目的:卵磷脂/壳聚糖纳米粒在治疗剂的经皮给药中显示出巨大的前景。黄芩素,一种天然的生物活性类黄酮,对皮肤病具有多种生物活性。然而,由于其固有的差的亲水性和亲脂性,其局部应用受到限制。在这项研究中,制备黄芩素-磷脂复合物以增强黄芩素的亲脂性,然后开发负载黄芩素-磷脂复合物的卵磷脂/壳聚糖纳米粒,以改善黄芩素的透皮保留和渗透性。
方法:通过溶剂注射法制备卵磷脂/壳聚糖纳米颗粒,并在粒径分布方面进行表征,zeta电位,和形态学。在体外释放,离体和体内渗透研究,并对卵磷脂/壳聚糖纳米粒进行安全性评价,以评价其增强黄芩素的透皮保留和通透性的有效性。
结果:通过壳聚糖和卵磷脂的自组装相互作用获得的卵磷脂/壳聚糖纳米颗粒不仅以高包封率(84.5%)有效地包封了药物,而且还提供了黄芩素的持续释放而没有初始爆发释放。重要的是,离体和体内渗透曲线的分析表明,卵磷脂/壳聚糖纳米颗粒延长了黄芩素在皮肤中的保留,并有效地穿透了角质层的屏障,而不表现出皮肤刺激。
结论:这些结果表明,药物-磷脂复合物在提高包封效率方面具有潜力,并且基于磷脂复合物的自组装卵磷脂/壳聚糖纳米颗粒在设计合理的透皮给药平台以通过增强其在皮肤中的经皮保留和渗透来提高透皮治疗的效率。
OBJECTIVE: Lecithin/chitosan nanoparticles have shown great promise in the transdermal delivery of therapeutic agents. Baicalein, a natural bioactive flavonoid, possesses multiple biological activities against dermatosis. However, its topical application is limited due to its inherently poor hydrophilicity and lipophilicity. In this study, the baicalein-phospholipid complex was prepared to enhance the lipophilicity of baicalein and then lecithin/chitosan nanoparticles loaded with the baicalein-phospholipid complex were developed to improve the transdermal retention and permeability of baicalein.
METHODS: Lecithin/chitosan nanoparticles were prepared by the solvent-injection method and characterized in terms of particle size distribution, zeta potential, and morphology. The in vitro release, the ex vivo and in vivo permeation studies, and safety evaluation of lecithin/chitosan nanoparticles were performed to evaluate the effectiveness in enhancing transdermal retention and permeability of baicalein.
RESULTS: The lecithin/chitosan nanoparticles obtained by the self-assembled interaction of chitosan and lecithin not only efficiently encapsulated the drug with high entrapment efficiency (84.5%) but also provided sustained release of baicalein without initial burst release. Importantly, analysis of the permeation profile ex vivo and in vivo demonstrated that lecithin/chitosan nanoparticles prolonged the retention of baicalein in the skin and efficiently penetrated the barrier of stratum corneum without displaying skin irritation.
CONCLUSIONS: These results indicate the potential of drug-phospholipid complexes in enhancing the entrapment efficiency and self-assembled lecithin/chitosan nanoparticles based on phospholipid complexes in the design of a rational transdermal delivery platform to improve the efficiency of transdermal therapy by enhancing its percutaneous retention and penetration in the skin.