Suppr超能文献

用于银屑病局部治疗的脂质基新型给药系统的开发表征及皮肤渗透潜力

Development characterization and skin permeating potential of lipid based novel delivery system for topical treatment of psoriasis.

作者信息

Pradhan Madhulika, Singh Deependra, Singh Manju Rawat

机构信息

University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur, Chhattisgarh, 492010, India.

University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur, Chhattisgarh, 492010, India.

出版信息

Chem Phys Lipids. 2015 Feb;186:9-16. doi: 10.1016/j.chemphyslip.2014.11.004. Epub 2014 Nov 20.

Abstract

The aim of this study was to develop, optimize and evaluate the potential of solid lipid nanoparticles (SLNs) as a topical delivery system for targeted and prolonged release of Fluocinolone acetonide (FA). FA loaded SLNs were successfully developed by an emulsification-ultrasonication method and optimized using 17-run, 3-factor, 3-level Box-Behnken design of Design Expert software. SLNs were evaluated for particle size, polydispersity index, zeta potential, drug encapsulation efficiency and drug loading. Shape and surface morphology of the SLNs confirmed spherical shape of nanoparticles when investigated under a transmission electron microscope. Complete encapsulation of drug in the nanoparticles was confirmed by powder X-ray diffraction and differential scanning calorimetry. The drug release study confirmed prolonged release from the SLNs following Higuchi release kinetics with R(2) value of 0.995 where as pure drug suspension exhibited faster drug release following zero order release kinetics with R(2) value of 0.992. Stability study confirmed that SLNs were stable for 3 months at 4 °C. Furthermore, in vitro skin distribution studies showed presence of significant amount of FA on the epidermal layer of skin when treated with FA loaded SLNs suspension while plain FA suspension showed minimum amount of FA in the epidermis and dermis. Moreover, selective accumulation of FA in the epidermis might eliminate adverse side effects associated with systemic exposure. Results demonstrated that FA loaded SLNs could be a promising modality for psoriasis treatment but to establish clinical utility of the present system further studies are required in clinically relevant models.

摘要

本研究的目的是开发、优化并评估固体脂质纳米粒(SLNs)作为醋酸氟轻松(FA)靶向和长效释放的局部给药系统的潜力。通过乳化超声法成功制备了负载FA的SLNs,并使用Design Expert软件的17次运行、三因素、三水平Box-Behnken设计进行优化。对SLNs的粒径、多分散指数、zeta电位、药物包封率和载药量进行了评估。在透射电子显微镜下观察时,SLNs的形状和表面形态证实了纳米粒呈球形。粉末X射线衍射和差示扫描量热法证实药物完全包裹在纳米粒中。药物释放研究证实,SLNs符合Higuchi释放动力学,呈现长效释放,R(2)值为0.995,而纯药物混悬液符合零级释放动力学,药物释放较快,R(2)值为0.992。稳定性研究证实,SLNs在4℃下可稳定3个月。此外,体外皮肤分布研究表明,用负载FA的SLNs混悬液处理皮肤时,表皮层存在大量FA,而普通FA混悬液在表皮和真皮中的FA含量最低。此外,FA在表皮中的选择性蓄积可能消除与全身暴露相关的不良副作用。结果表明,负载FA的SLNs可能是治疗银屑病的一种有前景的方式,但要确定本系统的临床实用性,还需要在临床相关模型中进行进一步研究。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验