Objectives
Breviscapine, a hydrophobic drug used for treating cardiovascular disease, was encapsulated in liposomes to improve its pharmaceutical characteristics. This study describes a novel liposome composition approach to specifically inhibit the P‐glycoprotein efflux system.
Methods
Breviscapine‐loaded Pluronic P85‐coated liposomes were prepared by the thin film hydration technique. The particle size, zeta potential and encapsulation efficiency of the formulations were characterized. In‐vitro drug release and permeability of Caco‐2 cells were investigated. In‐vitro characteristics and pharmacokinetics of the liposomes were evaluated in rat studies.
Key findings
The Pluronic P85‐modified liposomes dispersed individually and had an approximate diameter of 118.8 ± 4.9 nm and a zeta potential of −35.4 ± 1.5 mV. Encapsulation efficiency was more than 90%. The use of the P85‐coated liposomes resulted in significantly (P < 0.05) increased absorption of breviscapine in Caco‐2 cells and in 5.6‐fold enhancement in its oral bioavailability in rats.
Conclusion
The P85‐modified liposomes for the oral delivery of breviscapine were prepared using l‐α‐phosphatidylcholine (soy‐hydrogenated) and cholesterol with a narrow size distribution. This method seems to effectively enhance the bioavailability of breviscapine in rats.