Preparation of solid lipid microcapsules via solid-in-oil-in-water dispersions by premix membrane emulsification
Preparation of solid lipid microcapsules via solid-in-oil-in-water dispersions by premix membrane emulsification
复制标题
DOI：
10.1016/j.cej.2009.03.061
复制
发表时间：
2009-08-15
影响因子：
15.1
通讯作者：
Kukizaki, Masato
中科院分区：
文献类型：
--
作者：
Kukizaki, Masato
本研究提出了一种新方法，通过预混膜乳化和随后 S/O/W 分散体中油相的固化，通过水包油包固体 (S/O/W) 分散体制备具有窄粒径分布的亲水性药物封装的固体脂质微胶囊 (SLMC)，用于药物递送系统。这项工作的主要方面是在固体脂质中形成亲水性药物的纳米级固体颗粒，其次是将纳米级颗粒封装在尺寸控制的脂质微胶囊中。制备的胶囊具有由熔点为55℃的高熔点甘油三酯、三肉豆蔻酸甘油酯组成的基质型结构。在胶囊的亲脂性基质中，嵌入亲水性药物维生素B(12)(VB(12))的纳米级颗粒。首先，通过将初步制备的油包水乳液中含有 1.1 wt.% VB(12) 的水滴除水来制备油包固 (S/O) 分散体，然后在 60 ℃ 下与外部水相混合，形成粗 S/O/W 分散体。在此温度下，在25 kPa的跨膜压力下，迫使所得的S/O/W分散体通过平均孔径为14.8μm的Shirasu多孔玻璃（SPG）膜，以非常高的跨膜通量（11.8 m(3) m(-2) h(-1)）形成尺寸均匀的S/O液滴。随后 S/O/W 分散体中油相的固化产生平均粒径为 15.4 μm 且包封率较高（高达 93.5%）的 SLMC。在预混膜乳化中，跨膜压力影响 S/O/W 分散体和所得 SLMC 的性能。在较高的跨膜压力下，由于膜孔内较高的剪切应力，会产生较小的 S/O 液滴，其尺寸分布较宽，且封装效率较低。通过调节预混膜乳化中的膜孔径和跨膜压力来控制 SLMC 的粒径。 (C) 2009 Elsevier B.V. 保留所有权利。
This study presents a novel method for the preparation of hydrophilic drug-encapsulated solid lipid microcapsules (SLMCs) with a narrow particle size distribution for drug delivery systems via solid-in-oil-in-water (S/O/W) dispersions by premix membrane emulsification and subsequent solidification of the oil phase in the S/O/W dispersion. The primary aspect of this work is to form nano-order solid particles of hydrophilic drugs in solid lipids and the secondary is to encapsulate of the nano-order particles in size-controlled lipid microcapsules. The prepared capsules had a matrix type structure composed of a high-melting triglyceride, glycerol trimyristate with a melting point of 55 degrees C. In the lipophilic matrix of the capsule, nano-order particles of a hydrophilic drug, vitamin B(12) (VB(12)) were embedded. Initially, a solid-in-oil (S/O) dispersion was prepared by water removal of the water droplets containing 1.1 wt.% VB(12) in a water-in-oil emulsion preliminary prepared, followed by mixing with an external water phase at 60 degrees C to form a coarse S/O/W dispersion. By forcing the resultant S/O/W dispersion through a Shirasu porous glass (SPG) membrane with a mean pore diameter of 14.8 mu m at this temperature under a transmembrane pressure of 25 kPa, uniformly sized S/O droplets were formed at a very high transmembrane flux (11.8 m(3) m(-2) h(-1)). Subsequent solidification of the oil phase in the S/O/W dispersion resulted in SLMCs with a mean particle diameter of 15.4 mu m and a high encapsulation efficiency (up to 93.5%). In premix membrane emulsification the transmembrane pressure affected the properties of the S/O/W dispersion and the resultant SLMCs. At the higher transmembrane pressures, smaller S/O droplets with broader size distributions and lower encapsulation efficiencies were produced, due to the higher shear stresses inside the membrane pores. The particle size of SLMCs was controlled by adjusting the membrane pore size and transmembrane pressure in premix membrane emulsification. (C) 2009 Elsevier B.V. All rights reserved.