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开发和评价具有增强皮肤渗透性能的生物相容的局部凡士林-液晶制剂。

Development and Evaluation of Biocompatible Topical Petrolatum-liquid Crystal Formulations with Enhanced Skin Permeation Properties.

机构信息

Department of Pharmacy, Kut University College.

Department of Pharmaceutics, College of Pharmacy, University of Basrah.

出版信息

J Oleo Sci. 2022 Mar 2;71(3):459-468. doi: 10.5650/jos.ess21344. Epub 2022 Feb 15.

DOI:10.5650/jos.ess21344
PMID:35173089
Abstract

Transdermal administration represents a major advancement over traditional pharmaceutical dosing methods. However, a frequent issue is inadequate penetration of the active medicinal component through the skin. As a result, in the current research, we assessed the utility of newly developed petrolatum-liquid crystal (LC) ointment formulations and characterized their biocompatibility and function in the transdermal drug delivery system. To begin, we made petrolatum-LC formulations using p-aminobenzoic acid (PABA) as a hydrophilic model molecule. The viscosity, small-angle X-ray scattering (SAXS), particle diameters, and z-potential were measured to assess the physicochemical properties of the formulations. A dialysis release technique was used to evaluate medication release from petrolatum-LC formulations. In vitro testing was performed to determine the potential to enhance skin penetration. The biocompatibility of the produced formulations was further tested using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay and single-cell gel electrophoresis. According to the results, the novel petrolatum-LC formulations are biocompatible and effective in forming hexosomes. PABA skin penetration was significantly enhanced by the new petrolatum-LC formulations. According to this study, petroleum-LC formulations are more efficient than commercial petrolatum in terms of skin permeability improvement and PABA skin concentration.

摘要

经皮给药是对传统药物给药方法的重大改进。然而,一个常见的问题是活性药物成分不能充分穿透皮肤。因此,在当前的研究中,我们评估了新开发的凡士林液晶(LC)软膏制剂的效用,并对其在经皮给药系统中的生物相容性和功能进行了表征。首先,我们使用对氨基苯甲酸(PABA)作为亲水模型分子制备了凡士林-LC 制剂。通过测量粘度、小角 X 射线散射(SAXS)、粒径和 z 电位来评估制剂的物理化学性质。使用透析释放技术评估药物从凡士林-LC 制剂中的释放。进行了体外测试以确定增强皮肤渗透的潜力。通过 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基-2H-四唑溴盐(MTT)测定法和单细胞凝胶电泳进一步测试了所制备制剂的生物相容性。结果表明,新型凡士林-LC 制剂具有生物相容性,并能有效地形成六面体。新的凡士林-LC 制剂显著增强了 PABA 的皮肤渗透。根据这项研究,与商业凡士林相比,凡士林-LC 制剂在改善皮肤通透性和 PABA 皮肤浓度方面更有效。

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