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Molecules 2018, 23(2), 303; https://doi.org/10.3390/molecules23020303

Optimization of the Preparation Conditions of Borneol-Modified Ginkgolide Liposomes by Response Surface Methodology and Study of Their Blood Brain Barrier Permeability

1,2,3,4
,
2
,
2
,
1,2
,
1
and
1,3,4,*
1
College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China
2
Hanlin College, Nanjing University of Chinese Medicine, Taizhou 225300, China
3
Jiangsu Engineering Research Center for Efficient Delivery System of TCM, Nanjing 210046, China
4
Nanjing Engineering Research Center for Industrialization of Chinese Medicine Pellets, Nanjing 210046, China
*
Author to whom correspondence should be addressed.
Received: 24 November 2017 / Revised: 22 January 2018 / Accepted: 24 January 2018 / Published: 31 January 2018
(This article belongs to the Section Natural Products Chemistry)
View Full-Text   |   Download PDF [2858 KB, uploaded 31 January 2018]   |  

Abstract

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 Tmax of 15 min and a high drug concentration of 3.39 μg/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. View Full-Text
Keywords: ginkgolides; liposome; borneol; response surface methodology; blood-brain barrier permeability ginkgolides; liposome; borneol; response surface methodology; blood-brain barrier permeability
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Lv, Z.; Yang, Y.; Wang, J.; Chen, J.; Li, J.; Di, L. Optimization of the Preparation Conditions of Borneol-Modified Ginkgolide Liposomes by Response Surface Methodology and Study of Their Blood Brain Barrier Permeability. Molecules 2018, 23, 303.

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