丹皮酚自微乳经皮给药系统的处方优选及药剂学性质评价

Preparation of Paeonol Self-microemulsion Transdermal Delivery System with Peppermint Oil as Carrier

目的:制备丹皮酚自微乳给药系统并评价其透皮吸收特性。方法:采用加乳化剂滴定法绘制伪三元相图,筛选乳化剂、助乳化剂的种类及其各组分比例,考察丹皮酚自微乳的最大载药量,丹皮酚自微乳最优处方加入50倍量水乳化后,通过透射电镜观察丹皮酚自微乳的外观形态,利用激光粒度仪测定粒径分布及Zeta电位,采用Franz扩散池法考察丹皮酚自微乳的透皮吸收特性。结果:丹皮酚自微乳以薄荷油为油相,乳化剂为聚山梨酯-80,助乳化剂为无水乙醇,以上各组分比例为2∶6∶2,最大载药量100 mg·g^(-1),丹皮酚自微乳加水乳化后,外观为规整的球形,分布较均匀,粒径(63.2±0.27)nm,Zeta电位(0.14±0.29)mV;透皮吸收12 h时,丹皮酚自微乳的单位面积累计经皮渗透量589.10μg·cm-2。结论:制备的丹皮酚自微乳给药系统澄清透明、粒径适宜、性质稳定,符合自微乳制剂的要求,且体外透皮吸收效果较好。

Objective： To prepare paeonol self-microemulsion system and evaluate its transdermal absorption characteristics. Method： The pseudo-ternary phase diagram was prepared by adding the emulsifier titration method, the types and components of emulsifiers and co-emulsifier were screened, and the maximum drug loading of paeonol self-microemulsion was determined. The appearance of the microemulsion was observed by transmission electron microscopy （TEM）. The particle size distribution and Zeta potential of the microemulsion were determined by laser scattering particle size analyzer. The transdermal absorption characteristics of paeonol self-microemulsion were investigated by Franz diffusion cell method. Result： Taking peppermint oil as the oil phase, tween-80 as the emulsifier and absolute ethanol as the co-emulsifier, and the ratio of these components was 2 ： 6 ： 2. The maximum drug loading of paeonol self-microemulsion was 100 mg ·g^-1 its appearance was regularspherical, the average particle size was （63.2 ± 0.27） nm and the Zeta potential was （0.14 ± 0.29） mV. The cumulative release amount of paeonol in the self-microemulsion was 589.10 μg· cm^-1 per unit area at 12 h. Conclusion： The prepared paeonol self-microemulsion system is clear and transparent with stable properties, its particle size is suitable, which is in accordance with the requirement of self-microemulsion preparation, and the transdermal absorption effect of this preparation is good.