Preparation and in vitro evaluation of lipidic carriers and fillers for inhalation
Preparation and in vitro evaluation of lipidic carriers and fillers for inhalation
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DOI：
10.1016/j.ejpb.2005.11.003
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发表时间：
2006-05-01
影响因子：
4.9
通讯作者：
Amighi, K
中科院分区：
文献类型：
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作者：
Sebti, T;Amighi, K
本研究涉及由生物相容性磷脂和胆固醇组成的固体脂质微粒（SLmP）的组合物，以及它们作为载体或作为填料经由干粉吸入器（DPI）将药物直接递送至肺的用途。SLmP通过喷雾干燥获得，并配制成包埋布地奈德的药物基质或物理混合物（药物载体）。它们的开发是为了改善活性药物通过肺部途径的递送。评价SLmP的物理特性，并使用多级液体撞击器（MsLI）进行体外沉积测量。使用Pulmicort Turbuhaler DPI（AstraZeneca）作为比较产品。SLmP看起来是球形低密度材料，其特征在于具有光滑的表面。质量中值直径（D（0，5））和体积平均直径（D[4，3]）很小，分别为1.7 - 3.1 μ m和2.0 - 3.9 μ m。发现由吸入器递送的SLmP制剂释放93-113 μ g的细颗粒剂量（FPD），这与由Pulmicort Turbuhaler递送的FPD（68 μ g）相比是非常有希望的。(c)2005 Elsevier B. V.保留所有权利。
The present study relates to compositions of solid lipidic microparticles(SLmP), composed of biocompatible phospholipids and cholesterol, and their use as carriers or as fillers delivering drugs directly to the lungs via a dry powder inhaler (DPI). SLmP were obtained by spray-drying and were formulated as lipidic matrices entrapping budesonide or as physical blends (drug carrier). They were developed in order to improve the delivery of the active drug by the pulmonary route. The SLmP were evaluated for their physical characteristics and in vitro deposition measurements were performed using the Multi-stage Liquid Impinger (MsLI). The Pulmicort Turbuhaler (R) DPI (AstraZeneca) was used as a comparator product.The SLmP appeared to be spherical low-density material characterized by a smooth surface. The mass median diameters (D(0,5)), and the volume mean diameters (D[4,3]) were tiny and ranged from 1,7 to 3,1 mu m and from 2,0 to 3,9 mu m, respectively. The SLmP formulations, delivered by the Cyclohaler (R) inhaler, were found to emit a fine particle dose (FPD) of 93-113 mu g, which is very promising comparing to the FPD (68 mu g) delivered by the Pulmicort Turbuhaler (R). (c) 2005 Elsevier B.V. All rights reserved.