Dave Vivek, Bhardwaj Nishant, Gupta Nikita, Tak Kajal
Department of Pharmacy, Banasthali Vidyapith, Banasthali, Rajasthan 304022 India.
3 Biotech. 2020 Mar;10(3):97. doi: 10.1007/s13205-020-2083-z. Epub 2020 Feb 6.
This study includes development, characterization, and optimization of herbal ethosomal formulation. The aim of the present study is to develop drug loaded ethosomes capped with (neem) which, was further incorporated in Carbopol 934 K thereby, resulting in the formation of ethosomal gel. The formulation is aimed to express effective treatment against fungal infection. The build was formulated using drug (Luliconazole), soyalecithin, ethanolic neem extract and propylene glycol. In total nine ethosomal, formulations of distinct concentrations of ingredients were processed, to determine out the optimized formulation among the all. Further the prepared drug loaded ethosomes were subjected to various evaluation parameters like particle size, zeta potential, polydispersity index (PDI) and % entrapment efficiency. For the evaluation of its surface morphology, transmission electron microscopy was executed whereas, atomic force microscopy was carried out which contributes in detail and depth information of surface morphology. For the analysis of thermal behavior Thermal gravimetric analysis graph was obtained for luliconazole, soyalecithin, neem extract, physical mixture and optimized formulation (LF5). Attenuated total internal reflection Fourier transforms infra-red spectroscopy was performed for luliconazole, soyalecithin, neem extract, physical mixture, and optimized formulation (LF5) to examine the interaction between the drug and the excipients. Viscosity, pH, spreadability and extrudability of the ethosomal gel were calculated to determine the suitability of the formulation for topical application. In vitro drug permeation study and antifungal activity was executed out with the aid of Wistar albino rat skin model and tube dilution assay respectively. The complete study wrap up, that this herbal ethosomal approach provides advanced sustained and targeted delivery of luliconazole. On analyzing the results, ethosomal formulation LF5 was found to be optimized one, due to its optimum concentration of soyalecithin (300 mg) and ethanol (35%). Hence it has maximum entrapment efficiency of 86.56 ± 0.74%. Optimum vesicle size, zeta potential, and PDI were found to be 155.30 ± 1.2 nm, - 42.20 ± 0.3 mV, and 0.186 ± 0.07 respectively. In vitro drug permeation study expresses release of 83.45 ± 2.51 in 24 h whereas; the in vivo activity proved that LF5 is more active and effective against in comparison to . In the end, it was estimated that ethosomal suspension and lyophilized ethosomal suspension was utmost stable at 4 °C/60 ± 5 RH. The complete study clearly indicates that the buildup of ethosomal formulation with luliconazole and neem extract show synergistic effect thereby, expressing excellent result against the treatment of fungal infection.
本研究包括草药脂质体剂型的开发、表征和优化。本研究的目的是开发载药脂质体,其表面用印楝覆盖,然后进一步加入卡波姆934K,从而形成脂质体凝胶。该制剂旨在对真菌感染表现出有效的治疗作用。该制剂使用药物(卢立康唑)、大豆卵磷脂、乙醇印楝提取物和丙二醇配制而成。总共制备了九种不同成分浓度的脂质体制剂,以确定其中的优化制剂。此外,将制备的载药脂质体进行各种评价参数的测定,如粒径、zeta电位、多分散指数(PDI)和包封率。为了评价其表面形态,进行了透射电子显微镜检查,同时进行了原子力显微镜检查,以提供表面形态的详细和深度信息。为了分析热行为,获得了卢立康唑、大豆卵磷脂、印楝提取物、物理混合物和优化制剂(LF5)的热重分析图。对卢立康唑、大豆卵磷脂、印楝提取物、物理混合物和优化制剂(LF5)进行衰减全内反射傅里叶变换红外光谱分析,以研究药物与辅料之间的相互作用。计算脂质体凝胶的粘度、pH值、铺展性和挤出性,以确定该制剂用于局部应用的适用性。分别借助Wistar白化大鼠皮肤模型和试管稀释法进行体外药物渗透研究和抗真菌活性研究。整个研究总结表明,这种草药脂质体方法提供了卢立康唑的先进的持续和靶向递送。分析结果发现,脂质体制剂LF5是优化制剂,因为其大豆卵磷脂(300mg)和乙醇(35%)的浓度最佳。因此,它具有86.56±0.74%的最大包封率。最佳囊泡大小、zeta电位和PDI分别为155.30±1.2nm、-42.20±0.3mV和0.186±0.07。体外药物渗透研究表明,24小时内药物释放率为83.45±2.51;体内活性证明,与……相比,LF5对……更具活性和有效性。最后,据估计,脂质体悬浮液和冻干脂质体悬浮液在4°C/60±5%相对湿度下最稳定。整个研究清楚地表明,含卢立康唑和印楝提取物的脂质体制剂的组合显示出协同作用,从而在真菌感染治疗中表现出优异的效果。