Enhanced dissolution and stability of artemisinin by nano-confinement in ordered mesoporous SBA-15 particles

被引：22

作者：

Letchmanan, Kumaran ^{[1
,2
]}

Shen, Shou-Cang ^{[2
]}

Ng, Wai Kiong ^{[2
]}

Tan, Reginald B. H. ^{[1
,2
]}

机构：

[1] Natl Univ Singapore, Dept Chem & Biomol Engn, Singapore 117576, Singapore

[2] ASTAR, Inst Chem & Engn Sci, Singapore, Singapore

来源：

JOURNAL OF MICROENCAPSULATION | 2015年 / 32卷 / 04期

关键词：

Cytotoxicity; chemical stability; drug delivery; excipient; physical stability; supersaturation solubility; DRUG-DELIVERY SYSTEMS; POORLY SOLUBLE DRUGS; ORAL BIOAVAILABILITY; AMORPHOUS STATE; SOLID-STATE; SILICA; MICROPARTICLES; SOLUBILITY; RELEASE; SIZE;

D O I：

10.3109/02652048.2015.1035684

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Dissolution of poorly water-soluble drug, Artemisinin (ART), was enhanced by encapsulating the drug particles inside pore channels of ordered mesoporous silica, SBA-15, via co-spray drying. The drug release profiles of ART were investigated by using flow-through cell (USP IV) and in vitro dissolution tester (USP II). The co-spray-dried ART/SBA-15 samples demonstrated significantly improved dissolution rates and supersaturation compared to the untreated ART. The low cytotoxicity effect of ART and SBA-15 on Caco-2 cells after 24 h incubation demonstrated the biocompatibility of ART/SBA-15. Finally, the storage stability of the samples was investigated for 6 months under five different storage conditions. Overall, the solid dispersions exhibited excellent physical stability; however, their chemical stability was affected by humidity regardless of storage temperatures. The formulation of solid dispersions of ART/SBA-15 is potentially safe and an effective approach to enhance the solubility of poorly water-soluble ART.

引用

页码：390 / 400

页数：11

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