In situ microemulsion-gel obtained from bioadhesive hydroxypropyl methylcellulose films for transdermal administration of zidovudine
[Display omitted] •In situ microemulsion-gel (ME-Gel) was obtained for the first time from a polymeric film.•HPMC films were able to promote the formation of a ME-Gel at the application site.•In situ ME-Gel showed significant permeation-enhancing effect.•In situ ME-Gel was shown to be a promising sy...
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Veröffentlicht in: | Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2020-04, Vol.188, p.110739-110739, Article 110739 |
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Sprache: | eng |
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•In situ microemulsion-gel (ME-Gel) was obtained for the first time from a polymeric film.•HPMC films were able to promote the formation of a ME-Gel at the application site.•In situ ME-Gel showed significant permeation-enhancing effect.•In situ ME-Gel was shown to be a promising system for transdermal release of drugs.
This study aims to develop in situ microemulsion-gel (ME-Gel) obtained from hydroxypropyl methylcellulose (HPMC) films for transdermal administration of Zidovudine (AZT). Firstly, HPMC films containing propylene glycol (PG) and eucalyptus oil (EO) were obtained and characterized. Later, a pseudo-ternary phase diagram composed of water, EO, tween 80 and PG was obtained and one microemulsion (ME) with a similar proportion of the film components was obtained. ME was transformed in ME-Gel by the incorporation of HPMC. Finally, HPMC films were hydrated with Tween 80 solution to yield in situ ME-Gel and its effect on AZT skin permeation was compared with HPMC film hydrated with water (F5hyd). The results showed that the ME and ME-Gel presented a droplet size of 16.79 and 122.13 μm, respectively, polydispersity index (PDI) < 0.39 and pH between 5.10 and 5.40. The incorporation of HPMC resulted in viscosity about 2 times higher than the use of ME. The presence of AZT did not alter the formulation properties. The in situ ME-Gel promoted a two-fold increase in the permeated amount of AZT compared to F5hyd. The results suggest that it was possible to obtain an ME-Gel in situ from HPMC films and that its effect on transdermal permeation of AZT was significant. |
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ISSN: | 0927-7765 1873-4367 |
DOI: | 10.1016/j.colsurfb.2019.110739 |