Ansari Sartaj Akhtar, Qadir Abdul, Warsi Musarrat Husain, Mujeeb Mohd, Aqil Mohd, Mir Showkat Rasool, Sharma Sanchit
Department of Pharmacognosy and Phytochemistry, Phytomedicine Laboratory, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, 110062 India.
Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, 110062 India.
3 Biotech. 2021 Nov;11(11):456. doi: 10.1007/s13205-021-02978-3. Epub 2021 Oct 7.
The aim of the present study was to develop and characterize karanjin-loaded ethosomes-based gel formulation for enhanced topical delivery and effective therapy of skin acne. Karanjin-loaded ethosomes (K-ETH) presented a nanometric size of 140.87 ± 2.35 nm, entrapment of 71.41 ± 2.74% and enhanced permeation with 1.9 times increase in the flux and 2.4 times higher skin deposition compared to the hydro-ethanolic solution of karanjin. The DSC analysis confirmed successful entrapment of the karanjin within the ethosomes. The developed ethosomes were incorporated in the carbopol gel for adequate application on the skin surface. The ethosomal gel (K-EGF) also exhibited greater penetration in the rat skin as revealed by CLSM. The optimized K-EGF formulation was non-irritant to the skin as evident by Draize score test and histopathological examination. The highest zone of inhibition, 30.0 ± 1.52 mm and 36.22 ± 0.57 mm was produced by the K-EGF against and , respectively, indicating substantial antibacterial properties of the K-EGF. DPPH assay indicated its potent antioxidant effects. Substantial anti-inflammatory effects in the carrageenan-induced edema in the rat paw were evident with inhibition of rat paw edema by 66.66% and 70.37% upon application of K-EGF and standard anti-inflammatory agent, respectively. Anti-acne effects were also evident with K-EGF treatment with significant decrease in number and size of sebaceous gland units in dermis. Overall, the above findings vouch for a therapeutic opportunity to improve topical delivery of karanjin in acne treatment employing ethosomal gels as the promising carrier system.
The online version contains supplementary material available at 10.1007/s13205-021-02978-3.
本研究的目的是开发并表征基于载有羽扇豆醇的乙醇脂质体的凝胶制剂,以增强局部递送并有效治疗皮肤痤疮。载有羽扇豆醇的乙醇脂质体(K-ETH)呈现出纳米尺寸,为140.87±2.35 nm,包封率为71.41±2.74%,与羽扇豆醇的水乙醇溶液相比,通量增加了1.9倍,皮肤沉积量高2.4倍,渗透增强。DSC分析证实羽扇豆醇成功包封在乙醇脂质体内。将所制备的乙醇脂质体加入卡波姆凝胶中,以便在皮肤表面充分应用。如CLSM所示,乙醇脂质体凝胶(K-EGF)在大鼠皮肤中也表现出更大的渗透。经Draize评分试验和组织病理学检查证明,优化后的K-EGF制剂对皮肤无刺激性。K-EGF对痤疮丙酸杆菌和金黄色葡萄球菌产生的抑菌圈最大,分别为30.0±1.52 mm和36.22±0.57 mm,表明K-EGF具有显著的抗菌性能。DPPH试验表明其具有强大的抗氧化作用。在角叉菜胶诱导的大鼠足爪水肿中,K-EGF和标准抗炎剂分别使大鼠足爪水肿抑制率达66.66%和70.37%,具有明显的抗炎作用。K-EGF治疗的抗痤疮作用也很明显,真皮中皮脂腺单位的数量和大小显著减少。总体而言,上述研究结果证明了利用乙醇脂质体凝胶作为有前景的载体系统,在痤疮治疗中改善羽扇豆醇局部递送的治疗机会。
在线版本包含可在10.1007/s13205-021-02978-3获取的补充材料。