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基于微乳的含柠檬草叶精油(Cymbopogon citratus (DC.) Stapf)和芒果核仁提取物(Mangifera indica Linn)的局部水凝胶用于治疗痤疮:制备和体外评价。

Microemulsion-based topical hydrogels containing lemongrass leaf essential oil (Cymbopogon citratus (DC.) Stapf) and mango seed kernel extract (Mangifera indica Linn) for acne treatment: Preparation and in-vitro evaluations.

机构信息

Faculty of Pharmacy, Can Tho University of Medicine and Pharmacy, Can Tho, Vietnam.

DHG Pharmaceutical Joint-Stock Company, Can Tho, Vietnam.

出版信息

PLoS One. 2024 Oct 31;19(10):e0312841. doi: 10.1371/journal.pone.0312841. eCollection 2024.

Abstract

Current treatments for severe acne include combinations of synthetic anti-inflammatory and antibacterial drugs, which possess numerous side effects. Therefore, this study developed microemulsion-based hydrogel containing lemongrass leaf essential oil (Cymbopogon citratus (DC.) Stapf) and mango seed kernel extract (Mangifera indica Linn) as a potential natural therapy for inflammatory acne. To this end, the microemulsions were first prepared using pseudo-ternary phase diagrams with soybean oil and coconut oil, cremophor RH40, and PEG 400. The optimal formula could load 1% lemongrass oil and 10% mango extract, possessed a spherical droplet size of ~18.98 nm, a zeta potential of -5.56 mV, and a thermodynamic stability. Secondly, the microemulsion-based hydrogel was developed by simple mixing the optimal microemulsion in carbopol-940 hydrogel (3.5% w/w). The product showed a viscosity of ~3728 cPs, a pH of 5.4-6.2, a spreadability of ~24 cm, an in-vitro Franz-cell cumulative release rate of ~80% for polyphenol content and ~60% for citral within 12 h, and a good physicochemical stability of > 3 months. Thirdly, the skin compatibility/irritability of the microemulsion-based hydrogel was determined by the HET-CAM assay, which showed non-irritation level. Finally, the anti-inflammatory activities of the hydrogel, using heat-induced BSA denaturation assay and LPS-stimulated RAW 264.7 NO inhibition assay, was 4-times higher than that of the reference drug Klenzit-C® (adapalene and clindamycin gel). Moreover, the hydrogel possessed strong anti-biofilm activity in Cutibacterium acnes, comparable with Klenzit-C®. Conclusively, the microemulsion-based hydrogel containing lemongrass oil and mango seed extract demonstrated much potentials to be a promising natural drug for acne treatment.

摘要

目前治疗重度痤疮的方法包括使用合成抗炎和抗菌药物的组合,这些药物具有许多副作用。因此,本研究开发了一种含有柠檬草叶精油(Cymbopogon citratus(DC.)Stapf)和芒果核仁提取物(Mangifera indica Linn)的基于微乳液的水凝胶,作为一种治疗炎症性痤疮的潜在天然疗法。为此,首先使用伪三元相图用大豆油和椰子油、吐温 RH40 和聚乙二醇 400 制备微乳液。最佳配方可负载 1%柠檬草油和 10%芒果提取物,具有约 18.98nm 的球形液滴尺寸、-5.56mV 的 ζ 电位和热力学稳定性。其次,通过将最佳微乳液简单混合在卡波姆 940 水凝胶(3.5%w/w)中开发基于微乳液的水凝胶。该产品表现出约 3728cPs 的粘度、5.4-6.2 的 pH 值、约 24cm 的铺展性、在 12 小时内多酚含量的80%和柠檬醛的60%的体外 Franz 细胞累积释放率,以及超过 3 个月的良好物理化学稳定性。第三,通过 HET-CAM 测定法测定基于微乳液的水凝胶的皮肤相容性/刺激性,结果显示为非刺激性水平。最后,使用热诱导 BSA 变性测定法和 LPS 刺激 RAW 264.7NO 抑制测定法评估水凝胶的抗炎活性,其活性是参考药物 Klenzit-C®(阿达帕林和克林霉素凝胶)的 4 倍。此外,水凝胶在痤疮丙酸杆菌中具有很强的抗生物膜活性,与 Klenzit-C®相当。综上所述,含有柠檬草油和芒果核仁提取物的基于微乳液的水凝胶具有很大的潜力成为治疗痤疮的有前途的天然药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a464/11527213/02db53a094d4/pone.0312841.g001.jpg

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