title: In vitro skin permeation of artemisone and its nano-vesicular formulations.
abstract: The artemisinin derivative artemisone has antitumor activity. In particular when encapsulated in solid lipid nanoparticles (SLNs) and niosomes, it is active against human melanoma A-375 cells, although such formulations have a negligible effect on human keratinocyte cells. The aim here was to determine whether these formulations could enhance the topical delivery and skin permeation of artemisone as a prelude to evaluating use of artemisone and related compounds for melanoma treatment. In vitro skin permeation studies were conducted to determine the concentration of artemisone delivered into the stratum corneum-epidermis and epidermis-dermis. Artemisone-SLNs delivered artemisone into the stratum corneum-epidermis at significantly higher concentration (62.632 μg/mL) than the artemisone-niosomes (12.792 μg/mL). Neither of the controls delivered artemisone into the stratum corneum-epidermis. In the epidermis-dermis, artemisone (13.404 μg/mL) was only detected after application of the SLN formulation. Overall, the excellent topical delivery of artemisone with the SLN formulation coupled with the intrinsic activity of formulated artemisone confirms potential for use in treatment of melanoma.
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
authors.forename: Anupma
authors.initials: A
authors.lastname: Dwivedi
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
authors.forename: Anisha
authors.initials: A
authors.lastname: Mazumder
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
authors.forename: Lizelle T
authors.initials: LT
authors.lastname: Fox
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
authors.forename: Alicia
authors.initials: A
authors.lastname: Brümmer
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
authors.forename: Minja
authors.initials: M
authors.lastname: Gerber
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
authors.forename: Jan L
authors.initials: JL
authors.lastname: du Preez
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
authors.forename: Richard K
authors.initials: RK
authors.lastname: Haynes
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa. Electronic address: Jeanetta.DuPlessis@nwu.ac.za.
authors.forename: Jeanetta
authors.initials: J
authors.lastname: du Plessis
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage*; D037621:Artemisinins / Q000008:administration & dosage*; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D008081:Liposomes; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000008:administration & dosage* / Q000648:ultrastructure; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
chemical_list: D000970:Antineoplastic Agents; D037621:Artemisinins; D008081:Liposomes; C031327:artemisinin
keywords: Artemisone; Melanoma; Nano-vesicles; Niosomes; Skin permeation; Solid lipid nanoparticles