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载诺氟沙星纳米立方脂质体增强外耳道炎管理的研究:体外与体内评价。

Norfloxacin loaded nano-cubosomes for enhanced management of otitis externa: In vitro and in vivo evaluation.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; Department of Pharmaceutics, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Giza, Egypt.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; School of Life and Medical Sciences, University of Hertfordshire Hosted by Global Academic Foundation, Cairo, Egypt.

出版信息

Int J Pharm. 2021 May 1;600:120490. doi: 10.1016/j.ijpharm.2021.120490. Epub 2021 Mar 17.

DOI:10.1016/j.ijpharm.2021.120490
PMID:33744451
Abstract

The research's goal is to design and formulate nano-structured cubosomes loaded with norfloxacin (NFX)formanagement of otitis externa. In this study, glyceryl monooleate (GMO) as lipid phase, Cremophor EL as surfactant and either Pluronic F108 or Pluronic F127 as stabilizer were the used ingredients. The nano-cubosomal formulation "CUB 1" (its dispersed phase is composed of GMO (95%), Cremophor EL (2.5%) and Pluronic F108 (2.5%)) was the best achieved one. It had small particles size (216.75 ± 2.47 nm), good polydispersity index (0.339 ± 0.012) and acceptable zeta potential (-41.2 ± 2.262 mV). Images obtained after transmission electron microscopy examination ensured nearly cubic shape of formed nanoparticles with excellent dispersibility. Moreover, micrographs of rabbit ear skin specimens examined by confocal laser microscopy ensured good permeation capability of nano-structured cubosomes.In addition, in vivoskin deposition results revealed that higher amount of NFX was deposited in the rabbit ear skin throughout the study period (10 h) compared to drug suspension. Additionally, histopathological results proved that NFX loaded cubosomes can be safely applied topically on ear skin without any signs of inflammation nor skin irritation. Accordingly, these results anticipated the nano-structured cubosomal capabilities as a favorable nano-carrier for dermal NFX delivery to external ear skin for enhancing the management of otitis externa.

摘要

本研究旨在设计和制备载诺氟沙星(NFX)的纳米立方载体,用于治疗外耳炎。在这项研究中,使用了甘油单油酸酯(GMO)作为脂质相、吐温 EL 作为表面活性剂以及泊洛沙姆 F108 或 F127 作为稳定剂。纳米立方体制剂“CUB1”(其分散相由 GMO(95%)、吐温 EL(2.5%)和泊洛沙姆 F108(2.5%)组成)是最佳制剂。它具有较小的颗粒尺寸(216.75 ± 2.47nm)、良好的多分散指数(0.339 ± 0.012)和可接受的 zeta 电位(-41.2 ± 2.262mV)。透射电子显微镜检查获得的图像确保了形成的纳米粒子具有近乎立方的形状和良好的分散性。此外,共聚焦激光显微镜检查的兔耳皮肤标本的显微照片确保了纳米结构立方载体的良好渗透能力。此外,体内皮肤沉积结果表明,与药物混悬剂相比,NFX 在整个研究期间(10h)在兔耳皮肤中的沉积量更高。此外,组织病理学结果证明,载诺氟沙星的立方载体可安全地局部应用于耳部皮肤,没有任何炎症或皮肤刺激的迹象。因此,这些结果表明纳米立方载体具有作为外耳皮肤中 NFX 经皮传递的有利纳米载体的潜力,可增强对外耳炎的治疗效果。

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