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用于局部递送抗菌剂的脱水山梨醇单硬脂酸酯和芝麻油基有机凝胶的开发与表征

Development and characterization of sorbitan monostearate and sesame oil-based organogels for topical delivery of antimicrobials.

作者信息

Singh Vinay K, Pramanik Krishna, Ray Sirsendu S, Pal Kunal

机构信息

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

出版信息

AAPS PharmSciTech. 2015 Apr;16(2):293-305. doi: 10.1208/s12249-014-0223-7. Epub 2014 Oct 4.

Abstract

The current study explains the development of sorbitan monostearate and sesame oil-based organogels for topical drug delivery. The organogels were prepared by dissolving sorbitan monostearate in sesame oil (70°C). Metronidazole was used as a model antimicrobial. The formulations were characterized using phase contrast microscopy, infrared spectroscopy, viscosity, mechanical test, and differential scanning calorimetry. Phase contrast microscopy showed the presence of needle-shaped crystals in the organogel matrix. The length of the crystals increased with the increase in the sorbitan monostearate concentration. XRD studies confirmed the amorphous nature of the organogels. Viscosity study demonstrated shear thinning behavior of the organogels. The viscosity and the mechanical properties of the organogels increased linearly with the increase in the sorbitan monostearate concentration. Stress relaxation study confirmed the viscoelastic nature of the organogels. The organogels were biocompatible. Metronidazole-loaded organogels were examined for their controlled release applications. The release of the drug followed zero-order release kinetics. The drug-loaded organogels showed almost similar antimicrobial activity against Escherichia coli when compared to the commercially available Metrogyl® gel. In gist, it can be proposed that the developed organogels had sufficient properties to be used for controlled delivery of drugs.

摘要

本研究阐述了用于局部给药的单硬脂酸山梨坦和芝麻油基有机凝胶的开发。通过将单硬脂酸山梨坦溶解在芝麻油中(70°C)制备有机凝胶。甲硝唑用作模型抗菌剂。使用相差显微镜、红外光谱、粘度、力学测试和差示扫描量热法对制剂进行表征。相差显微镜显示有机凝胶基质中存在针状晶体。晶体长度随单硬脂酸山梨坦浓度的增加而增加。X射线衍射研究证实了有机凝胶的无定形性质。粘度研究表明有机凝胶具有剪切变稀行为。有机凝胶的粘度和力学性能随单硬脂酸山梨坦浓度的增加而线性增加。应力松弛研究证实了有机凝胶的粘弹性性质。有机凝胶具有生物相容性。对负载甲硝唑的有机凝胶进行了控释应用研究。药物释放遵循零级释放动力学。与市售的灭滴灵凝胶相比,载药有机凝胶对大肠杆菌显示出几乎相似的抗菌活性。总之,可以认为所开发的有机凝胶具有足够的性质可用于药物的控释。

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