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制备 BCS II 类药物的电纺纳米纤维以增强皮肤的溶解和渗透。

Fabrication of electrospun nanofibres of BCS II drug for enhanced dissolution and permeation across skin.

机构信息

Department of Pharmaceutics, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandwane, Pune 411 038, Maharashtra, India.

出版信息

J Adv Res. 2016 May;7(3):483-9. doi: 10.1016/j.jare.2016.03.009. Epub 2016 Apr 4.


DOI:10.1016/j.jare.2016.03.009
PMID:27222753
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4856818/
Abstract

The present work reports preparation of irbesartan (IBS) loaded nanofibre mats using electrospinning technique. The prepared nanofibres were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction analysis, in vitro diffusion and ex vivo skin permeation studies. FTIR studies revealed chemical compatibility of IBS and polyvinyl pyrrolidine (PVP K-30). SEM images confirmed formation of nanofibres wherein IBS existed in amorphous form as revealed by DSC and XRD analyses. The prepared nanofibre mats of IBS were found to be superior to IBS loaded as cast films when analysed for in vitro IBS release and ex vivo skin permeation studies since the flux of IBS loaded nanofibres was 17 times greater than as cast film. The improvement in drug delivery kinetics of IBS loaded nanofibres could be attributed to amorphization with reduction in particle size of IBS, dispersion of IBS at molecular level in PVP matrix and enormous increase in the surface area for IBS release due to nanonization. Thus transdermal patch of IBS loaded nanofibres can be considered as an alternative dosage form in order to improve its biopharmaceutical properties and enhance therapeutic efficacy in hypertension.

摘要

本工作报道了采用静电纺丝技术制备厄贝沙坦(IBS)负载纳米纤维垫。通过扫描电子显微镜、傅里叶变换红外光谱、差示扫描量热法、X 射线衍射分析、体外扩散和离体皮肤渗透研究对制备的纳米纤维进行了表征。FTIR 研究表明 IBS 和聚乙烯吡咯烷酮(PVP K-30)具有化学相容性。SEM 图像证实了纳米纤维的形成,其中 DSC 和 XRD 分析表明 IBS 以无定形形式存在。在进行 IBS 体外释放和离体皮肤渗透研究时,与负载 IBS 的铸膜相比,制备的 IBS 纳米纤维垫表现出优越性,因为负载 IBS 的纳米纤维的通量比铸膜高 17 倍。IBS 负载纳米纤维的药物传递动力学的改善可归因于 IBS 粒径减小的无定形化、IBS 在 PVP 基质中的分子水平分散以及由于纳米化而使 IBS 释放的表面积极大增加。因此,IBS 负载纳米纤维的透皮贴剂可以被认为是一种替代剂型,以改善其生物制药特性并提高在高血压中的治疗效果。

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本文引用的文献

[1]
Enhanced oral bioavailability and anticancer activity of novel curcumin loaded mixed micelles in human lung cancer cells.

Phytomedicine. 2015-8-28

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Eur J Pharm Sci. 2015-2-20

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