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一种小疏水药物(桂利嗪)对通过薄膜水化法和微流控法制备的脂质体物理化学特性的短期影响

Brief Effect of a Small Hydrophobic Drug (Cinnarizine) on the Physicochemical Characterisation of Niosomes Produced by Thin-Film Hydration and Microfluidic Methods.

作者信息

Yeo Li Key, Olusanya Temidayo O B, Chaw Cheng Shu, Elkordy Amal Ali

机构信息

School of Pharmacy and Pharmaceutical Sciences, University of Sunderland, Sunderland SR1 3SD, UK.

出版信息

Pharmaceutics. 2018 Oct 13;10(4):185. doi: 10.3390/pharmaceutics10040185.

Abstract

Novel niosomal formulations containing cinnarizine were developed to enhance its drug characteristics. In this work, niosomes (non-ionic surfactant vesicles) were prepared by conventional thin-film hydration (TFH) and microfluidic (MF) methods with sorbitan monostearate (Span 60), cholesterol, and co-surfactants (Cremophor ELP, Cremophor RH40 and Solutol HS15) as key excipients. The aim was to study the effect of cinnarizine on the characteristics of different niosomal formulations manufactured by using different methods. For effective targeted oral drug delivery, the efficacy of niosomes for therapeutic applications is correlated to their physiochemical properties. Niosome vesicles prepared were characterised using dynamic light scattering technique and the morphology of niosomes dispersion was characterised using optical microscopy. Dialysis was carried out to purify niosome suspensions to determine drug loading and drug release studies was performed to study the potential use of niosomal systems for cinnarizine.

摘要

开发了含有桂利嗪的新型脂质体剂型以增强其药物特性。在这项工作中,以单硬脂酸山梨醇酯(司盘60)、胆固醇和助表面活性剂(聚氧乙烯蓖麻油ELP、聚氧乙烯蓖麻油RH40和聚乙二醇蓖麻油HS15)作为关键辅料,通过传统薄膜水化法(TFH)和微流控法(MF)制备了脂质体(非离子表面活性剂囊泡)。目的是研究桂利嗪对采用不同方法制备的不同脂质体剂型特性的影响。为实现有效的靶向口服给药,脂质体用于治疗应用的功效与其物理化学性质相关。使用动态光散射技术对制备的脂质体囊泡进行表征,并使用光学显微镜对脂质体分散体的形态进行表征。进行透析以纯化脂质体悬浮液,以测定载药量,并进行药物释放研究以研究脂质体系统用于桂利嗪的潜在用途。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c903/6321096/05cdc7cfac5a/pharmaceutics-10-00185-g001.jpg

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