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载有环丙沙星的脂质体的抗微生物作用及其在兔眼内的眼部递药。

Anti-microbial Effect and in Vivo Ocular Delivery of Ciprofloxacin-loaded Liposome through Rabbit's Eye.

机构信息

Infectious Ophthalmologic Research Center, Ahvaz Jundishapur University of Medical Sciences , Ahvaz, Iran.

Department of Ophthalmology, Imam Khomeini Hospital, Ahvaz Jundishapur University of Medical Sciences , Ahvaz, Iran.

出版信息

Curr Eye Res. 2020 Oct;45(10):1245-1251. doi: 10.1080/02713683.2020.1728777. Epub 2020 Feb 18.

Abstract

: The main purpose of this study was to increase the concentration and bioavailability of Ciprofloxacin (CPX) in the rabbit eye by liposomal formulation. : CPX- loaded liposomes with and without Carbomer 934 (carbomer) were prepared by a thin-layer hydration method. Liposomal formulations after evaluation for characters such as particle size and entrapment efficiency were used in in-vivo experimental for installation into the rabbit's eyes. This experimental study consisted of 10 rabbits divided into two groups. Group 1 (liposomes without coating) and group 2 (carbomer coated liposomes) received one drop per h of liposomes consists of 0.3% CPX in the right eye and commercial CPX eye drop in the left eye until 6 h. Aqueous humor and vitreous samples were collected from all rabbits at the baseline, 1, 3 and 6 h and the drug concentration determined by high pressure liquid chromatography (HPLC). On the other hand, minimum inhibitor concentration (MIC) and minimum bactericidal concentration (MBC) of CPX-loaded in liposomes were determined. : liposomal formulations increased ocular bioavailability of CPX around four-folds compared with a commercial CPX eye drop. The increase in the ocular bioavailability may be effective and help to treat bacterial endophthalmitis as well as can be used in prophylaxis of post-operative endophthalmitis. : The concentrations of CPX on the aqueous humor and vitreous after liposomes application were more than MIC of CPX against pseudomonas auroginosa and staphylococcus aurous but for commercial eye drop was less than MIC. Therefore liposomes modified the pharmacokinetics of CPX and improved pharmacodynamics property.

摘要

本研究的主要目的是通过脂质体制剂提高环丙沙星(CPX)在兔眼内的浓度和生物利用度。采用薄膜水化法制备载有 CPX 的脂质体和载有卡波姆 934(carbomer)的 CPX 载脂质体。对脂质体进行粒径和包封效率等特性评价后,将其用于体内实验,安装到兔子的眼睛中。这项实验研究包括 10 只兔子,分为两组。第 1 组(无涂层脂质体)和第 2 组(涂有 carbomer 的脂质体)每小时在右眼滴一滴含有 0.3% CPX 的脂质体和左眼滴一滴市售 CPX 眼药水,持续 6 小时。在基线、1、3 和 6 小时时从所有兔子中采集房水和玻璃体样本,并通过高效液相色谱法(HPLC)测定药物浓度。另一方面,测定了载 CPX 的脂质体的最低抑菌浓度(MIC)和最低杀菌浓度(MBC)。与市售 CPX 眼药水相比,脂质体制剂使 CPX 的眼部生物利用度增加了约四倍。眼部生物利用度的增加可能有效,有助于治疗细菌性眼内炎,也可用于预防术后眼内炎。脂质体给药后房水和玻璃体内 CPX 的浓度均高于 CPX 对铜绿假单胞菌和金黄色葡萄球菌的 MIC,但市售眼药水的 CPX 浓度则低于 MIC。因此,脂质体改变了 CPX 的药代动力学,提高了药效学特性。

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