title: Enhanced dissolution and stability of artemisinin by nano-confinement in ordered mesoporous SBA-15 particles.
abstract: 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.
authors.affiliation: Department of Chemical and Biomolecular Engineering, The National University of Singapore , Singapore and.
authors.forename: Kumaran
authors.initials: K
authors.lastname: Letchmanan
authors.forename: Shou-Cang
authors.initials: SC
authors.lastname: Shen
authors.forename: Wai Kiong
authors.initials: WK
authors.lastname: Ng
authors.forename: Reginald B H
authors.initials: RB
authors.lastname: Tan
mesh_terms: D000890:Anti-Infective Agents / Q000737:chemistry* / Q000633:toxicity; D037621:Artemisinins / Q000737:chemistry* / Q000633:toxicity; D018938:Caco-2 Cells / Q000187:drug effects; D002214:Capsules; D002470:Cell Survival / Q000187:drug effects; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry* / Q000633:toxicity; D006801:Humans; D010316:Particle Size; D016062:Porosity; D012822:Silicon Dioxide / Q000737:chemistry* / Q000633:toxicity; D012995:Solubility; D014867:Water / Q000737:chemistry*
chemical_list: D000890:Anti-Infective Agents; D037621:Artemisinins; D002214:Capsules; D005079:Excipients; C509969:SBA-15; D014867:Water; D012822:Silicon Dioxide; C031327:artemisinin
keywords: Cytotoxicity; chemical stability; drug delivery; excipient; physical stability; supersaturation solubility