Department of Pharmaceutical Technology, Medical University of Białystok, Mickiewicza 2c, 15-222 Białystok, Poland.
Molecules. 2022 Dec 28;28(1):235. doi: 10.3390/molecules28010235.
Topical administration of drug is an attractive alternative to the oral administration as it provides a reduction in adverse reactions and an enhancement of therapeutic effects. The use of lipid carriers in hydrogel structures makes it possible to introduce lipophilic substances in a dissolved form. In this study, an NSAID from the BCS class II, etodolac (ETD), was used. The nanostructured lipid carriers (NLC) obtained with ETD were incorporated into semi-solid forms (gels). Hydrogels with the suspended drug and oleogel were also prepared for comparison purposes. The obtained gels were tested in terms of pH, viscosity, rheological, mechanical, and bioadhesive properties. The release and permeation through membranes were also studied. All tested formulations were characterized by a pH below 7, which ensured the physiological state of the skin. The viscosities of all gels decreased with increasing shear rate, indicating non-Newtonian behavior. The fastest ETD release was observed for NLC with a Carbopol base (formulation F1); a similar result was noticed in the permeation test. The developed gel formulations containing ETD-NLC dispersion and Carbopol or Poloxamer as gelling agents were stable and possessed beneficial pharmaceutical properties.
局部给药是替代口服给药的一种有吸引力的方法,因为它可以减少不良反应并增强治疗效果。在水凝胶结构中使用脂质载体可以使亲脂性物质以溶解形式被引入。在本研究中,使用了 BCS 分类 II 中的一种 NSAID,即依托度酸(ETD)。用 ETD 获得的纳米结构化脂质载体(NLC)被掺入半固体形式(凝胶)中。为了比较,还制备了含有悬浮药物的水凝胶和油凝胶。根据 pH 值、粘度、流变学、机械和生物黏附特性对获得的凝胶进行了测试。还研究了释放和通过膜的渗透。所有测试的制剂的 pH 值均低于 7,这确保了皮肤的生理状态。所有凝胶的粘度均随剪切率的增加而降低,表明呈非牛顿行为。在含有 Carbopol 基质的 NLC(配方 F1)中观察到 ETD 释放最快;在渗透测试中也注意到了类似的结果。包含 ETD-NLC 分散体和 Carbopol 或 Poloxamer 作为胶凝剂的开发的凝胶制剂是稳定的,并具有有益的药物特性。