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绘制极性非质子溶剂对甘油单油酸酯/油酸体系微观结构和动态相变的影响

Mapping the Impact of a Polar Aprotic Solvent on the Microstructure and Dynamic Phase Transition in Glycerol Monooleate/Oleic Acid Systems.

作者信息

Kazi Marzuka Shoeb, Dehghan Mohammed Hassan

机构信息

Y.B. Chavan College of Pharmacy, Department of Pharmaceutics, Dr. Rafiq Zakaria Campus, Aurangabad, India.

出版信息

Turk J Pharm Sci. 2020 Jun;17(3):307-318. doi: 10.4274/tjps.galenos.2019.26096. Epub 2020 Jun 22.

DOI:10.4274/tjps.galenos.2019.26096
PMID:32636709
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7336036/
Abstract

OBJECTIVES

The impact of incorporating a polar aprotic solvent, dimethyl sulfoxide (DMSO), in glycerol monooleate/oleic acid systems was evaluated briefly to map its influence on the gel microstructure and dynamic phase transition in controlling the performance of a polyene antifungal drug delivery system.

MATERIALS AND METHODS

An gelling fluid precursor system (IGFPS) exhibiting inverse lyotropic liquid crystalline phases was developed by simple solution add-mixture method. Polarized light microscopy, small angle X-ray scattering (SAXS), differential scanning calorimetry (DSC), and oscillatory rheological assessments were performed to ascertain microstructural modulations. The developed system was examined for minimum gelling volume, gelling time, swelling behavior, mucoadhesion, antifungal activity, and drug release.

RESULTS

The SAXS study identifies the coexistence of Im3m cubic phase with HCP P63/mmc hexagonal structures. The SAXS and DSC data highlight DMSO's unique ability to work both as a kosmotropic or chaotropic solvent and to be a function of its concentration. The antifungal test results indicate the concentration of DMSO to be a controlling factor in drug release and diffusion. The drug release kinetic studies reveal that most of the gel samples follow the matrix model and anomalous type release as implied by Peppas model.

CONCLUSION

Finally, the antifungal IGFPS formulated was found to have the required low viscosity, responsive sol-gel phase transition, appreciative mechanical properties, and desirable antifungal effect with sustained drug release performance.

摘要

目的

简要评估在甘油单油酸酯/油酸体系中加入极性非质子溶剂二甲基亚砜(DMSO)对凝胶微观结构和动态相变的影响,以确定其在控制多烯抗真菌药物递送系统性能方面的作用。

材料与方法

通过简单的溶液混合法开发了一种呈现逆溶致液晶相的凝胶流体前体系统(IGFPS)。采用偏光显微镜、小角X射线散射(SAXS)、差示扫描量热法(DSC)和振荡流变学评估来确定微观结构的调制情况。对所开发的系统进行了最小凝胶体积、凝胶化时间、溶胀行为、黏膜粘附性、抗真菌活性和药物释放等方面的研究。

结果

SAXS研究确定了Im3m立方相和HCP P63/mmc六方结构的共存。SAXS和DSC数据突出了DMSO作为促溶剂或离液剂的独特能力及其浓度的作用。抗真菌测试结果表明,DMSO的浓度是药物释放和扩散的控制因素。药物释放动力学研究表明,大多数凝胶样品遵循基质模型和Peppas模型所暗示的异常类型释放。

结论

最后,发现所制备的抗真菌IGFPS具有所需的低粘度、响应性溶胶-凝胶相变、良好的机械性能以及具有持续药物释放性能的理想抗真菌效果。

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