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该研究的目的在于制备姜黄素-胡椒碱复方自微乳给药系统(Cur-PIP-SMEDDS),并对其质量进行评价。该研究通过选择合适的油相、表面活性剂和助表面活性剂,以姜黄素和胡椒碱为模型药物,采用单纯形网格法优化设计Cur-PIPSMEDDS处方;以乳剂的载药量、平均粒径为评价指标,通过Design Expert 8.06软件进行试验设计和模型构建,响应面数据分析优化和验证最佳处方组成。通过观察微乳外观和微观形态并测定其粒径、电位、包封率及载药量对其进行质量评价。结果显示优化得Cur-PIP-SMEDDS最佳处方为丙二醇单辛酸酯(Capryol 90)-聚氧乙烯氢化蓖麻油(Cremophor RH40)-二乙二醇单乙基醚(Transcutol HP)(10∶60∶30),所形成的微乳外观澄清、透明,呈圆球型,粒径分布均匀,平均粒径为(15.33±0.80)nm,姜黄素和胡椒碱的载药量分别为40.90,0.97 mg·g-1,包封率分别为94.98%,90.96%。研究表明Cur-PIP-SMEDDS可以显著改善姜黄素的水溶性和稳定性,有望提高姜黄素的口服生物利用度,以期为其剂型开发提供新的思路和方法,进而促进其在临床上的应用。
The purpose of this study was to prepare Cur-PIP-SMEDDS and assess the quality of curcumin-piperine self-microemulsion system. In this study, curcumin and piperine were selected as model drugs by selecting appropriate oil phase, surfactant and cosurfactant, and the formulation of Cur-PIPSMEDDS was optimized by simplex grid method. The drug loading of emulsion, As an evaluation index, Design Design and Model Building were done with Design Expert 8.06 software. Response surface data analysis was used to optimize and validate the optimal formulation. The quality of microemulsion was evaluated by observing its appearance and microscopic morphology and measuring the particle size, potential, entrapment efficiency and drug loading. The results showed that the optimized formulation of Cur-PIP-SMEDDS was Capryol 90-Cremophor RH40-Transcutol HP (10:60 : 30). The formed microemulsion has the appearance of clear, transparent and spherical shape with uniform particle size distribution (15.33 ± 0.80) nm. The drug loadings of curcumin and piperine were 40.90 and 0.97 mg · G-1, encapsulation efficiency were 94.98%, 90.96%. Cur-PIP-SMEDDS can significantly improve the water solubility and stability of curcumin, which is expected to improve the oral bioavailability of curcumin in order to provide new ideas and methods for the formulation development of curcumin, thereby further promoting its clinical application.