A mix & act liposomes of phospholipase A2-phosphatidylserine for acute brain detoxification by blood‒brain barrier selective-opening

Zinan Zhang; Wenbin Cao; Huanchun Xing; Shuai Guo; Lijuan Huang; Lin Wang; Xin Sui; Kui Lu; Yuan Luo; Yongan Wang; Jun Yang

doi:10.1016/j.apsb.2023.11.015

A mix & act liposomes of phospholipase A2-phosphatidylserine for acute brain detoxification by blood‒brain barrier selective-opening

Acta Pharm Sin B. 2024 Apr;14(4):1827-1844. doi: 10.1016/j.apsb.2023.11.015. Epub 2023 Nov 11.

Authors

Zinan Zhang¹, Wenbin Cao¹, Huanchun Xing², Shuai Guo³, Lijuan Huang¹, Lin Wang¹, Xin Sui¹, Kui Lu², Yuan Luo¹, Yongan Wang¹, Jun Yang¹

Affiliations

¹ State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institutes of Pharmacology and Toxicology, Beijing 100850, China.
² Tianjin University of Science and Technology, Tianjin 300222, China.
³ Hebei University of Science and Technology, Shijiazhuang 050018, China.

Abstract

In the treatment of central nervous system disease, the blood-brain barrier (BBB) is a major obstruction to drug delivery that must be overcome. In this study, we propose a brain-targeted delivery strategy based on selective opening of the BBB. This strategy allows some simple bare nanoparticles to enter the brain when mixed with special opening material; however, the BBB still maintains the ability to completely block molecules from passing through. Based on the screening of BBB opening and matrix delivery materials, we determined that phospholipase A2-catalyzed 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoserine liposomes can efficiently carry drugs into the brain immediately. At an effective dose, this delivery system is safe, especially with its effect on the BBB being reversible. This mix & act delivery system has a simple structure and rapid preparation, making it a strong potential candidate for drug delivery across the BBB.

Keywords: Blood–brain barrier; Liposomes; Mix & act; Phospholipase A2; Phosphoserine; Selectively open.