Tackling acne vulgaris by fabrication of tazarotene-loaded essential oil-based microemulsion: In vitro and in vivo evaluation

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Noha M. Badawi , Rania M. Yehia , Caroline Lamie , Khaled A. Abdelrahman , Dalia A. Attia , Doaa A. Helal
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Abstract

This study aimed to formulate and optimize an anti-acne drug namely tazarotene (TZR) in essential oil-based microemulsion (ME) using either Jasmine oil (Jas) or Jojoba oil (Joj). TZR-MEs were prepared using two experimental designs (Simplex Lattice Design®) and characterized for droplet size, polydispersity index, and viscosity. Further in vitro, ex vivo, and in vivo investigations were performed for the selected formulations. Results revealed that TZR-selected MEs exhibited suitable droplet size, homogenous dispersions, and acceptable viscosity, in addition to spherical-shaped particles in morphology. The ex vivo skin deposition study showed a significant TZR accumulation in all skin layers for the Jas-selected ME over the Joj one. Further, TZR didn't show any antimicrobial activity against P. acnes, however, it was boosted when it was incorporated into the selected MEs. The in vivo study results of the infected mice ears induced by P. acnes revealed that our selected MEs successfully reached a high level of ear thickness reduction of 67.1% and 47.4% for Jas and Joj selected MEs, respectively, versus only 4% for the market product. Finally, the findings confirmed the ability to use essential oil-based ME, particularly with Jas, as a promising carrier for topical TZR delivery in the treatment of acne vulgaris.

Abstract Image

他扎罗汀负载精油微乳剂治疗寻常痤疮的体内外评价
本研究旨在使用茉莉油(Jas)或荷荷巴油(Joj)在精油基微乳(ME)中配制和优化抗痤疮药物,即他扎罗汀(TZR)。使用两种实验设计(Simplex Lattice Design®)制备TZR ME,并对液滴尺寸、多分散指数和粘度进行表征。对所选制剂进行了进一步的体外、离体和体内研究。结果表明,TZR选择的ME除了在形态上呈球形颗粒外,还表现出合适的液滴尺寸、均匀的分散体和可接受的粘度。离体皮肤沉积研究显示,Jas选择的ME比Joj选择的ME在所有皮肤层中都有显著的TZR积累。此外,TZR对痤疮假单胞菌没有表现出任何抗菌活性,然而,当它被掺入选定的ME中时,它得到了增强。由P.acnes诱导的受感染小鼠耳朵的体内研究结果显示,我们选择的ME成功地达到了高水平,Jas和Joj选择的ME的耳朵厚度分别减少了67.1%和47.4%,而市场产品仅减少了4%。最后,研究结果证实了使用精油基ME的能力,特别是与Jas一起使用,作为治疗寻常痤疮的局部TZR递送的有前途的载体。
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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
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