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通过电喷雾法制备载布地奈德的聚己内酯纳米珠用于药物控释。

Preparation of budesonide-loaded polycaprolactone nanobeads by electrospraying for controlled drug release.

作者信息

Midhun B T, Shalumon K T, Manzoor K, Jayakumar R, Nair S V, Deepthy M

机构信息

a Amrita Centre for Nanosciences & Molecular Medicine, Amrita Institute of Medical Sciences and Research Centre, Amrita Vishwa Vidhyapeetham University, Cochin-682 041, India.

出版信息

J Biomater Sci Polym Ed. 2011;22(18):2431-44. doi: 10.1163/092050610X540486.

DOI:10.1163/092050610X540486
PMID:21144167
Abstract

Corticosteroids such as budesonide are the drugs of choice for the treatment of inflammatory disorders with an inherent limitation, viz., rapid elimination. To overcome this constraint and attain sustained release, budesonide was encapsulated in a biodegradable polymer, polycaprolactone (PCL), by DC electrospraying. By varying the experimental parameters involved in electrospraying such as applied voltage, flow rate, viscosity as well as conductivity of the polymer solution, the dimensionality of nanostructures was tuned from 1-D nanofibers to spherical nanoparticles. By adopting this rapid and viable method of DC electrospraying, we successfully prepared aqueous suspensions of nearly monodispersed, nano-sized drug encapsulated PCL. Drug encapsulation efficiency, in vitro drug release as well as biocompatibility studies of budesonide-loaded PCL nanobeads were carried out. The cytocompatible nanobeads prepared by electrospraying exhibited good encapsulation efficiency (approx. 75%), with controlled drug release enabled by the dissolution of the polymer. Our results demonstrate the potential of this novel technique of electrospraying in developing efficient drug encapsulated polymeric nanocarriers possessing sustained drug release profile.

摘要

诸如布地奈德之类的皮质类固醇是治疗具有固有局限性(即快速消除)的炎症性疾病的首选药物。为了克服这一限制并实现持续释放,通过直流电喷雾将布地奈德包裹在可生物降解的聚合物聚己内酯(PCL)中。通过改变电喷雾过程中涉及的实验参数,如施加电压、流速、聚合物溶液的粘度以及电导率,纳米结构的维度从一维纳米纤维调整为球形纳米颗粒。通过采用这种快速且可行的直流电喷雾方法,我们成功制备了几乎单分散的、纳米尺寸的药物包裹PCL的水悬浮液。进行了药物包封效率、体外药物释放以及布地奈德负载PCL纳米珠的生物相容性研究。通过电喷雾制备的细胞相容性纳米珠表现出良好的包封效率(约75%),聚合物的溶解实现了药物的可控释放。我们的结果证明了这种新型电喷雾技术在开发具有持续药物释放特性的高效药物包裹聚合物纳米载体方面的潜力。

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