Lo Jen-Ting, Lee Tzer-Min, Chen Bing-Hung
Department of Chemical Engineering, National Cheng Kung University, Tainan 70101, Taiwan.
Institute of Oral Medicine, National Cheng Kung University, Tainan 70101, Taiwan.
Materials (Basel). 2016 Sep 7;9(9):761. doi: 10.3390/ma9090761.
The strategy using nonionic microemulsion as a solubilizer for hydrophobic drugs was studied and is demonstrated in this work. The aqueous phase behaviors of mixed nonionic surfactants with various oils at 37 °C are firstly constructed to give the optimal formulations of nonionic microemulsions with applications in the enhanced solubilization of the model hydrophobic drug, paclitaxel, at 37 °C. Briefly, the suitable oil phase with paclitaxel significantly dissolved is microemulsified with appropriate surfactants. Surfactants utilized include Tween 80, Cremophor EL, and polyethylene glycol (4.3) cocoyl ether, while various kinds of edible oils and fatty esters are used as the oil phase. On average, the apparent solubility of paclitaxel is increased to ca. 70-100 ppm in the prepared microemulsions at 37 °C using tributyrin or ethyl caproate as the oil phases. The sizes of the microemulsions attained are mostly from ca. 60 nm to ca. 200 nm. The cytotoxicity of the microemulsion formulations is assessed with the cellular viability of 3T3 cells. In general, the cell viability is above 55% after 24 h of cultivation in media containing these microemulsion formulations diluted to a concentration of total surfactants equal to 50 ppm and 200 ppm.
研究了使用非离子微乳液作为疏水性药物增溶剂的策略，并在本工作中进行了展示。首先构建了在37°C下混合非离子表面活性剂与各种油的水相行为，以给出非离子微乳液的最佳配方，用于在37°C下增强模型疏水性药物紫杉醇的增溶作用。简而言之，将能显著溶解紫杉醇的合适油相与适当的表面活性剂进行微乳化。使用的表面活性剂包括吐温80、聚氧乙烯蓖麻油和聚乙二醇（4.3）椰油醚，而各种食用油和脂肪酸酯用作油相。平均而言，在37°C下使用丁酸甘油酯或己酸乙酯作为油相制备的微乳液中，紫杉醇的表观溶解度增加到约70 - 100 ppm。所获得的微乳液大小大多在约60 nm至约200 nm之间。用3T3细胞的细胞活力评估微乳液制剂的细胞毒性。一般来说，在含有稀释至总表面活性剂浓度等于50 ppm和200 ppm的这些微乳液制剂的培养基中培养24小时后，细胞活力高于55%。
