An alkylpolyglucoside surfactant as a prospective pharmaceutical excipient for topical formulations: the influence of oil polarity on the colloidal structure and hydrocortisone in vitro/in vivo permeation.
There is a growing need for research into new skin- and environment-friendly surfactants. This paper focuses on a natural surfactant of an alkylpolyglucoside type, which can form both thermotropic and lyotropic liquid-crystalline phases. The aim of this study was to relate some physicochemical properties (characterised by polarisation and transmission electron microscopy, thermal analysis and rheology) of the three formulations based on cetearyl glucoside and cetearyl alcohol, to the results of in vitro and in vivo bioavailability of hydrocortisone (HC). The three formulations contained oils of different polarity (medium chain triglycerides: MG, isopropyl myristate: IPM and light liquid paraffin: LP), respectively. In vitro permeation was followed through the artificial skin constructs (ASC), while the parameters measured in vivo were erythema index: EI (using instrumental human skin blanching assay), transepidermal water loss (TEWL) and stratum corneum hydration (SCH). The vehicles based on cetearyl glucoside and cetearyl alcohol showed a complex colloidal structure of lamellar liquid-crystalline and lamellar gel-crystalline type, depending on oil polarity. Rheological profile of the vehicle was directly related to the in vitro profile of the HC permeation. In vivo results suggested that the vehicle with MG retarded the HC permeation, whereas less polar IPM and non-polar LP enhanced it. It is suggested that the enhancement is achieved either by a direct interaction with lipid lamellae of the SC or indirectly by improving skin hydration. There were no adverse effects during in vivo study, which indicates a good safety profile of this alkylpolyglucoside surfactant.
Savić
S
S
Institute of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia and Montenegro. snexs@pharmacy.bg.ac.yu
Savić
M
M
Tamburić
S
S
Vuleta
G
G
Vesić
S
S
Müller-Goymann
C C
CC
D000287:Administration, Topical; D000328:Adult; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D002478:Cells, Cultured; D002626:Chemistry, Pharmaceutical; D003102:Colloids; D004339:Drug Compounding; D004548:Elasticity; D005079:Excipients / Q000737:chemistry* / Q000494:pharmacology; D005233:Fatty Alcohols / Q000737:chemistry*; D005260:Female; D005960:Glucosides / Q000737:chemistry*; D006801:Humans; D006854:Hydrocortisone / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D050866:Liquid Crystals; D008899:Mineral Oil / Q000737:chemistry; D009226:Myristates / Q000737:chemistry; D009821:Oils / Q000737:chemistry*; D010539:Permeability; D012869:Skin Absorption / Q000187:drug effects; D013501:Surface-Active Agents / Q000737:chemistry* / Q000494:pharmacology; D014280:Triglycerides / Q000737:chemistry; D014783:Viscosity; D014867:Water / Q000737:chemistry / Q000378:metabolism
D000893:Anti-Inflammatory Agents; D003102:Colloids; D005079:Excipients; D005233:Fatty Alcohols; D005960:Glucosides; D009226:Myristates; D009821:Oils; D013501:Surface-Active Agents; D014280:Triglycerides; D014867:Water; C008205:isopropyl myristate; C419308:cetearyl alcohol; D008899:Mineral Oil; D006854:Hydrocortisone