Preparation,characterization, and biodistribution of breviscapine proliposomes in heart |
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| Authors: | Xiong Fei Xiong Chen Ge Liang Chen Yue-Jian Wang Hao |
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| Institution: | 1. State Key Laboratory of Bioelectronics, Jiangsu Laboratory for Biomaterials and Devices, School of Biological Science and Medical Engineering, Southeast University, Nanjing, People’s Republic of China;2. Department of Pharmacology, School of Basic Medicine, Hebei Medical University, Shijiazhuang, People’s Republic of China;3. Pharmaceutical Research Institute, China Pharmaceutical University, Nanjing, People’s Republic of China;4. Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, People’s Republic of China |
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| Abstract: | Breviscapine proliposomes were prepared by ethanol injection–homogenization–lyophilization method. On contact with 5% glucose, the proliposomes were rapidly converted into a liposomal dispersion, in which a certain amount of breviscapine was entrapped by the liposomes. The entrapment efficiency measured by reverse dialysis method was 77.89?±?0.28%. The particle size, polydispersity index, and zeta potential of breviscapine liposomes were 504.83?±?52.88?nm (by intensity), 0.17?±?0.02, and ?(20.31?±?1.03) mV, respectively (mean ± SD, n = 3). In mimic-biomembrane model experiment, breviscapine was distributed not only to n-octanol and buffer phase but also to interfacial phase. After bolus administration, the elimination phase (t1/2(β) = 66.386) of liposomal formulation in plasma was 4.8 times longer than that of solution formulation (t1/2(β) = 13.695). The AUC and MRT values of liposomal formulation in heart were increased more than 11.7- and 3.2-fold versus solution formulation, respectively. These results were all beneficial to heart disease therapy. |
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| Keywords: | Breviscapine proliposomes reverse dialysis mimic-biomembrane biodistribution in heart |
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