神经酰胺修饰醇质体的制备与表征

Preparation and Characterization of Ceramide Modified Ethosomes

摘要:

为了提高醇质体的稳定性，作者采用神经酰胺Ⅲ（ceramide III，Cer3） 修饰醇质体，首先考察了Cer3质量浓度对醇质体稳定性的影响，后将视黄醇棕榈酸酯（retinyl palmitate，RP） 作为脂溶性活性物载入Cer3醇质体，研究了RP-Cer3醇质体的稳定性、稳定机制及体外释放性能。结果显示，当Cer3质量浓度为1 mg/mL时，Cer3醇质体的稳定性最好。RP-Cer3醇质体的RP质量浓度为2 mg/mL时，粒径为（68.4±1.1） nm，室温储存120 d，外观和粒径均无明显变化。X射线衍射和全反射傅里叶红外光谱表明RP被很好地包载于醇质体中，同时，红外光谱图也说明了RP与醇质体存在氢键相互作用。研究表明，Cer3的加入会降低醇质体流动性从而提高其稳定性，且RP-Cer3醇质体具有较好的体外释放性能。

Abstract:

In order to improve the stability of ethosomes, ceramide III (Cer3) was used to modify the ethosomes for the first time. The effect of Cer3 amount on the stability of ethosomes was investigated. Subsequently, retinyl palmitate (RP) was loaded into Cer3 ethosomes as a lipid-soluble active substance to investigate the stability, stabilization mechanism and in vitro release performance of RP-Cer3 ethosomes. The results showed that the best stability of Cer3 ethosomes was achieved at 1 mg/mL Cer3. When the RP content of RP-Cer3 ethosomes was 2 mg/mL, the particle size was (68.4±1.1) nm. The appearance and particle size insignificantly changed when stored at room temperature for 120 d. X-ray diffraction (XRD) and total reflection Fourier infrared (FTIR) indicated that RP was well encapsulated in the ethosomes, at the meanwhile, FTIR also indicated that there was hydrogen bond interaction between RP and the ethosomes. The results showed that the addition of Cer3 could reduce the fluidity of ethosomes and thus improve their stability, and RP-Cer3 ethosomes had better in vitro release performance.