen. Construction of Enzyme-Sensitive Polypeptide Micelles and Feasibility of Drug Delivery to T Cells. Chinese Pharmaceutical Journal, 2020, 55(23): 1955-1961.
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2020, Vol. 55 
