Mesoporous silicon microparticles for oral drug delivery:: Loading and release of five model drugs
Mesoporous silicon microparticles for oral drug delivery:: Loading and release of five model drugs
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DOI：
10.1016/j.jconrel.2005.08.017
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发表时间：
2005-11-28
影响因子：
10.8
通讯作者：
Lehto, VP
中科院分区：
文献类型：
--
作者：
Salonen, J;Laitinen, L;Lehto, VP
采用热碳化（TCPSi）或热氧化（TOPSi）制备介孔硅（PSi）微粒，以获得适合口服给药应用的表面。研究了5种模型药物（安替比林、布洛芬、灰黄霉素、雷尼替丁和呋塞米）的加载及其随后的释放行为。将药物加载到TCPSi和TOPSi微颗粒中表明，除了影响颗粒在水溶剂或有机溶剂存在下的稳定性外，表面性质还会影响化合物对颗粒的亲和力。除了表面性质外，药物和装载溶液的化学性质似乎对装载过程至关重要。这反映在获得的加载效率上，TCPSi颗粒的加载效率在9%到45%之间变化。负载药物从TCPSi微颗粒的释放速度取决于原料药的特征溶解行为。当游离/卸载药物的溶出速度高时，微颗粒引起延迟释放。然而，对于溶解性差的药物，加载到介孔微粒中明显改善了溶解性。此外，当药物被装载到微颗粒中时，溶解的pH依赖性降低。(c) 2005 Elsevier B.V.版权所有
Mesoporous silicon (PSi) microparticles were produced using thermal carbonization (TCPSi) or thermal oxidation (TOPSi) to obtain surfaces suitable for oral drug administration applications. The loading of five model drugs (antipyrine, ibuprofen, griseofulvin, ranitidine and furosemide) into the microparticles and their subsequent release behaviour were studied. Loading of drugs into TCPSi and TOPSi microparticles showed, that in addition to effects regarding the stability of the particles in the presence of aqueous or organic solvents, surface properties will affect compound affinity towards the particle. In addition to the surface properties, the chemical nature of the drug and the loading solution seems to be critical to the loading process. This was reflected in the obtained loading efficiencies, which varied between 9% and 45% with TCPSi particles. The release rate of a loaded drug from TCPSi microparticles was found to depend on the characteristic dissolution behaviour of the drug substance. When the dissolution rate of the free/unloaded drug was high, the microparticles caused a delayed release. However, with poorly dissolving drugs, the loading into the mesoporous microparticles clearly improved dissolution. In addition, pH dependency of the dissolution was reduced when the drug substance was loaded into the microparticles. (c) 2005 Elsevier B.V. All rights reserved.