title: Glycerosomes: a new tool for effective dermal and transdermal drug delivery.
abstract: This work describes glycerosomes, vesicles composed of phospholipids, glycerol, and water, as novel vesicular carriers for (trans)dermal drug delivery. In this work, glycerosomes were prepared by hydrating dipalmitoylglycerophosphatidylcholine-cholesterol films with glycerol aqueous solutions (10-30%, v/v). The model drug was diclofenac sodium salt and conventional liposomes were used as control. Prepared formulations were characterized in terms of size distribution, morphology, zeta potential, and vesicle deformability. Glycerosomes and liposomes were oligo/multilamellar vesicles, spherical in shape with a mean diameter ranging between 81 and 97 nm and a fairly narrow distribution (P.I.=0.14-0.19), negative zeta potential values (from -35 to -48) and drug loading capacity between 64 and 73%. Deformability index of both conventional liposomes and glycerosomes showed that glycerol is able to act as edge activator for dipalmitoylglycerophosphatidylcholine bilayers when used in concentration higher than 10%. DSC studies suggested that glycerosomes are in a more fluid state than conventional liposomes. In vitro transdermal delivery experiments showed an improved skin deposition and permeation of diclofenac when 20 and 30% glycerosomes were used. MTT test demonstrated that glycerosomes were able to reduce the in vitro drug toxicity versus keratinocytes.
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, CNBS, University of Cagliari, Cagliari 09124, Italy.
authors.forename: Maria Letizia
authors.initials: ML
authors.lastname: Manca
authors.forename: Marco
authors.initials: M
authors.lastname: Zaru
authors.forename: Maria
authors.initials: M
authors.lastname: Manconi
authors.forename: Francesco
authors.initials: F
authors.lastname: Lai
authors.forename: Donatella
authors.initials: D
authors.lastname: Valenti
authors.forename: Chiara
authors.initials: C
authors.lastname: Sinico
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Fadda
mesh_terms: D015060:1,2-Dipalmitoylphosphatidylcholine / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D000831:Animals, Newborn; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D004008:Diclofenac / Q000008:administration & dosage* / Q000737:chemistry; D016503:Drug Delivery Systems; D005990:Glycerol / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D015603:Keratinocytes / Q000187:drug effects; D008081:Liposomes; D012867:Skin / Q000378:metabolism*; D013552:Swine
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D008081:Liposomes; D004008:Diclofenac; D015060:1,2-Dipalmitoylphosphatidylcholine; D005990:Glycerol
keywords: Cell viability; DSC; Glycerol; Keratinocytes; Liposomes; Phospholipids