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

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Karaman E. F., ÇELİK B., Ozdemir S., Tekkeli E. K., Demirkoz A. B., Gonullu U., ...Daha Fazla

FARMACIA, cilt.68, sa.4, ss.646-655, 2020 (SCI-Expanded, Scopus) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 68 Sayı: 4
  • Basım Tarihi: 2020
  • Doi Numarası: 10.31925/farmacia.2020.4.9
  • Dergi Adı: FARMACIA
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, EMBASE, International Pharmaceutical Abstracts
  • Sayfa Sayıları: ss.646-655
  • Anahtar Kelimeler: 18-beta glycyrrhetinic acid, enoxolone, anti-inflammatory drugs, skin penetration, penetration enhancers, SKIN PENETRATION, STRATUM-CORNEUM, ESSENTIAL OILS, PERMEATION, MECHANISM
  • Açık Arşiv Koleksiyonu: AVESİS Açık Erişim Koleksiyonu
  • Bezmiâlem Vakıf Üniversitesi Adresli: Evet

Özet

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.