Mouri Abdelkader, Legrand Philippe, El Ghzaoui Abdeslam, Dorandeu Christophe, Maurel Jean Claude, Devoisselle Jean-Marie
Institut Charles Gerhardt Montpellier, UMR 5253CNRS-ENSCM-UM2-UM1, Equipe MACS, 8 rue de l'Ecole Normale, 34296 Montpellier, France; Medesis Pharma, S.A, Avenue du Golf, L'Orée des Mas, Les Cyprès, 34670 Baillargues, France.
Institut Charles Gerhardt Montpellier, UMR 5253CNRS-ENSCM-UM2-UM1, Equipe MACS, 8 rue de l'Ecole Normale, 34296 Montpellier, France.
Int J Pharm. 2016 Apr 11;502(1-2):117-24. doi: 10.1016/j.ijpharm.2016.01.072. Epub 2016 Feb 4.
Lithium biocompatible microemulsion based on Peceol(®), lecithin, ethanol and water was studied in attempt to identify the optimal compositions in term of drug content, physicochemical properties and stability. Lithium solubilization in microemulsion was found to be compatible with a drug-surfactant binding model. Lithium ions were predominantly solubilized within lecithin head group altering significantly the interfacial properties of the system. Pseudo-ternary phase diagrams of drug free and drug loaded microemulsions were built at constant ethanol/lecithin weight ratio (40/60). Lithium loaded microemulsion has totally disappeared in the Peceol(®) rich part of phase diagram; critical fractions of lecithin and ethanol were required for the formation of stable microemulsion. The effect of lithium concentration on the properties and physical stability of microemulsions were studied using microscopy, Karl Fischer titrations, rheology analyses, conductivity measurements and centrifugation tests. The investigated microemulsions were found to be stable under accelerated storage conditions. The systems exhibited low viscosity and behaved as Newtonian fluid and no structural transition was shown.
研究了基于聚乙二醇单油酸酯(Peceol®)、卵磷脂、乙醇和水的锂生物相容性微乳液,试图确定在药物含量、物理化学性质和稳定性方面的最佳组成。发现锂在微乳液中的增溶与药物-表面活性剂结合模型相符。锂离子主要增溶在卵磷脂头部基团内,显著改变了体系的界面性质。在乙醇/卵磷脂重量比恒定(40/60)的情况下绘制了无药和载药微乳液的拟三元相图。载锂微乳液在相图中富含聚乙二醇单油酸酯(Peceol®)的部分完全消失;形成稳定微乳液需要卵磷脂和乙醇的临界比例。使用显微镜、卡尔费休滴定法、流变学分析、电导率测量和离心试验研究了锂浓度对微乳液性质和物理稳定性的影响。研究发现,所研究的微乳液在加速储存条件下是稳定的。这些体系表现出低粘度,呈牛顿流体行为,未显示结构转变。