西吡氯铵修饰的脂质体用于氯诺昔康的经皮局部递送

Surfactant modified liposomes for topical delivery of lornoxicam

目的:研究一种可用于氯诺昔康局部递送的经皮给药系统。方法:比较不同处方脂质体(普通脂质体和传递体)的理化性质,优选最佳处方;将该给药系统应用于猪皮肤,通过Franz扩散池进行离体皮肤渗透研究。结果:以0.8%的磷脂酰胆碱制备的囊泡具有较高的包封率和载药量,粒径小于200 nm,粒径分布均匀(PDI<0.3);比较囊泡通量值发现,传递体具有最高的渗透系数,沉积在表皮层和真皮层中的药物量也观察到类似的结果。结论:传递体的形变能力使其能更好地渗透到更深的皮肤层;阳离子表面活性剂对角质层脂质组织的破坏增强了药物在皮肤中的递送能力。传递体有效增强了活性成分的吸收,在治疗作用上将表现得更好。

OBJECTIVE Investigation of a transdermal drug delivery system that can be used for topical delivery of lornoxicam.METHODS The physicochemical properties of liposomes(plain liposomes and transfersomes) with different prescriptions were compared to optimize the best prescription.This drug delivery system was applied to porcine skin for ex vivo skin permeation study through Franz diffusion cells.RESULTS The vesicles prepared with 0.8% phosphatidylcholine showed higher encapsulation efficiency and drug loading, with a particle size less than 200 nm and a uniform size distribution(PDI<0.3).From the comparison of vesicle flux values, we found that the transfersomes had the highest permeability coefficient, and similar results were also observed for the amount of drug deposited in the epidermal and dermal layers.CONCLUSION The deformability of transfersomes allows it to penetrate better into deeper skin layers. The disruption of the lipid organization in the stratum corneum by cationic surfactants enhances the drug delivery ability in the skin.Transfersomes effectively enhance the absorption of active ingredients, which can be expected to perform better in potential therapeutic effects.