Doxorubicin biocompatible O/W microemulsion stabilized by mixed surfactant containing soya phosphatidylcholine
Doxorubicin biocompatible O/W microemulsion stabilized by mixed surfactant containing soya phosphatidylcholine
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DOI：
10.1016/j.colsurfb.2006.05.005
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发表时间：
2006-08-01
影响因子：
5.8
通讯作者：
Oliveira, A. G.
中科院分区：
文献类型：
--
作者：
Formariz, T. R.;Sarmento, V. H. V.;Oliveira, A. G.
研究了以大豆磷脂酰胆碱(SPC/聚氧乙基甘油三酯40(Eu)/油酸钠(SO)为表面活性剂胆固醇(CHO)的微乳液(ME)。在SPC/Eu/SO质量比为3.5：3.5：3.0时，通过滴定得到了所研究体系的拟三元相图，以表征各组分之间的比例，从而形成清晰的体系。动态光散射结果表明，随着表面活性剂/油相比例的增加，油滴尺寸明显减小。根据组成的不同，ME体系可能表现出触变性行为。未加药和载药ME的表观粘度分别是胆固醇浓度的25倍和13倍。阿霉素(DOX)的正辛醇/水的缓冲分配系数(K-O/B)与pH有关，在pH 6.0以上突然增大。在ME中加入2.24 mg/ml的DOX是可能的。在ME体系中加入DOX增加了体系中使用的所有表面活性剂浓度的液滴尺寸。结果表明，在所研究的pH条件下，DOX与ME的微观结构相互作用，显著提高了药物的溶解度。可以得出结论，所研究的微球作为阿霉素给药的药物载体是一种非常有前途的载体。(C)2006爱思唯尔B.V.保留所有权利。
Microemulsions (ME) containing soya phosphatidylcholine (SPC/polyoxyethylenglycerol trihydroxystearate 40 (EU)/sodium oleate (SO) as surfactant cholesterol (CHO) as oil phase and aqueous buffer were studied. Pseudo-ternary phase diagrams of the investigated systems were obtained at constant SPC/EU/SO weight ratio 3.5:3.5:3.0 by titration, in order to characterize the proportions between the components to form clear systems. The dynamic light scattering results showed that the size of the oil droplets decreases significantly with the ratio of surfactant/oil phase added to system. Depending on the composition ME system could exhibit a thixotropic behavior. The apparent viscosity increased 25- and 13-folds with cholesterol concentration for drug-free and drug-load ME, respectively. It was also verified that the octanol/aqueous buffer partition coefficient (K-O/B) of doxorubicin (DOX) was pH dependent increasing abruptly above pH 6.0. It was possible to incorporate 2.24 mg/ml of DOX into ME. The incorporation of DOX in the ME systems increased the droplets size for all surfactant concentrations used in the system. The results suggest that DOX interacts with the microstructure of the ME at the studied pH increasing significantly the drug solubility. It was possible to conclude that the investigated ME can be a very promising vehicle as drug-carrier for administration of doxorubicin. (c) 2006 Elsevier B.V. All rights reserved.