Li Qiu-Ping, Dai Jun-Dong, Zhai Wen-Wen, Jiang Qiao-Li
Zhongguo Zhong Yao Za Zhi. 2014 Oct;39(20):3936-44.
The objective of the study was to prepare and evaluate the quality of curcumin-piperinedual drug loaded self-microemulsifying drug delivery system(Cur-PIP-SMEDDS). Simplex lattice design was constructed using optimal oil phase, surfactant and co-surfactant concentration as independent variables, and the curcumin and piperine were used as model drugs to optimize Cur-PIP-SMEDDS formulation. In the present study, the drug loadings of curcumin and piperine, mean particle size of Cur-PIP-SMEDDS were made as indicators, and the experiment design, model building and response surface analysis were established using Design Expert 8. 06 software to optimize and verify the composition of SMEDDS formulation. The quality of Cur-PIP-SMEDDS was evaluated by observing the appearance status, transmission electron microscope micrographs and determining particle diameter, electric potential, drug entrapment efficiency and drug loading of it. As a result, the optimal formulation of SMEDDS was CapryoL 90-Cremophor RH40-TranscutoL HP (10:60:30). The appearance of Cur-PIP-SMEDDS remained clarified and transparent, and the microemulsion droplets appeared spherical without aggregation with uniform particle size distribution. The mean size of microemulsion droplet formed from Cur-PIP-SMEDDS was 15.33 nm, the drug loading of SMEDDS for Cur and PIP were 40.90 mg · g(-1) and 0.97 mg · g(-1), respectively, the drug entrapment efficiency were 94.98% and 90.96%, respectively. The results show that Cur-PIP-SMEDDS can increase the solubility and stability of curcumin significantly, in the expectation of enhancing the bioavailability of it. Taken together, these findings can provide the reference to a preferable choice of the Cur formulation and contribute to therapeutic application in clinical research.
本研究的目的是制备并评价姜黄素 - 胡椒碱双药负载自微乳化给药系统（Cur-PIP-SMEDDS）的质量。以最佳油相、表面活性剂和助表面活性剂浓度为自变量构建单纯形格子设计，以姜黄素和胡椒碱作为模型药物来优化Cur-PIP-SMEDDS制剂。在本研究中，以姜黄素和胡椒碱的载药量、Cur-PIP-SMEDDS的平均粒径为指标，使用Design Expert 8.06软件进行实验设计、模型构建和响应面分析，以优化和验证SMEDDS制剂的组成。通过观察Cur-PIP-SMEDDS的外观状态、透射电子显微镜照片以及测定其粒径、电位、药物包封率和载药量来评价其质量。结果表明，SMEDDS的最佳制剂为CapryoL 90-聚氧乙烯氢化蓖麻油RH40-肉豆蔻酸异丙酯（10:60:30）。Cur-PIP-SMEDDS的外观保持澄清透明，微乳液滴呈球形，无聚集，粒径分布均匀。由Cur-PIP-SMEDDS形成的微乳液滴的平均粒径为15.33 nm，SMEDDS对Cur和PIP的载药量分别为40.90 mg·g(-1)和0.97 mg·g(-1)，药物包封率分别为94.98%和90.96%。结果表明，Cur-PIP-SMEDDS能显著提高姜黄素的溶解度和稳定性，有望提高其生物利用度。综上所述，这些研究结果可为姜黄素制剂的优选提供参考，并有助于其在临床研究中的治疗应用。
