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负载 var. 生物活性提取物的纳米乳液凝胶的研制与评价:一种增强皮肤渗透性和抗真菌活性的新方法。

Development and evaluation of nanoemulsion gel loaded with bioactive extract of var. : A novel approach for enhanced skin permeability and antifungal activity.

作者信息

Akhter Ambreen, Shirazi Jafir Hussain, Shoaib Khan Haji Muhammad, Hussain Muhammad Delwar, Kazi Mohsin

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, 63100, Punjab, Pakistan.

Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland Eastern Shore, Princess Anne, MD, 21853, USA.

出版信息

Heliyon. 2024 Jul 24;10(15):e35069. doi: 10.1016/j.heliyon.2024.e35069. eCollection 2024 Aug 15.

Abstract

The utilization of phytoconstituents in skin care products has emerged as a notable trend due to their recognized safety and therapeutic efficacy. However, the challenge lies in improving the effective delivery of phytoconstituents to specific tissues, primarily attributed to their poor solubility and low permeability. This study endeavors to address this challenge by developing, optimizing and characterizing var. (CME) extract loaded nanoemulsion gel (CME-NEG), aiming to enhance the skin permeability and antifungal activity. Herein, nanoemulsions encapsulating the plant extract were prepared using ultrasonication technique and were characterized for droplet size, zeta potential, polydispersity index (PDI) and entrapment efficiency. Further, Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM) analysis were conducted to characterize the optimized CME extract loaded nanoemulsion (CME-NE 3) formulation. The optimized formulation was blended with Carbopol 940 gel to develop CME-NEG, which was evaluated for release kinetics, permeation and antifungal activity. High performance liquid chromatography (HPLC) analysis confirmed the presence of gallic acid, chlorogenic acid, 4-Hydroxy benzoic acid (HB acid), kaempferol, caffeic acid and quercetin. Findings of 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay showed that the ethanolic extract had highest antioxidant activity (88.88 %). The optimized formulation displayed smooth spherical nanodroplets with size of 175.5 ± 1.56 nm, zeta potential of -21.5 ± 0.12 mV, PDI of 0.192 ± 0.06, and highest entrapment efficiency (EE) of 91.35 ± 1.65 %. The release profile of CME-NE exhibited a controlled release characteristic and the release kinetic mechanism was best described by the Korsmeyer-Peppas (Kp) model. In a 24 h permeation study, it was observed that the permeation of CME-NEG was 58.63 %, significantly higher than that of CME extract loaded plain gel (CME-PG) with an enhancement ratio of 2.12. The prepared CME-NEG formulation also presented enhanced antifungal activity as compared to pure CME extract. In conclusion, the designed CME-NEG offers a promising topical drug delivery system with enhanced skin permeability and antifungal activity.

摘要

由于植物成分公认的安全性和治疗功效,其在护肤品中的应用已成为一个显著趋势。然而,挑战在于提高植物成分向特定组织的有效递送,这主要归因于它们的低溶解度和低渗透性。本研究致力于通过开发、优化和表征 var.(CME)提取物负载的纳米乳凝胶(CME-NEG)来应对这一挑战,旨在提高皮肤渗透性和抗真菌活性。在此,使用超声技术制备了包裹植物提取物的纳米乳,并对其粒径、zeta电位、多分散指数(PDI)和包封率进行了表征。此外,进行了傅里叶变换红外光谱(FTIR)和扫描电子显微镜(SEM)分析,以表征优化后的负载CME提取物的纳米乳(CME-NE 3)配方。将优化后的配方与卡波姆940凝胶混合以制备CME-NEG,并对其释放动力学、渗透和抗真菌活性进行了评估。高效液相色谱(HPLC)分析证实了没食子酸、绿原酸、4-羟基苯甲酸(HB酸)、山奈酚、咖啡酸和槲皮素的存在。2,2-二苯基-1-苦基肼(DPPH)测定结果表明,乙醇提取物具有最高的抗氧化活性(88.88%)。优化后的配方呈现出光滑的球形纳米液滴,粒径为175.5±1.56 nm,zeta电位为-21.5±0.12 mV,PDI为0.192±0.06,最高包封率(EE)为91.35±1.65%。CME-NE的释放曲线呈现出控释特性,释放动力学机制最好用Korsmeyer-Peppas(Kp)模型描述。在24小时的渗透研究中,观察到CME-NEG的渗透率为58.63%,显著高于负载CME提取物的普通凝胶(CME-PG),增强比为2.12。与纯CME提取物相比,制备的CME-NEG配方还具有增强的抗真菌活性。总之,设计的CME-NEG提供了一种有前景的局部给药系统,具有增强的皮肤渗透性和抗真菌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2f0c/11336325/1124fe18c065/ga1.jpg

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