title: Physicochemical properties and skin permeation of Span 60/Tween 60 niosomes of ellagic acid.
abstract: Ellagic acid (EA) is a potent antioxidant phytochemical substance which has limitation to use due to its poor biopharmaceutical properties, low solubility and low permeability. The aim of the present study was to develop niosomal formulations obtained from the mixture of Span 60 and Tween 60 that could encapsulate EA for dermal delivery. The EA-loaded niosomes were prepared with 1:0, 2:1, 1:1, 0:1 Span 60 and Tween 60, using polyethylene glycol 400 (PEG 400), propylene glycol (PG) or methanol (MeOH) as a solubilizer. The influence of formulations on vesicle size, entrapment efficiency and stability of EA-loaded niosomes was investigated. It was found that all ratios of surfactants could produce EA-loaded niosomes when using 15% (v/v) PG, 15% (v/v) PEG 400 or 20% (v/v) MeOH. The niosomes were spherical multilamellar vesicles showing the localization of EA in the vesicles. The vesicle sizes of the niosomes after extrusion were 124-752 nm with PI less than 0.4. The percentages of entrapment efficiency (% E.E.) of all EA-loaded niosomes varied between 1.35% and 26.75% while PEG 400 niosomes gave the highest % E.E. The most stable and highest entrapped formulation was 2:1 Span 60 and Tween 60 niosomes. Additionally, the in vitro skin permeation revealed that penetration of EA from the niosomes depended on vesicle size, the amount of EA entrapped and the added solubilizers which could act as a permeation enhancer. From skin distribution study, the EA-loaded niosomes showed more efficiency in the delivery of EA through human epidermis and dermis than EA solution. The results indicated that the Span 60 and Tween 60 niosomes may be a potential carrier for dermal delivery of EA.
authors.affiliation: Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand. pyvbp@mahidol.ac.th
authors.forename: Varaporn Buraphacheep
authors.initials: VB
authors.lastname: Junyaprasert
authors.forename: Pratyawadee
authors.initials: P
authors.lastname: Singhsa
authors.forename: Jiraphong
authors.initials: J
authors.lastname: Suksiriworapong
authors.forename: Doungdaw
authors.initials: D
authors.lastname: Chantasart
mesh_terms: D000279:Administration, Cutaneous; D000328:Adult; D000975:Antioxidants / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D002626:Chemistry, Pharmaceutical; D004339:Drug Compounding; D004610:Ellagic Acid / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D005260:Female; D006601:Hexoses / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008081:Liposomes; D018613:Microscopy, Confocal; D008875:Middle Aged; D010316:Particle Size; D010539:Permeability; D011136:Polysorbates / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility; D013501:Surface-Active Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D000975:Antioxidants; D006601:Hexoses; D008081:Liposomes; D011136:Polysorbates; D013501:Surface-Active Agents; D004610:Ellagic Acid; C009298:sorbitan monostearate