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载环丙沙星的纳米结构脂质载体的制备、表征及抗菌性能及其在抗感染治疗中的应用

Preparation, characterisation and antibacterial property of ciprofloxacin-loaded nanostructured lipid carrier for treatment of infection.

机构信息

a Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Drug Delivery and Nanomedicines Research Group , University of Nigeria , Nsukka , Nigeria.

d Department of Drug Delivery , Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Saarland University , Saarbrücken , Germany.

出版信息

J Microencapsul. 2019 Jan;36(1):32-42. doi: 10.1080/02652048.2019.1582724. Epub 2019 Mar 4.

Abstract

In this study, controlled ciprofloxacin (CIPRO) nanostrustructured lipid carriers of Precirol ATO 5/Transcutol HP (batch A) and tallow fat/Transcutol HP (batch B) was carreid out. Objective: The aim was to improve solubility and bioavailability of CIPRO. Study of controlled ciprofloxacin (CIPRO) nanostructured lipid carriers of Precirol ATO 5/Transcutol HP (batch A) and tallow fat/Transcutol HP (batch B). CIPRO concentrations C (0.0, 0.2, 0.5, 0.8, and 1.0% w/w) as AC and BC were prepared by hot homogenisation and characterised by zetasizer, differential scanning calorimetry, Fourier transform infra-red spectroscopy, drug release and growth inhibitory zone diameter (IZD) on agar-seeded . AC achieved polydispersed particles of ∼605 nm, 92% encapsulation efficiency (EE) and -28 mV similar to BC (∼789 nm, 91% EE, and -31 mV). Crystallinity indices (AC and BC) were low at 3 and 5%, respectively. CIPRO release in AC was ∼98% in SGF (pH 1.2) and BC similarly ∼98% in SIF (pH 6.8). AC had superior growth inhibition of at lower concentration (1.2 µg/mL) than BC and CIPRO controls; hence could serve as possible sustained delivery system of CIPRO.

摘要

本研究制备了载有环丙沙星(CIPRO)的纳米结构脂质载体,载体由 Precirol ATO 5/Transcutol HP(A 批)和牛脂/Transcutol HP(B 批)组成。目的:旨在提高 CIPRO 的溶解度和生物利用度。

研究载有环丙沙星(CIPRO)的纳米结构脂质载体,载体由 Precirol ATO 5/Transcutol HP(A 批)和牛脂/Transcutol HP(B 批)组成。

CIPRO 浓度 C(0.0、0.2、0.5、0.8 和 1.0%w/w)分别作为 AC 和 BC 通过热匀浆法制备,并通过激光粒度仪、差示扫描量热法、傅里叶变换红外光谱、药物释放和琼脂接种的抑菌圈直径(IZD)进行了表征。AC 获得了约 605nm 的多分散性颗粒,92%的包封效率(EE)和-28mV,与 BC(约 789nm,91%EE 和-31mV)相似。结晶度指数(AC 和 BC)分别为 3%和 5%,均较低。AC 在 SGF(pH 1.2)中的 CIPRO 释放约为 98%,BC 则在 SIF(pH 6.8)中同样约为 98%。AC 在较低浓度(1.2μg/mL)下对的生长抑制作用优于 BC 和 CIPRO 对照,因此可能作为 CIPRO 的可持续输送系统。

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