熊果苷磷脂复合物的制备、表征及理化性质研究

Preparation, characterization and physicochemical properties of arbutin phospholipid complex

目的制备熊果苷磷脂复合物(APC)以改善熊果苷的皮肤通透性并探讨其形成机制。方法采用溶剂蒸发法制备APC,差示扫描量热法(DSC)、X射线衍射(XRD)、红外光谱(IR)、1H核磁共振(1H-NMR)和扫描电子显微镜和透射电子显微镜用于分析APC的形成机制,并对APC的溶解度、皮肤渗透和酪氨酸酶抑制能力进行测定。结果分析表明磷脂和熊果苷分子之间弱的相互作用力形成了APC;APC中的熊果苷在正辛醇中的溶解度从1.29μg/mL增加到9.54μg/mL,APC的形成有效地提高了熊果苷的亲脂性;体外释放研究中APC展现出持续释放行为;体外渗透研究表明,熊果苷难以通过皮肤到达皮下组织,但APC显示出强大的渗透能力,其渗透通量从0.02 mg/cm2提高到0.42 mg/cm2;酶活性研究中APC的酪氨酸酶活性的抑制效果约为熊果苷的1.85倍。结论复合物的形成提高了熊果苷的生物利用度,并且具有较高的药用和美白应用潜力。

Objectives To prepare arbutin phospholipid complex(APC) to improve the skin permeability of arbutin and discuss the formation mechanism of APC. Methods Solvent evaporation method was used to prepare APC. The formation of APC was confirmed by differential scanning calorimetry(DSC), X-ray diffraction(XRD), infrared spectroscopy(IR), ~1H nuclear magnetic resonance(~1H-NMR), scanning electron microscopy(SEM) and transmission electron microscope(TEM). The solubility, skin permeability and the ability to inhibit tyrosinase of APC were evaluated. Results The analysis showed that the weak interaction between phospholipid and arbutin molecules formed APC. The solubility of arbutin in APC in n-octanol increased from 1.29 μg/mL to 9.54 μg/mL, and the formation of APC effectively increased the lipophilicity of arbutinn. In vitro release study demonstrated that APC exhibited sustained release behavior. Ex vitro penetration studies showed that arbutin was difficult to reach the subcutaneous tissue through the skin, but APC showed strong penetration ability, of which permeation flux was improved from 0.02 mg/cm^2 to 0.42 mg/cm^2. Enzyme inhibitory activity test showed that the inhibition of APC on tyrosinase activity was 1.85 times of arbutin. Conclusions The formation of the complex improved the bioavailability of arbutin, and the complex held higher application potential for medicinal and cosmetic.