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可吸入纳米复合微粒:制备、表征及影响制剂的因素

Inhalable nanocomposite microparticles: preparation, characterization and factors affecting formulation.

作者信息

Elsayed Ibrahim, AbouGhaly Mohamed Hassan Hany

机构信息

a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Cairo University , Cairo 11562 , Egypt Tel: +20 1149944306 ; Fax: +20 233058256 ;

b College of Pharmacy , Gulf Medical University , Ajman , UAE.

出版信息

Expert Opin Drug Deliv. 2016;13(2):207-22. doi: 10.1517/17425247.2016.1102224. Epub 2015 Oct 29.

Abstract

INTRODUCTION

Nanocomposite microparticles are intelligent carriers utilised for pulmonary drug delivery. These carriers are composed of drug-encapsulated nanoparticles dispersed in microstructures of polysaccharides. Upon administration, the inhaled microparticles can penetrate and be deposited deeply in the lung due to their adjusted aerodynamic particle size. Subsequently, the nanoparticles are released into the lung and are retained there for a prolonged time due to their resistance to immunological opsonisation, engulfment and digestion.

AREA COVERED

Nanocomposite microparticles may be prepared by spray drying, spray freeze drying, spray drying fluidised bed granulation or dry coating techniques. The selection of the included excipients, preparation technique and optimisation of the operational parameter play a significant role in the determination of the aerodynamic particle size, redispersibility of the nanoparticles, morphology, yield, moisture content, flowability and in vitro drug release. Moreover, the in vivo behaviour of this novel carrier may be optimised and traced by studying the lung deposition of the inhaled particles and the biological activity of the encapsulated drug.

EXPERT OPINION

Nanocomposite microparticles have been found to be superior to both nanoparticles and microparticles and may represent a promising carrier for pulmonary drug delivery.

摘要

引言

纳米复合微粒是用于肺部药物递送的智能载体。这些载体由分散在多糖微结构中的药物包封纳米颗粒组成。给药时,吸入的微粒因其调整后的空气动力学粒径可穿透并深入沉积在肺部。随后,纳米颗粒释放到肺部,并由于其对免疫调理、吞噬和消化的抗性而在那里长时间滞留。

涵盖领域

纳米复合微粒可通过喷雾干燥、喷雾冷冻干燥、喷雾干燥流化床制粒或干包衣技术制备。所包含辅料的选择、制备技术和操作参数的优化在空气动力学粒径、纳米颗粒的再分散性、形态、产率、水分含量、流动性和体外药物释放的测定中起着重要作用。此外,通过研究吸入颗粒的肺部沉积和包封药物的生物活性,可以优化和追踪这种新型载体的体内行为。

专家观点

已发现纳米复合微粒优于纳米颗粒和微粒,可能是一种有前途的肺部药物递送载体。

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