难溶性药物姜黄素作为纳米晶稳定剂制备Pickering乳剂的研究

Preparation of poorly soluble drug curcumin nanocrystalline self-stabilized Pickering emulsion

目的使用姜黄素纳米晶(curcumin nanocrystalline,Cur-NC)作为固体颗粒稳定剂,制备Cur-NC自稳定Pickering乳剂(Cur-NC self-stabilized Pickering emulsion,Cur-NCSPE)。方法采用高压均质机制备Cur-NCSPE;比较不同的均质压力对Cur-NC粒径的影响,考察Cur-NC的加入量对Cur-NCSPE形成的影响,用光学显微镜、扫描电子显微镜观察乳剂的形态与结构,对Cur-NCSPE的稳定性及体外药物释放进行考察。结果随着高压均质压力的增加,Cur-NC的粒径逐渐减小,当高压均质压力大于100 MPa后,Cur-NC的粒径变化趋于平稳;随着姜黄素(curcumin,Cur)投入量的增加,Cur-NC对油滴的包裹量增大,乳滴的粒径逐渐减小,当加入的药物量能够将油滴完全包裹时,继续增大药物量对乳滴粒径的影响不再明显。Cur-NCSPE的稳定性比Cur-NC和Cur高,Cur-NCSPE的体外释放速率比Cur-NC和Cur的释放速率显著加快。结论成功制备了Cur-NCSPE,有望为中药难溶性成分提供新的口服给药技术平台。

Objective To prepare curcumin nanocrystalline（Cur-NC） self-stabilized Pickering emulsion（Cur-NCSPE）. Methods Cur-NCSPE was prepared by high pressure homogenization. The influences of homogenization pressure on Cur-NC size and drug content on Cur-NCSPE formation were studied. The morphology and structure of emulsion droplets were observed by optical microscope and scanning electron microscope. Furthermore, the stability and in vitro release properties of Cur-NCSPE were evaluated. Results The particle size of Cur-NC was slightly changed when homogeneous pressure was greater than 100 MPa. With the increase of Cur, the amount of Cur-NC on the surface of oil droplets increases, and the particle size decreases. When the amount of drug added can completely cover the surface of oil droplets, increasing the amount of drug had little effect on the particle size. Cur-NCSPE was more stable than Cur-NC and Cur, and the in vitro release rate of Cur-NCSPE was significantly higher than that of Cur-NC and Cur coarse power. Conclusion The Cur-NCSPE is prepared successfully, which is expected to provide a novel oral administration technology platform for the poorly soluble drugs.