title: Preparation of curcuminoid niosomes for enhancement of skin permeation.
abstract: Curcuminoids (curcumin, desmethoxycurcumin, and bisdesmethoxycurcumin) are major bioactive substances found in turmeric (Curcuma longa L.) extracts and possess antioxidant, anti-inflammatory, antimicrobial and anticancer properties. In this study, curcuminoid niosomes prepared with a series of Span non-ionic surfactants were developed to enhance the skin permeation of curcuminoids. Formulations were evaluated based on aggregation of niosomes, curcuminoid loading, % entrapment efficiency and in vitro permeation of curcuminoids through shed snake skin. Optimal formulations of curcuminoid niosomes including sorbitan monooleate, cholesterol, and Solulan C-24 at a mole ratio of 47.5:47.5:5 were obtained. Up to 11 micromoles of curcuminoids could be loaded in the niosome with a % entrapment efficiency of 83%. About 90% of the niosomes had a diameter of 12.25 +/- 5.00 microm. The niosomes significantly enhanced permeation of curcuminoids compared with a methanolic solution of curcuminoids: 4% of entrapped curcuminoids traversed the shed snake skin, whereas permeation from the methanolic solution was undetectable. The fluxes of curcumin, desmethoxycurcumin, and bisdesmethoxycurcumin were 1.117, 0.263, and 0.057 microg/(cm2h), respectively, consistent with the relative hydrophobicity of curcumin > desmethoxycurcumin > bisdesmethoxycurcumin. In conclusion, our data show that curcuminoids can be successfully formulated as niosomes and that such formulations have improved properties for transdermal delivery.
authors: Pharmaceutical Technology (International) Program, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok, Thailand.
authors: N
authors: N
authors: Rungphanichkul
authors: U
authors: U
authors: Nimmannit
authors: W
authors: W
authors: Muangsiri
authors: P
authors: P
authors: Rojsitthisak
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical; D002784:Cholesterol; D002851:Chromatography, High Pressure Liquid; D003474:Curcumin / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D006601:Hexoses; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D008081:Liposomes / Q000138:chemical synthesis*; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D010539:Permeability; D015203:Reproducibility of Results; D012869:Skin Absorption / Q000187:drug effects*; D012911:Snakes; D013501:Surface-Active Agents
chemical_list: D006601:Hexoses; D007202:Indicators and Reagents; D008081:Liposomes; D013501:Surface-Active Agents; C018665:sorbitan monooleate; C061705:sorbitan monopalmitate; D002784:Cholesterol; D003474:Curcumin; C009298:sorbitan monostearate