Romanian Society of Pharmaceutical Sciences
 

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INFLUENCE OF VEHICLES AND PENETRATION ENHANCERS ON ANTI-INFLAMMATORY EFFECT OF 18-β GLYCYRRHETINIC ACID: KINETIC MODELLING OF DRUG RELEASE, IN VIVO AND EX VIVO EXPERIMENTS

ECEM FATMA KARAMAN 1, BURAK ÇELIK 2, SAMET ÖZDEMIR 3, EVRIM KEPEKÇI TEKKELI 4, ASLI BARLA DEMIRKOZ 5,6, ÜMIT GÖNÜLLÜ 1, MELIKE ÜNER 1*

1.Istanbul University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Beyazit 34116, Istanbul, Turkey
2.Bezmialem Vakif University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Adnan Menderes Bulvari, Vatan Caddesi, Fatih 34093, Istanbul, Turkey
3.Yeditepe University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Inonu Mah., Kayisdagi Cad., 26 Agustos Yerlesimi, Atasehir 34755, Istanbul, Turkey
4.Bezmialem Vakif University, Faculty of Pharmacy, Department of Pharmaceutical Analytical Chemistry, Adnan Menderes Bulvari, Vatan Caddesi, Fatih 34093, Istanbul, Turkey
5.Department of Research and Development Center, Aromsa Flavours and Food Additives San. ve Tic. A.S., Kocaeli, Turkey
6.Haliç University, Faculty of Engineering, Sütlüce, Beyoğlu 34445, Istanbul, Turkey

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Topical formulations of 18-β glycyrrhetinic acid (18-β GA) were designed for use in relieving inflammatory and painful conditions of the skin. Formulations were containing penetration enhancers that differ in penetration enhancing mechanisms. Anti-inflammatory effects of formulations and effects of penetration enhancers on penetration and permeation of the drug through rat skin were investigated. The total amount of 18-β GA permeated from the base oil/water emulsion (53.19 ± 22.25 mcg/cm2) was approximately twice higher than the base oleaginous cream (29.17 ± 3.85 mcg/cm2) while there was no 18-β GA permeation from the base hydrogel formulation to the skin (p < 0.05). Incorporation of propylene glycol was generally found to increase 18-β GA permeation to the skin. The highest oedema inhibiting activity was achieved in the oil/water emulsion containing propylene glycol followed by the base oil/water emulsion without a penetration enhancer (p < 0.05). This result was consistent with the ex vivo study. Limonene and oleic acid were found to be insufficient in 18-β GA permeation to the skin.