PURPOSE: The aim of this study was to investigate the effect of elastic and rigid vesicles on the penetration of pergolide across human skin. METHODS: Vesicles used consisted of the bilayer-forming surfactant L-595 (sucrose laurate ester) and the micelle-forming surfactant PEG-8-L (octaoxyethylene laurate ester), together with the stabilizer sulfosuccinate. A series of L-595/PEG-8-L/sulfosuccinate vesicles were investigated, ranging from very rigid to very elastic. Pergolide-loaded elastic and rigid vesicles were visualized using Cryo-TEM and characterized for size and stability. Transdermal penetration of pergolide from different vesicle compositions was studied in vitro using flow-through Franz diffusion cells. A saturated buffer solution served as the control. RESULTS: Vesicle composition had a major effect on the physicochemical characteristics, morphology and drug solubility of the vesicular system. L-595/PEG-8-L/sulfosuccinate (70/30/5) elastic vesicles gave the best balance between vesicle stability and elasticity, as well as the highest drug solubility. Transport studies clearly showed that elastic vesicles were superior to rigid vesicles. Elastic vesicles enhanced the drug transport compared to the buffer control, although rigid vesicles decreased the drug transport. The best drug transport was achieved from L-595/PEG-8-L/sulfosuccinate (70/30/5) elastic vesicles, resulting in a steady-state flux of 13.6 +/- 2.3 ng/ (h*cm2). This was a 6.2-fold increase compared to the most rigid vesicles. CONCLUSIONS: This study supports the hypothesis that elastic vesicles are superior to rigid vesicles as vehicles for transdermal drug delivery.
PURPOSE: The aim of this study was to investigate the effect of elastic and rigid vesicles on the penetration of pergolide across human skin. METHODS: Vesicles used consisted of the bilayer-forming surfactant L-595 (sucrose laurate ester) and the micelle-forming surfactant PEG-8-L (octaoxyethylene laurate ester), together with the stabilizer sulfosuccinate. A series of L-595/PEG-8-L/sulfosuccinate vesicles were investigated, ranging from very rigid to very elastic. Pergolide-loaded elastic and rigid vesicles were visualized using Cryo-TEM and characterized for size and stability. Transdermal penetration of pergolide from different vesicle compositions was studied in vitro using flow-through Franz diffusion cells. A saturated buffer solution served as the control. RESULTS: Vesicle composition had a major effect on the physicochemical characteristics, morphology and drug solubility of the vesicular system. L-595/PEG-8-L/sulfosuccinate (70/30/5) elastic vesicles gave the best balance between vesicle stability and elasticity, as well as the highest drug solubility. Transport studies clearly showed that elastic vesicles were superior to rigid vesicles. Elastic vesicles enhanced the drug transport compared to the buffer control, although rigid vesicles decreased the drug transport. The best drug transport was achieved from L-595/PEG-8-L/sulfosuccinate (70/30/5) elastic vesicles, resulting in a steady-state flux of 13.6 +/- 2.3 ng/ (h*cm2). This was a 6.2-fold increase compared to the most rigid vesicles. CONCLUSIONS: This study supports the hypothesis that elastic vesicles are superior to rigid vesicles as vehicles for transdermal drug delivery.
Authors: M Kirjavainen; A Urtti; I Jääskeläinen; T M Suhonen; P Paronen; R Valjakka-Koskela; J Kiesvaara; J Mönkkönen Journal: Biochim Biophys Acta Date: 1996-12-13
Authors: Gelen Rodríguez; Guadalupe Soria; Elisenda Coll; Laia Rubio; Lucyanna Barbosa-Barros; Carmen López-Iglesias; Anna M Planas; Joan Estelrich; Alfons de la Maza; Olga López Journal: Biophys J Date: 2010-07-21 Impact factor: 4.033
Authors: Gelen Rodríguez; Laia Rubio; Clara Barba; Carmen López-Iglesias; Alfons de la Maza; Olga López; Mercedes Cócera Journal: Eur Biophys J Date: 2012-12-27 Impact factor: 1.733
Authors: Ana L Riveros; Cynthia Eggeling; Sebastián Riquelme; Carolina Adura; Carmen López-Iglesias; Fanny Guzmán; Eyleen Araya; Mario Almada; Josué Juárez; Miguel A Valdez; Ignacio A Fuentevilla; Olga López; Marcelo J Kogan Journal: Int J Nanomedicine Date: 2020-03-17