Geniposide-Loaded Liposomes for Brain Targeting: Development, Evaluation, and In Vivo Studies.

Abstract

Geniposide (GE) possesses excellent neuroprotective effects but with poor brain targeting and short half-life. Liposome was considered to have great potential for brain diseases. Therefore, this research aimed to develop a geniposide liposome (GE-LP) as a brain delivery system for cerebral ischemia reperfusion injury (CIRI) therapy and evaluate its characterization, pharmacokinetics, brain targeting, and neuroprotective effects in vivo. Then, a reverse-phase evaporation method was applied to develop the GE-LP and optimize the formulation. Notably, the GE-LP had suitable size, which was 223.8 nm. Subsequently, the pharmacokinetic behavior of GE solution and GE-LP in mice plasma was investigated, and the brain targeting was also researched. The results showed that GE in plasma of GE-LP displayed three folds longer distribution half-life and a higher bioavailability and brain targeting compared to GE solution. In vivo neuroprotective effects was evaluated through the middle cerebral artery occlusion (MCAO) rat model, and GE-LP exhibited a stronger tendency in preventing the injury of CIRI, which can significantly improve neurological deficits. Overall, this study demonstrates GE-LP as a new formulation with ease of preparation, sustained release, and high brain targeting, which has significant development prospects on CIRI; this is expected to improve the efficacy of GE and reduce the frequency of administration.

• Authors: Jinyan Wan, Yu Long, Songyu Liu, Yulu Zhang, Yan Xiang, Dan Li, Ai Shi, Yu Shuang, Ying Li, Yanan He, Nan Li, Yongmei Guan
• Journal: AAPS PharmSciTech (AAPS PharmSciTech) Vol. 22 Issue 7 Pg. 222 (Aug 18 2021) ISSN: 1530-9932 [Electronic] United States
• PMID: 34409515 (Publication Type: Journal Article)
• Copyright: © 2021. American Association of Pharmaceutical Scientists.

Chemical References

• Iridoids
• Liposomes
• geniposide

Topics

• Animals
• Brain
• Iridoids
• Liposomes
• Mice
• Rats
• Rats, Sprague-Dawley
• Reperfusion Injury (drug therapy)