期刊
MOLECULES
卷 23, 期 2, 页码 -出版社
MDPI
DOI: 10.3390/molecules23020303
关键词
ginkgolides; liposome; borneol; response surface methodology; blood-brain barrier permeability
资金
- Natural Science Foundation of Jiangsu province [BK20161371]
- University Natural Scientific Foundation of Jiangsu Province [14KJD360005, 15KJB360011]
- Nanjing University of Chinese Medicine Hanlin College, China
Ginkgolides (GG), containing ginkgolide A (GA), ginkgolide B (GB) and ginkgolide C (GC), are mainly prescribed for ischemic stroke and cerebral infarction. However, the ginkgolides can hardly pass the blood-brain barrier (BBB) into the brain. The purpose of this study was to prepare borneol-modified ginkgolides liposomes (GGB-LPs) to study whether borneol could enhance the transport of ginkgolides across the BBB. The preparation conditions of GGB-LPs were optimized by a response surface-central composite design. Also, pharmacokinetics and biodistribution studies of GGB-LPs were conducted using UPLC-MS. The optimal preparation conditions for GGB-LP were as follows: ratio of lipid to drug (w/w) was 9:1, ratio of phospholipid to cholesterol (w/w) was 7:1, and hydrate volume was 17.5 mL. Under these conditions, the GGB-LP yield was 89.73 +/- 3.45%. With GGB-LPs, borneol significantly promoted the transport of ginkgolide across the BBB. The pharmacokinetic parameters of GGB-LP were significantly improved too, with T-max of 15 min and a high drug concentration of 3.39 mu g/g in brain. Additionally, the drug targeting index and relative uptake rate of GGB-LP was increased. Borneol-modified ginkgolide liposomes can thus potentially be used to improve the BBB permeability of gingkolide formulations.
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