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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Preparation and in vitro evaluation of salbutamol-loaded lipid microparticles for sustained release pulmonary therapy
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Preparation and in vitro evaluation of salbutamol-loaded lipid microparticles for sustained release pulmonary therapy

机译:沙丁胺醇负载脂质微粒的制备及其体外缓释肺评价

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摘要

The aim of this study was to prepare lipid microparticles (LMs) loaded with the polar bronchodilator agent salbutamol, and designed for sustained release pulmonary delivery. The microparticles were produced by melt emulsification followed by a sonication step, using different biocompatible lipid carriers (tristearin, stearic acid and glyceryl behenate) and phosphatidylcholine as the surfactant. The use of salbutamol free base, rather than salbutamol sulphate, was necessary to obtain the incorporation of the drug in the lipid particle matrix. The prolonged release of salbutamol base was achieved only by the glyceryl behenate microparticles (40.9% of encapsulated drug being released after 8h). The salbutamol loading was 4.2% ±0.1 and the mass median diameter, determined by laser diffraction, ranged from 4.8 to 5.4 μm. The sustained release of LMs were formulated as a carrier-free dry powder for inhalation and exhibited a fine particle fraction of 17.3% ±2.2, as measured by multi-stage liquid impinger.
机译:这项研究的目的是制备载有极性支气管扩张剂沙丁胺醇的脂质微粒(LMs),并设计用于持续释放的肺部递送。通过使用不同的生物相容性脂质载体(丁香精,硬脂酸和山hen酸甘油酯)和磷脂酰胆碱作为表面活性剂,通过熔融乳化和随后的超声处理步骤来生产微粒。为了使药物掺入脂质颗粒基质中,必须使用沙丁胺醇游离碱而不是硫酸沙丁胺醇。沙丁胺醇碱的延长释放仅通过山hen酸甘油酯微粒实现(8小时后释放了40.9%的封装药物)。沙丁胺醇的负载量为4.2%±0.1,通过激光衍射测定的质量中值直径为4.8至5.4μm。 LM的持续释放被配制成用于吸入的无载体干粉,并表现出通过多级液体冲击器测量的17.3%±2.2的细颗粒分数。

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