Romanian Society of Pharmaceutical Sciences
 

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DEVELOPMENT OF MICROEMULSION-LOADED HYDROGEL FORMULATIONS FOR TOPICAL DELIVERY OF METOPROLOL TARTRATE: PHYSICOCHEMICAL CHARACTERIZATION AND EX VIVO EVALUATION

LAVINIA VLAIA 1#, IOANA OLARIU 1#, GEORGETA CONEAC1*, ANA MARIA MUŢ1, CĂLIN POPOIU2, STĂNCIULESCU CORINA2, DAN FLORIN ANGHEL3, MONICA ELISABETA MAXIM3, SAMI KALAS4, VICENŢIU VLAIA5

1.“Victor Babeş” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Technology, 2 Eftimie Murgu Square, 300041, Timişoara, Romania
2.“Victor Babeş” University of Medicine and Pharmacy, Faculty of Medicine, Department of Pediatrics, 2 Eftimie Murgu Square, 300041, Timişoara, Romania
3.“Ilie Murgulescu” Institute of Physical Chemistry of the Romanian Academy, Laboratory of Colloid Chemistry, 202 Splaiul Independenţei, 060021, Bucharest, Romania
4.“Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmaceutics, 6th Traian Vuia Street, 020956, Bucharest, Romania
5.“Victor Babeş” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Organic Chemistry, 2 Eftimie Murgu Square, 300041, Timişoara, Romania

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This study aimed to develop and assess microemulsion-loaded hydrogels (ME GEL) as novel topical drug delivery vehicles for a hydrophilic drug, metoprolol tartrate (MT). Solubility studies for metoprolol tartrate were conducted using various oils, non-ionic surfactants and cosurfactants for screening the microemulsion components. To define the microemulsion region, pseudoternary phase diagrams, created by a new method (Phase Diagram by Micro Plate Dilution method), were used. The selected MT loaded microemulsions were converted into gel form, using Carbopol EDT 2020 and were characterised for droplet size, polydispersity index and zeta potential. The permeation of MT through excised pig ear skin was studied using vertical diffusion cells; the permeation (flux, permeability coefficient, lag time) and release (release rate, diffusion coefficient) parameters of MT in the ME GEL formulations and hydrogel were calculated. The skin permeation profile of metoprolol tartrate from the experimental formulations followed both Korsmeyer-Peppas and Higuchi kinetics. Their stability, safety and therapeutic efficacy need to be further investigated by in vitro and in vivo studies.