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

• Main Authors: Zinan Zhang (Author), Wenbin Cao (Author), Huanchun Xing (Author), Shuai Guo (Author), Lijuan Huang (Author), Lin Wang (Author), Xin Sui (Author), Kui Lu (Author), Yuan Luo (Author), Yongan Wang (Author), Jun Yang (Author)
• Format: Book
• Published: Elsevier, 2024-04-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 2211-3835; 10.1016/j.apsb.2023.11.015
• Keywords: Liposomes; Phospholipase A2; Phosphoserine; Blood-brain barrier; Selectively open; Mix & act; Therapeutics. Pharmacology; RM1-950
• Source: Acta Pharmaceutica Sinica B, Vol 14, Iss 4, Pp 1827-1844 (2024)

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.