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基于硬脂酸盐有机凝胶-明胶水凝胶的双凝胶:物理化学、热学、力学表征及体外药物递送应用

Stearate organogel-gelatin hydrogel based bigels: physicochemical, thermal, mechanical characterizations and in vitro drug delivery applications.

作者信息

Sagiri Sai Sateesh, Singh Vinay K, Kulanthaivel Senthilguru, Banerjee Indranil, Basak Piyali, Battachrya M K, Pal Kunal

机构信息

Department of Biotechnology and Medical Engineering, National Institute of Technology, Rourkela 769008, India.

School of Bioscience & Engineering, Jadavpur University, Kolkata 700032, India.

出版信息

J Mech Behav Biomed Mater. 2015 Mar;43:1-17. doi: 10.1016/j.jmbbm.2014.11.026. Epub 2014 Dec 5.

DOI:10.1016/j.jmbbm.2014.11.026
PMID:25549573
Abstract

Over the past decade, researchers have been trying to develop alternative gel based formulations in comparison to the traditional hydrogels and emulgels. In this perspective, bigels were synthesized by mixing gelatin hydrogel and stearic acid based organogel by hot emulsification method. Two types of bigels were synthesized using sesame oil and soy bean oil based stearate organogels. Gelatin based emulgels prepared using sesame oil and soy bean oil were used as the controls. Microscopic studies revealed that the bigels contained aggregates of droplets, whereas, emulgels showed dispersed droplets within the continuum phase. The emulgels showed higher amount of leaching of oils, whereas, the leaching of the internal phase was negligible from the bigels. Presence of organogel matrix within the bigels was confirmed by XRD, FTIR and DSC methods. Bigels showed higher mucoadhesive and mechanical properties compared to emulgels. Cyclic creep-recovery and stress relaxation studies confirmed the viscoelastic nature of the formulations. Four elemental Burger's model was employed to analyze the cyclic creep-recovery data. Cyclic creep-recovery studies suggested that the deformation of the bigels were lower due to the presence of the organogels within its structure. The formulations showed almost 100% recovery after the creep stage and can be explained by the higher elastic nature of the formulations. Stress relaxation study showed that the relaxation time was higher in the emulgels as compared to the bigels. Also, the % relaxation was higher in emulgels suggesting its fluid dominant nature. The in vitro biocompatibility of the bigels was checked using human epidermal keratinocyte cell line (HaCaT). Both emulgels and bigels were biocompatible in nature. The in vitro drug (ciprofloxacin) release behavior indicated non-Fickian diffusion of the drug from the matrices. The drug release showed good antimicrobial effect against Escherichia coli. Based on the results, it was concluded that the developed bigels may have huge potential to be used as alternatives to emulgels.

摘要

在过去十年中,与传统水凝胶和乳胶相比,研究人员一直在尝试开发基于凝胶的替代配方。从这个角度来看,通过热乳化法将明胶水凝胶和硬脂酸基有机凝胶混合合成了双凝胶。使用基于芝麻油和大豆油的硬脂酸酯有机凝胶合成了两种类型的双凝胶。使用芝麻油和大豆油制备的基于明胶的乳胶用作对照。显微镜研究表明,双凝胶含有液滴聚集体,而乳胶在连续相中显示出分散的液滴。乳胶显示出较高的油浸出量,而双凝胶中内相的浸出可以忽略不计。通过XRD、FTIR和DSC方法证实了双凝胶中有机凝胶基质的存在。与乳胶相比,双凝胶显示出更高的粘膜粘附性和机械性能。循环蠕变恢复和应力松弛研究证实了配方的粘弹性性质。采用四元素伯格模型分析循环蠕变恢复数据。循环蠕变恢复研究表明,由于其结构中存在有机凝胶,双凝胶的变形较小。在蠕变阶段后,配方显示几乎100%的恢复,这可以通过配方较高的弹性性质来解释。应力松弛研究表明,乳胶中的松弛时间比双凝胶中的更高。此外,乳胶中的%松弛更高,表明其以流体为主导的性质。使用人表皮角质形成细胞系(HaCaT)检查双凝胶的体外生物相容性。乳胶和双凝胶在本质上都是生物相容的。体外药物(环丙沙星)释放行为表明药物从基质中的非菲克扩散。药物释放对大肠杆菌显示出良好的抗菌效果。基于这些结果,得出的结论是,开发的双凝胶作为乳胶的替代品可能具有巨大的潜力。

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