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壳聚糖定制的夫西地酸脂质纳米结构作为治疗伤口感染的有前途的载体:一项探索性研究。

Chitosan-tailored lipidic nanoconstructs of Fusidic acid as promising vehicle for wound infections: An explorative study.

机构信息

University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh 160 014, India.

University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh 160 014, India; UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles & Nanocomposites (Biomedical Sciences), Panjab University, Chandigarh 160 014, India.

出版信息

Int J Biol Macromol. 2018 Aug;115:1012-1025. doi: 10.1016/j.ijbiomac.2018.04.092. Epub 2018 Apr 19.

Abstract

The current research study intends to explore the combined potential of lipid nanoparticles and chitosan as an optimum therapy for the management of wound infections. Fusidic acid (FA), a steroidal antibiotic employed for treatment of primary and secondary topical infections was encapsulated within the nanoengineered lipid-polymer hybrid nanoparticles (FA-LPHNs). A number of variables like lipid/polymer ratio, lipid, surfactant and chitosan concentration, stirring speed were optimized to get the desired particle size and % entrapment efficiency. The developed carriers were further characterized for particle size, antibacterial activity, cytotoxicity studies in HaCat cell lines, ex vivo permeation studies and skin safety profile. The developed LPHNs offered nanometric size (284.67 ± 5.67 nm), sustained drug release (79.31 ± 0.45%) and enhanced drug permeation (72.09 ± 1.26%). The changes in viability of HaCat cells were insignificant indicating the safety profile of LPHNs. The administration of FA-LPHNs resulted in 5-times and 4-times decrease in its inhibitory concentration against MRSA 33591 and MSSA 25921 respectively, along with antibacterial activity for a longer duration. Further, hydrogel incorporated nanoparticles were found to be topically applicable and compatible with mice skin. The studies indicated the superiority of FA-LPHNs for better management of wounds and associated infections over the conventional marketed product.

摘要

本研究旨在探索脂质纳米粒和壳聚糖联合应用于治疗伤口感染的潜力。将被福沙那韦(FA),一种用于治疗原发性和继发性局部感染的甾体抗生素包封于纳米工程化的脂质-聚合物杂化纳米粒(FA-LPHN)中。优化了多种变量,如脂质/聚合物比、脂质、表面活性剂和壳聚糖浓度、搅拌速度,以获得所需的粒径和包封效率。进一步对所开发的载体进行了粒径、抗菌活性、HaCat 细胞系的细胞毒性研究、体外渗透研究和皮肤安全性评价。所开发的 LPHN 具有纳米级粒径(284.67±5.67nm)、持续的药物释放(79.31±0.45%)和增强的药物渗透(72.09±1.26%)。HaCat 细胞活力的变化不显著,表明 LPHN 具有安全性。与传统市售产品相比,FA-LPHN 给药后,对 MRSA 33591 和 MSSA 25921 的抑制浓度分别降低了 5 倍和 4 倍,同时具有更长时间的抗菌活性。此外,发现水凝胶结合的纳米粒具有局部应用和与小鼠皮肤相容的特性。这些研究表明,FA-LPHN 可更好地管理伤口及其相关感染。

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