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Colloids Surf B Biointerfaces ; 188: 110739, 2020 Apr.
Article in English | MEDLINE | ID: mdl-31901623

ABSTRACT

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.


Subject(s)
Methylcellulose/chemistry , Prodrugs/chemistry , Zidovudine/chemistry , Administration, Cutaneous , Animals , Emulsions/administration & dosage , Emulsions/chemistry , Emulsions/metabolism , Eucalyptus Oil/administration & dosage , Eucalyptus Oil/chemistry , Eucalyptus Oil/metabolism , Gels/administration & dosage , Gels/chemistry , Gels/metabolism , Male , Methylcellulose/administration & dosage , Methylcellulose/metabolism , Particle Size , Prodrugs/administration & dosage , Prodrugs/metabolism , Propylene Glycol/administration & dosage , Propylene Glycol/chemistry , Propylene Glycol/metabolism , Rats , Rats, Wistar , Skin/chemistry , Skin/metabolism , Skin Absorption , Surface Properties , Zidovudine/administration & dosage , Zidovudine/metabolism
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