Barot Tejas, Rawtani Deepak, Kulkarni Pratik
National Forensic Sciences University, Nr. DFS Head Quarters, Sector 9, Gandhinagar, Gujarat 382007, India.
Heliyon. 2021 Sep 11;7(9):e07968. doi: 10.1016/j.heliyon.2021.e07968. eCollection 2021 Sep.
The aim of the study was to formulate and characterize the farnesol loaded niosomes comprising gel formulation and perform their in vitro-in vivo evaluation for applications in the treatment of oral candidiasis infections.
Various gelling systems were evaluated for their rheological and stability properties. The formulation was statistically optimized using experimental design method (Box-Behnken). Transmission electron microscopy (TEM) and Atomic force microscopy (AFM) were used to observe the niosomal surface morphology. Centrifugation method and dialysis method were used to find out the % entrapment efficiency (%EE) and in-vitro release of Farnesol, respectively. In-vitro antifungal effect and cell biocompatibility of the Farnesol loaded niosomal gel was also performed using () as the model organism and epithelial cell line (SW480) by MTT cytotoxicity assay. In-vivo skin irritation test was performed on rabbit skin.
Farnesol loaded niosomes were integrated into polymeric gel solution. The optimized formulation demonstrated acceptable % EE (>80%) and an optimum particle size (168.8 nm) along with a sustained release and a long-term storage stability for up to a period of 6 months. TEM and AFM observations displayed a spherical niosome morphology. Farnesol niosomal gel showed a higher antifungal efficacy, ex-vivo skin permeation and deposition in comparison to plain farnesol solution. The niosomal gel also showed negligible cytotoxicity to normal cells citing biocompatibility and was found to be non-toxic and non-irritant to rabbit skin.
This novel niosome loaded gel-based formulation could make the oral candidiasis healing process more efficient while improving patient compliance. With the optimized methodology used in this work, such formulation approaches can become an efficient, industrially scalable, and cost-effective alternatives to the existing conventional formulations.
本研究旨在制备并表征含法尼醇的脂质体凝胶制剂,并对其治疗口腔念珠菌感染的体内外效果进行评估。
对多种凝胶体系的流变学和稳定性进行评估。采用实验设计方法(Box-Behnken)对制剂进行统计学优化。利用透射电子显微镜(TEM)和原子力显微镜(AFM)观察脂质体的表面形态。分别采用离心法和透析法测定法尼醇的包封率(%EE)和体外释放情况。以()为模式生物,采用MTT细胞毒性试验,对含法尼醇的脂质体凝胶进行体外抗真菌效果和细胞生物相容性研究。对兔皮肤进行体内皮肤刺激性试验。
含法尼醇的脂质体被整合到聚合物凝胶溶液中。优化后的制剂显示出可接受的包封率(>80%)和最佳粒径(168.8 nm),同时具有缓释和长达6个月的长期储存稳定性。TEM和AFM观察显示脂质体呈球形形态。与普通法尼醇溶液相比,法尼醇脂质体凝胶显示出更高的抗真菌效果、体外皮肤渗透和沉积。脂质体凝胶对正常细胞的细胞毒性可忽略不计,具有生物相容性,且对兔皮肤无毒无刺激。
这种新型的基于脂质体的凝胶制剂可提高口腔念珠菌的愈合效率,同时提高患者的依从性。通过本研究中使用的优化方法,此类制剂方法可成为现有传统制剂的高效、工业可扩展且经济高效的替代方案。