Novel biodegradable application of chitosan/lysine compounds for delivery of ligustrazine

Abstract

Ligustrazine (Lig) is one of the main effective components of Ligusticum chuanxiong Hort and possesses a variety of biological activities against cardiovascular and cerebrovascular diseases. However, its volatility and poor bioavailability limit its clinical application to some degree. It is challenging to deliver Lig effectively to the disease location with optimized exposure and long-term effects when treating cardiovascular and cerebrovascular diseases. In this study, the authors developed a novel biodegradable and long-acting carrier to improve the delivery of Lig, combining the benefits of chitosan (CS) and lysine (l-Lys) to obtain CS/l-Lys as a drug delivery system for carrying Lig, which could improve the delivery of Lig and increase the drug-loading capacity efficiently. The physicochemical properties of the carrier were characterized. The cytotoxicity of CS/l-Lys and CS/l-Lys/Lig was evaluated by using Cell Counting Kit-8. Furthermore, the in vitro drug release profile and blood compatibility were evaluated. The results showed that the CS/l-Lys nanoparticle (NP) delivery system was suitable for carrying Lig and release the drug effectively and CS/l-Lys/Lig NPs could be a potential platform for improving the treatment of cardiovascular and cerebrovascular diseases.