Construction of a nanoformulation with active targeting and preliminary study on its in vitro pharmacodynamics
LIU Miao1 PENG Ying2 ZHOU Xingchen3
1.Department of Pharmacy, Hunan Cancer Hospital, Hunan Province, Changsha 410011, China;
2.Xiangya School of Pharmaceutical Sciences, Central South University, Hunan Province, Changsha 410013, China;
3.Department of Pharmacy, Xiangya Hospital, Central South University, Hunan Province, Changsha 410008, China
Abstract：Objective To construct an active targeting nanoformulation loaded with the chemotherapeutic Doxorubicin (DOX). Methods PLGA/DOX@PDA-PEG-FA nanoformulations were prepared by using polylactic acid-glycolic acid copolymer (PLGA), DOX, dopamine (DA), amino-modified polyethylene glycol folic acid (NH2-PEG-FA). Particle size, potential, drug loading, encapsulation efficiency, drug release characteristics were characterized, and cell uptake, biocompatibility, cytotoxicity were preliminarily discussed by fluorescence inverted microscope and thiazolyl blue (MTT) colorimetry. Results In this study, PLGA/DOX@PDA-PEG-FA nano-formulations were successfully prepared, which had an obvious core-shell structure with a particle size of about 120 nm, a shell thickness of about 18 nm, and ζ potential of -18.1 mV. The encapsulation efficiency and drug loading were 43.56% and 1.86%, respectively, and it had obvious sustained-release properties. MTT assay showed that the carrier material had good biocompatibility and the cytotoxicity was dose-dependent. Conclusion The nanocomposite prepared in this experiment has good biocompatibility and anti-tumor effect in vitro. The preparation provides a new idea for the wide application of PLGA and the effective reduction of adverse reactions of chemotherapy drugs.
刘淼1 彭颖2 周星辰3. 具有主动靶向作用的纳米制剂的构建及体外药效学探讨[J]. 中国医药导报, 2023, 20(1): 4-8.
LIU Miao1 PENG Ying2 ZHOU Xingchen3. Construction of a nanoformulation with active targeting and preliminary study on its in vitro pharmacodynamics. 中国医药导报, 2023, 20(1): 4-8.
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