吡罗昔康纳米结构脂质载体的制备及体外透皮特性研究

Preparation and Transdermal Absorption in vitro of Piroxicam Nanostructured Lipid Carrier

目的:制备吡罗昔康纳米结构脂质载体,并考察其体外透皮吸收性质。方法:采用热熔乳化超声-低温固化法制备吡罗昔康纳米结构脂质载体,并对其外观、微观形态、粒径分布、多分散系数(Pd I)、Zeta电位等理化性质进行评价;同时采用Franz扩散池法对其体外透皮吸收性质进行考察。结果:制备的吡罗昔康纳米结构脂质载体外观呈淡蓝色透明状液体,透射电镜可见呈圆整球状分布,平均粒径为(106.4±31.6)nm,Pd I为(0.217±0.07),Zeta电位为(-31.6±2.5)m V;吡罗昔康纳米结构脂质载体经12 h体外药物累积透皮量显著高于吡罗昔康溶液。结论:纳米结构脂质载体可以显著提高吡罗昔康的体外累积透皮量,有望成为吡罗昔康的新型局部给药制剂。

Objective： To prepare piroxicam nanostructured lipid carrier and investigate its transdermal absorption behavior in vitro. Methods： Piroxicam nanostructured lipid carrier was prepared by a melt-emulsion ultrasonication and low temperature-solidifica- tion method. The physicochemical properties such as appearance, morphology, particle size distribution, PdI and zeta potential of pi- roxicam nanostructured lipid carrier were evaluated. The transdermal absorption in vitro was investigated using Franz diffusion ceils. Results ： Piroxicam nanostructured lipid carrier was clear and transparent with small spherical shape as seen under a transmission elec- tron microscope. The particle size distribution, PdI and zeta potential was （106.4 ± 31. 6） nm, （0.217 ± 0.07） and （ -31.6± 2.5 ） mV, respectively. Piroxicam nanostructured lipid carrier had higher cumulative transdermal amount in 12 h than piroxicam solution. Conclusion： The nanostructured lipid carrier can remarkably improve piroxicam permeation into skin, which provides reference for the new dosage form for the topical use of piroxicam.