表没食子儿茶素没食子酸酯明胶纳米粒的制备及体外透皮性质研究

Preparation of epigallocatechin-3-gallate-gelatin nanoparticles and detection of transdermal penetration in vitro

目的:制备表没食子儿茶素没食子酸酯-明胶纳米粒(EGCG-N)并研究其体外透皮性。方法:以激光粒度仪测定EGCG-N的粒度及Zeta电位,超滤-HPLC法测定EGCG-N的载药量及包封率,Franz扩散装置检测EGCG-N体外透皮性。结果:所制备的EGCG-N粒径分布均匀,平均粒径为(72.63±0.47)nm,Zeta电位为-28.0mV。EGCG-N中EGCG的载药量和包封率分别为(29.82±2.16)%和(83.91±0.93)%。EGCG-N中EGCG 24 h单位面积累积透过量及皮肤滞留量分别为(133.77±22.79)μg/cm^2和(492.57±37.68)μg/g均明显高于EGCG溶液剂(53.30±21.12)μg/cm^2和(165.88±17.96)μg/g(均P <0.01)。结论:EGCG-N制备简便,能够提高EGCG的经皮渗透能力。

Objective: To prepare the epigallocatechin-3-gallate- gelatin nanoparticles (EGCG-N) and investigate its in vitro transdermal diffusion characteristics. Methods: The particle size, zeta potential and encapsulation efficiency of EGCG-N were measured by laser scattering particle size distribution analyzer and ultrafiltration-HPLC method. The percutaneous diffusion characteristics of the EGCG-N were detected by Franz diffuser device. Results: The EGCG-N had an average size of (72.63±0.47) nm with surface charge of -28.0 mV. The drug- loading capacity and encapsulation efficiency of EGCG were (29.82±2.16)% and (83.91± 0.93 )%, respectively. The cumulative penetration concentration and drug retention concentration of the EGCG-N were (133.77±22.79)μg/cm^2 and (492.57±37.68)μg/g, respectively,which were significant higher than that in EGCG-solution (53.30±21.12)μg/cm^2 and (165.88±17.96)μg/g ( P s<0.01). Conclusion: EGCG-N is prepared simply and can improve the precutaneous permeability of EGCG.