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载醋氯芬酸的泊洛沙姆F108/L81混合聚合物胶束:亲水亲油平衡值对增溶作用的影响

Aceclofenac-loaded pluronic F108/L81 mixed polymeric micelles: effect of HLB on solubilization.

作者信息

Senthilkumar M, Dash Sasmita, Vigneshwari R, Paulraj E

机构信息

Department of Chemistry, Annamalai University, Chidambaram, India.

出版信息

Des Monomers Polym. 2022 Jan 28;25(1):1-11. doi: 10.1080/15685551.2022.2028373. eCollection 2022.

Abstract

Pluronic block copolymers have phase behavioural characteristics which are extensively studied for drug delivery applications. In this study, we explored hydrophilic pluronic F108 (HLB = 27), hydrophobic pluronic L81 (HLB = 2) and their mixed micelles acting as solubilising mediums for model drug aceclofenac. The drug solubilisation and interactions have been analysed using UV-visible spectroscopy, Fluorescence spectroscopy, Rheology studies, Fourier-transform infrared spectroscopy, Scanning electron microscope, Dynamic light scattering, Cloud point and partition coefficient measurements. The investigation from UV-spectrophotometry demonstrated that mixed pluronic entrapped greater number of aceclofenac molecules than both the neat pluronics at same concentration. Excimer formation was evidenced from fluorescence spectra with pyrene as a probe. The rheological studies showed difference in viscosity over low shear range. Studies on FTIR demonstrated probable bonding between the aceclofenac and mixed pluronic molecules. The DLS studies on mixed pluronic showed swelling of micellar diameter from 317.6 nm to 413.5 nm. Thermodynamic parameters of the above system revealed higher partition coefficient value for mixed pluronic and spontaneity in drug solubilisation. This study can be exploited to use a hydrophobic copolymeric micelle in mixed pluronic formulation for better drug solubilisation.

摘要

普朗尼克嵌段共聚物具有相行为特征,这些特征在药物递送应用中得到了广泛研究。在本研究中,我们探索了亲水性普朗尼克F108(HLB = 27)、疏水性普朗尼克L81(HLB = 2)及其混合胶束作为模型药物醋氯芬酸的增溶介质。使用紫外可见光谱、荧光光谱、流变学研究、傅里叶变换红外光谱、扫描电子显微镜、动态光散射、浊点和分配系数测量对药物增溶和相互作用进行了分析。紫外分光光度法的研究表明,在相同浓度下,混合普朗尼克比两种纯普朗尼克捕获的醋氯芬酸分子数量更多。以芘为探针的荧光光谱证明了激基缔合物的形成。流变学研究表明在低剪切范围内粘度存在差异。傅里叶变换红外光谱研究表明醋氯芬酸与混合普朗尼克分子之间可能存在键合。对混合普朗尼克的动态光散射研究表明胶束直径从317.6 nm膨胀到413.5 nm。上述体系的热力学参数表明混合普朗尼克具有更高的分配系数值以及药物增溶的自发性。本研究可用于在混合普朗尼克制剂中使用疏水性共聚物胶束以实现更好的药物增溶。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a31/8803101/9b084a003ff7/TDMP_A_2028373_F0001_OC.jpg

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