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
* corresponding author: ioana_curescu@yahoo.co.uk
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Abstract:
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...
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