生物相容性脂质纳米载体改善醋酸氟西诺酮皮肤递送:理化和体外性能

Q4 Pharmacology, Toxicology and Pharmaceutics Arhiv za Farmaciju Pub Date : 2023-01-01 DOI:10.5937/arhfarm73-46312
Tijana Stanković, Tanja Ilić, Vladimir Dobričić, Anđela Tošić, Ivana Pantelić, Snežana Savić
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引用次数: 0

摘要

为了改善局部皮质类固醇进入炎性皮肤病变的递送,同时减少不良反应的可能性,脂质纳米载体受到越来越多的关注。因此,本研究旨在通过优化处方和工艺参数,开发生物相容性纳米乳(NEs)和纳米结构脂质载体(NLCs)作为氟西诺酮醋酸酯(FA)的载体。在分析了相关的理化参数和稳定性测试后,进行了体外释放和渗透测试,以评估纳米载体与常规参考产品(Sinoderm®霜)相比,是否影响FA进入/通过皮肤的渗透。所制得的NEs具有良好的物理化学性能(液滴尺寸200 nm, pdi0.2, ZP>|-30| mV, pH ~ 4.75)和长期稳定性。虽然开发的NLCs最初具有令人满意的性能,但在储存3个月后观察到凝胶化,这意味着需要进一步的配方测试来解决这些系统的有限稳定性。体外释放/渗透研究结果表明,与Sinoderm®面霜相比,开发的纳米载体(尤其是NEs)可以更好地将FA输送到皮肤中。因此,具有10%脂质相(中链甘油三酯/油酸3:1)的卵磷脂为基础的NE是一种很有前途的策略,可以改善FA对发炎皮肤的输送,使其易于应用,特别是对较大的皮肤表面和毛发区域。
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Biocompatible lipid nanocarriers for improved skin delivery of fluocinolone acetonide: Physicochemical and in vitro performances
In order to improve the delivery of topical corticosteroids into inflammatory skin lesions while reducing the likelihood of adverse effects, lipid nanocarriers have received increasing attention. Hence, this study aimed to develop biocompatible nanoemulsions (NEs) and nanostructured lipid carriers (NLCs) as carriers for fluocinolone acetonide (FA) by carefully optimizing the formulation and process parameters. After an analysis of the relevant physicochemical parameters and stability testing, in vitro release and permeation tests were performed to evaluate whether the nanocarriers affected the penetration of FA into/through the skin compared to a conventional reference product (Sinoderm® cream). The developed NEs exhibited satisfactory physicochemical properties (droplet size <200 nm, PDI<0.2, ZP>|-30| mV, pH ~ 4.75) and long-term stability. Although the developed NLCs initially had satisfactory properties, gelation was observed within 3 months of storage, implying that further formulation testing is required to resolve the limited stability of these systems. In vitro release/permeation findings suggest that the developed nanocarriers (especially NEs) provide better delivery of FA into/though the skin compared to the Sinoderm® cream. Therefore, a lecithin-based NE with a 10% lipid phase (medium-chain triglycerides/oleic acid 3:1) is a promising strategy for improved delivery of FA to the inflamed skin, allowing for ease of application, especially to larger skin surfaces and hairy regions.
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来源期刊
Arhiv za Farmaciju
Arhiv za Farmaciju Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
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发文量
19
审稿时长
12 weeks
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