Role of medium-chain fatty acids in the emulsification mechanistics of self-micro-emulsifying lipid formulations.

Role of medium-chain fatty acids in the emulsification mechanistics of self-micro-emulsifying lipid formulations.
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DOI:
10.1016/j.jsps.2014.02.005
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发表时间:
2014-12
影响因子:
4.1
通讯作者:
Hasan, Naser M. Y.
Hasan, Naser M. Y.
中科院分区:
医学3区
文献类型:
--
作者:
Hasan, Naser M. Y.

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本研究的目的是设计和开发稳定的O/W型微乳液,包括米格列醇812、伊维特988和他格特TO作为非离子表面活性剂。这是基于颗粒大小测量和相行为研究。在不同的模拟生理条件下,还证实了中链单甘油酯/双甘油酯在脂肪基质中加入乳化机理过程中的经验作用。考察了油、助表面活性剂和表面活性剂等不同关键成分的脂类混合物的自乳化效率。用激光衍射和光散射技术测量了液滴直径。进行了平衡相研究,确定了脂类-水体系的相界。微乳体系由Miglyol 812、Imwitor 988和Tagat TO的混合物制成。优化处方为:{Miglyol812/Imwitor988}和泰格特,在水乳剂中自乳化,水滴直径为∼50 nm。相平衡图显示,在没有任何液晶材料存在的情况下,在水溶区(L2)有显著的增强。通过混合{Miglyol 812/Imwitor 988}和Tagat TO作为非离子表面活性剂,开发了潜在的SMEDDS配方,以提高难溶化合物的生物利用度。“扩散和搁浅”似乎是乳化的主要机制。
The objective of the present study was to design and develop stable o/w microemulsions comprising Miglyol 812, Imwitor 988 and Tagat TO as a non ionic surfactant. This was based on particle size measurements and phase behavior studies. The empirical role of incorporating medium-chain mono/di-glycerides in the lipid matrix in the mechanistic processes of emulsification was also established in various simulating physiological conditions. The efficiency of self-emulsification was evaluated under conditions of varying key compositions in the lipid mixtures; oil, cosurfactant and surfactant. Droplet diameter was measured using laser diffraction and light scattering techniques. Equilibrium phase studies were performed and phase boundaries were determined for the lipid–water systems. Microemulsion systems were produced from blends of Miglyol 812, Imwitor 988 and Tagat TO. An optimized formulation consisted of {Miglyol 812/Imwitor 988} and Tagat TO spontaneously self-emulsified in water producing dispersions with droplet diameters of ∼50 nm. Phase equilibrium diagrams have revealed significant enhancement in the water-solubilized region (L2) without any presence of liquid crystalline materials. Potential SMEDDS formulations for the bioavailability enhancement of poorly water-soluble compounds were developed by mixing blends of {Miglyol 812/Imwitor 988} and Tagat TO as a non-ionic surfactant. ‘Diffusion and stranding’ appears to be the dominant mechanism of emulsification.
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