盐酸洛哌丁胺-酪蛋白纳米复合物的制备及体外释放的研究

Study on the preparation and release in vitro of Loperamide-loaded casein nanoparticles

目的 制备载盐酸洛哌丁胺（LOP）的酪蛋白（Cas）纳米粒,考察其体外释药行为。方法 利用Cas在水中能自组装成稳定的纳米结构特性,制备了载LOP的Cas纳米复合物（LOP-Cas）,并以包封率和载药量为指标优化了制备工艺。通过透射电镜和差示扫描量热法表征了LOP-Cas,并研究了LOP-Cas在不同环境下的体外释放行为。结果 运用优化工艺制备的LOP-Cas近球形,具有相对光滑的表面,平均包封率为95.10%±2.83%,平均载药量为1.86%±0.06%,平均粒径为97.1±6.5 nm,Zeta电位为-10.92±1.08 mV;LOP-Cas在人工胃液环境中,2 h内释放87.12%;而在无人工胃液作用的环境中,LOP-Cas显示出了一定的缓释特性,12 h内仅释放了75.85%。结论 成功制备了LOP-Cas,其在人工胃液中能迅速释放。

OBJECTIVE To prepare Loperamide hydrochloride（LOP） loaded casein（Cas） nanoparticles and to evaluate its release behavior. METHODS LOP - Cas was prepared using the self - assembly characters of Cas in water and the preparation method was optimized by using entrapment efficiency（EE） and loading efficiency（LE） as indexes. Then,TEM and DSC were adopted to character- ize LOP - Cas. Additionally,in vitro release behaviors of LOP - Cas in different circumstances were also evaluated. RESULTS The LOP - Cas prepared with optimal method was spherical and relatively smooth. The particle size and Zeta potential of LOP - Cas were 97.1±6.5 nm（PD=0.451±0.123） and -10.92±1.08 mV with the EE and LE of 95.10%±2.83% and 1.86%±0.06%, respectively. The cumulative release of LOP - Cas in the stimulated gastric fluid for 2 h was 87.12%, whereas the release in PBS （pH7. 4） for 12 h was only 75.85 %, which showed a sustained release characterization. CONCLUSION LOP - Cas is successfully prepared and it can rapidly release in stimulated gastric fluid,laying a base for further research in vivo.