用于组合活性物透皮共递送的环糊精复合物传质体的制备与表征

Preparation and characterization of active-in-cyclodextrin-intransfersomes for combined drug transdermal co-delivery

以卵磷脂、胆固醇、表面活性剂为壁材制备传质体,通过薄膜水合法分别将苯乙基间苯二酚(PR)与白藜芦醇/羟丙基-β-环糊精(RSV/HP-β-CD)复合物包封在传质体的磷脂双分子层和水性隔室中,获得环糊精复合物传质体(DCTs)。研究了膜软化剂及其添加量、添加方式对DCTs粒径、PDI、Zeta电位、包封率的影响。结果表明,使用0.012 mol/L的T20制得的DCTs粒径较小,为112.43 nm,PDI为0.16,Zeta电位为-34.90 mV,PR与RSV包封率最高,分别为77.07%和60.67%。通过对DCTs体外释放、透皮、细胞毒性及B16-F10细胞内黑色素含量研究,发现DCTs实现了活性物缓释并防止活性物降解,减小了组合活性物透皮递送的渗透性差异,降低了游离活性物的细胞毒性,增强了组合活性物的协同效果,从而减少了B16-F10细胞的黑素生成。

Active-in-cyclodextrin-in-transfersomes(DCTs),which encapsulated phenylethyl resorcinol(PR)and resveratrol/hydroxypropyl-β-cyclodextrin(RSV/HP-β-CD)inclusion complexes in the phospholipid bilayer and aqueous compartments of the transfersomes,were prepared by thin film hydration using lecithin,cholesterol,and surfactant as encapsulation materials.The effects of edge activator,their concentrations and addition methods on the particle size,PDI,Zeta potential and encapsulation efficiency of DCTs were studied.Results show that the particle size of DCTs prepared by 0.012 mol/L Tween 20 is 112.43 nm,PDI is 0.16,Zeta potential is-34.90 mV,and the high entrapment efficiency of PR and RSV are achieved as 77.07%and 60.67%,respectively.Through in vitro release,transdermal,cytotoxicity and melanin content in B16-F10 cells of DCTs,it was found that DCTs achieved drug sustained release and prevented drug degradation,reduced the permeability difference of transdermal delivery of combination drugs,decreased the cytotoxicity of free drugs,enhanced the synergistic effect of the combination drug,and reduced the melanin content of B16-F10 cells.