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

被引:3
作者
Karaman, Ecem Fatma [1 ]
Celik, Burak [2 ]
Ozdemir, Samet [3 ]
Tekkeli, Evrim Kepekci [4 ]
Demirkoz, Asli Barla [5 ,6 ]
Gonullu, Umit [1 ]
Uner, Melike [1 ]
机构
[1] Istanbul Univ, Dept Pharmaceut Technol, Fac Pharm, TR-34116 Istanbul, Turkey
[2] Bezmialem Vakif Univ, Fac Pharm, Dept Pharmaceut Technol, Adnan Menderes Bulvari,Vatan Caddesi, TR-34093 Istanbul, Turkey
[3] Yeditepe Univ, Fac Pharm, Dept Pharmaceut Technol, Inonu Mah,Kayisdagi Cad,26, TR-34755 Istanbul, Turkey
[4] Bezmialem Vakif Univ, Fac Pharm, Dept Pharmaceut Analyt Chem, Adnan Menderes Bulvari,Vatan Caddesi, TR-34093 Istanbul, Turkey
[5] Aromsa Flavours & Food Addit San & Tic AS, Dept Res & Dev Ctr, Kocaeli, Turkey
[6] Halic Univ, Fac Engn, TR-34445 Istanbul, Turkey
关键词
18-beta glycyrrhetinic acid; enoxolone; anti-inflammatory drugs; skin penetration; penetration enhancers; SKIN PENETRATION; STRATUM-CORNEUM; ESSENTIAL OILS; PERMEATION; MECHANISM;
D O I
10.31925/farmacia.2020.4.9
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Topical formulations of 18-beta glycyrrhetinic acid (18-beta 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-beta GA permeated from the base oil/water emulsion (53.19 +/- 22.25 mcg/cm(2) ) was approximately twice higher than the base oleaginous cream (29.17 +/- 3.85 mcg/cm(2)) while there was no 18-beta GA permeation from the base hydrogel formulation to the skin (p < 0.05). Incorporation of propylene glycol was generally found to increase 18-beta 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-beta GA permeation to the skin.
引用
收藏
页码:646 / 655
页数:10
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