Preparation of braining-targeting liposomes and the structural stability of Ac4MAN on the surface of liposome in vitro
LI Rubing1 WANG Na2 LIU Xiaoying2 TANG Shukun2 PENG Haisheng1,2 TAO Haiquan3
1.Research Center of Life Sciences and Environmental Sciences, Harbin University of Commerce, Heilongjiang Province, Harbin 150028, China;
2.Department of Pharmaceutics, Campus of Harbin Medical University(Daqing), Heilongjiang Province, Daqing 163319, China;
3.Department of Neurosurgery, the 2nd Affiliated Hospital of Harbin Medical Hospital, Heilongjiang Province, Harbin 150000, China
Abstract：Objective To construct a modified Ac4MAN (p-carboxybenzene-α-D-acetylmannose) brain-targeted liposome and investigate the structural stability of Ac4MAN. Methods Ac4MAN was incubated with porcine liver esterase (PLE) at 37°C, pH 7.4 and sampled at different time points. High performance liquid chromatography (HPLC) and ultra performance liquid chromatography-mass spectrometry (UPLC-MS) were used to analyze it. Ac4MAN liposomes were prepared and characterized. Flow cytometry was used to detect the uptake of Ac4MAN liposomes and Ac4MAN liposomes plus PLE by glioma cells U87. Results The results of HPLC showed that the area of Ac4MAN decreased from 578.4 to 37.9 after incubation for 0-3 h. The area of Ac4MAN peak was close to 0 after incubation for 4-7 h. The peak area of the formed MAN (p-aminobenzene-α-D-pyran mannoside) increased from 0 to 363.0, indicating that with the prolongation of incubation time, Ac4MAN gradually decreased and MAN gradually increased. Conclusion The Ac4MAN liposome prepared in this study has a particle size of (120.3±2.0) nm and a potential of (-15.76±1.23) mV. The uptake of AC4MAN liposomes by U87 cells is enhanced after adding enzymes.
李茹冰1 王娜2 刘肖莹2 唐淑坤2 彭海生1，2 陶海泉3. 脑靶向脂质体构建及其靶分子Ac4MAN体外结构稳定性研究[J]. 中国医药导报, 2019, 16(11): 4-8.
LI Rubing1 WANG Na2 LIU Xiaoying2 TANG Shukun2 PENG Haisheng1,2 TAO Haiquan3. Preparation of braining-targeting liposomes and the structural stability of Ac4MAN on the surface of liposome in vitro. 中国医药导报, 2019, 16(11): 4-8.
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2019, Vol. 16 
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