Effect of Mixed Micelle Formulations Including Terpenes on the Transdermal Delivery of Diclofenac

The significant inhibitory action of diclofenac formulated in mixed micelles of lecithin with cholate or deoxycholate was observed on the rat hind paw edema induced by carrageenan. In the primary stage, mixed micelle formulation of deoxycholate was more effective compared with that of cholate. Howev...

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Bibliographic Details
Published in:Biological & Pharmaceutical Bulletin 2003, Vol.26(12), pp.1739-1743
Main Authors: Hendradi, Esti, Obata, Yasuko, Isowa, Koichi, Nagai, Tsuneji, Takayama, Kozo
Format: Article
Language:English
Subjects:
Administration, Cutaneous
Animals
anti-inflammatory effect
Bile Acids and Salts - administration & dosage
Bile Acids and Salts - chemistry
Biological and medical sciences
Biological Availability
Biological Transport - physiology
Bones, joints and connective tissue. Antiinflammatory agents
Carrageenan - administration & dosage
Carrageenan - adverse effects
Cholates - administration & dosage
Cholates - pharmacokinetics
cyclic monoterpene
Cyclohexenes
Deoxycholic Acid - administration & dosage
Deoxycholic Acid - pharmacokinetics
diclofenac
Diclofenac - administration & dosage
Diclofenac - pharmacokinetics
Drug Compounding - methods
Drug Evaluation, Preclinical
Edema - chemically induced
Edema - metabolism
Edema - prevention & control
Hindlimb - drug effects
Injections
Irritants - adverse effects
lecithin bile-salt mixed micelle
Limonene
Male
Medical sciences
Menthol - administration & dosage
Menthol - pharmacokinetics
Micelles
Monoterpenes - administration & dosage
Monoterpenes - chemistry
Pharmacology. Drug treatments
Rats
Rats, Wistar
Skin - drug effects
Skin - physiopathology
Skin Absorption - drug effects
Terpenes - administration & dosage
Terpenes - pharmacokinetics
transdermal drug delivery
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Summary:The significant inhibitory action of diclofenac formulated in mixed micelles of lecithin with cholate or deoxycholate was observed on the rat hind paw edema induced by carrageenan. In the primary stage, mixed micelle formulation of deoxycholate was more effective compared with that of cholate. However, in the final term, the inhibitory action was similar in both formulations. In a previous study, the flux of diclofenac was greater in the mixed micelle formulation of deoxycholate compared with that of cholate. It was suggested that the permeation rate of diclofenac through skin was proportional to the pharmacological activity. The hind paw edema was quickly inhibited when cyclic monoterpene such as d-limonene or l-menthol was included in the formulations. All the micelle formulations significantly decreased the value of AUC estimated the hind paw thickness–time profile. This suggests that the micelle formulation of cholate in addition to deoxycholate showed significant anti-inflammatory activity to hind paw edema of rats. Incorporation of d-limonene or l-menthol was more effective on the decrease of AUC. A pharmacological study revealed that micelle formulations were able to reduce the skin irritation of chemicals.
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.26.1739