Romanian Society of Pharmaceutical Sciences

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PERCUTANEOUS PENETRATION ENHANCEMENT OF PROPRANOLOL HYDROCHLORIDE FROM HPMC-BASED HYDROETHANOLIC GELS CONTAINING TERPENES

LAVINIA VLAIA1, IOANA OLARIU1*, GEORGETA CONEAC1, VICENŢIU VLAIA2, CĂLIN POPOIU3, STĂNCIULESCU CORINA3, ANA MARIA MUŢ1, ZOLTAN SZABADAI4, DUMITRU LUPULEASA5

1.”Victor Babeş” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Technology, Eftimie Murgu Square 1, 300041, Timişoara, Romania
2.“Victor Babeş” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Organic Chemistry, Eftimie Murgu Square 1, 300041, Timişoara, Romania
3.“Victor Babeş” University of Medicine and Pharmacy, Faculty of Medicine, Department of Pediatrics, Eftimie Murgu Square 1, 300041, Timişoara, Romania
4.”Victor Babeş” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Drug Analysis, Eftimie Murgu Square 1, 300041, Timişoara, Romania
5”Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Technology, Traian Vuia 6, 020956, Bucharest, Romania

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The aim of the present study was to investigate the enhancing effect of five terpenes (menthol, camphor, eucalyptol, thymol and α-bisabolol) at 5% w/w concentration on the in vitro percutaneous penetration of propranolol hydrochloride (PRHCl) from hydroxypropylmethylcellulose (HPMC) gels containing ethanol 60% w/w. Permeation experiments were performed on excised pig ear skin. Permeation (flux, permeability coefficient, lag time) and release (release rate, diffusion coefficient) parameters of PRHCl in the gels with and without terpene enhancers were calculated. The results showed that each of the studied terpenes increased significantly the transdermal permeation of PRHCl through pig ear skin compared to control. Eucalyptol was the most effective accelerant, producing the highest enhancement ratio of flux (ERflux = 12.74) and the lowest lag time (1.97 h). Menthol and α-bisabolol showed mild enhancing activity, PRHCl having a rate of permeation 8.98- and 6.74-fold higher than that of control and a lag time of 4.12 and 2 h respectively. The enhancing effect of thymol on PRHCl skin permeation was lower than that of menthol, although the drug showed comparable lag time values in the presence of both terpenes. In the presence of camphor, PRHCl exhibited the lowest flux and a lag time value similar to that of thymol containing gel. The in vitro PRHCl permeation through pig ear skin was best described by the zero-order model (in the case of the control gel and that with camphor) and by the Korsmeyer-Pepas model (in the case of all the other studied formulations). The results suggest the potential use of HPMC-based hydroethanolic gels containing 5% eucalyptol or α-bisabolol as vehicles for topical delivery of PRHCl.