Anti-inflammatory and analgesic activities of Tunisian Citrullus colocynthis Schrad. immature fruit and seed organic extracts.

BACKGROUND AND OBJECTIVES: Inflammations and immune-related diseases including rheumatoid arthritis are widespread in the entire globe. The treatment of these illnesses is mainly based on the use of synthetic and biotechnological drugs, in recent years. Tunisian traditional medicine is a potential source of new remedies namely Citrullus colocynthis Schrad. (Cucurbitaceae): endemic in southern Tunisia and used in folk medicine to treat many inflammation disorders. Our goal was to assess the in vivo analgesic and anti-inflammatory activities of Tunisian Citrullus colocynthis immature fruit and seed organic extracts (petroleum ether, chloroform, ethyl acetate, acetone and finely methanol extract). MATERIAL AND METHODS: Yields of prepared organic extracts are gravimetrically determined. For the analgesic and anti-inflammatory activities, we have used respectively, the acetic acid writhing test in mice and the carrageenan-induced paw edema assay in rats. RESULTS AND DISCUSSION: All extracts displayed an important analgesic and anti-inflammatory activities at different doses without inducing any side effects. This study has demonstrated the analgesic and anti-inflammatory activities of Citrullus colocynthis immature fruit and seed extracts. Experiment results provide scientific insight into the ancient practice of utilizing Citrullus colocynthis Schrad. as analgesic and as anti-inflammatory agents.

Influence of drug concentration on the diffusion parameters of caffeine.

BACKGROUND AND OBJECTIVES: In the fields of the pharmaceutical and cosmetic industries and in toxicology, the study of the skin penetration of molecules is very interesting. Various studies have considered the impact of different physicochemical drug characteristics, skin thickness, and formulations, on the transition from the surface of the skin to the underlying tissues or to the systemic circulation; however, the influence of drug concentration on the permeation flux of molecules has rarely been raised. Our study aims to discover the influence of caffeine concentration in a formulation on the percutaneous penetration from gels, as a result of different dose applications to polysulfate membrane and human skin. MATERIALS AND METHODS: For this purpose, three identical base gels were used at 1, 3, and 5% of caffeine, to evaluate the effect of the concentration of caffeine on in vitro release through the synthetic membrane and ex vivo permeation through the human skin, using diffusion Franz(TM) cells. RESULTS: The diffusion through the epidermal tissue was significantly slower than through the synthetic membrane, which recorded an increase of flux with an increase in the concentration of caffeine. The skin permeation study showed that diffusion depended not only on the concentration, but also on the deposited amount of gel. Nevertheless, for the same amount of caffeine applied, the flux was more significant from the less concentrated gel. CONCLUSION: Among all the different concentrations of caffeine examined, 1% gel of caffeine applied at 5 mg / cm(2) showed the highest absorption characteristics across human skin.

Concentration of temarotene (Ro 15-0778) and its metabolite Ro 14-6113 in plasma and skin of hairless rat.

The aim of this preliminary report was to measure plasma and skin concentrations of Ro 15-0778 and its phenolic metabolite Ro 14-6113 in hairless rats receiving orally 10 mg/kg of Temarotene once daily during 10 days. Blood (2-3 ml) and skin (200-300 mg) samples were taken at different time points between 0.5 and 240 h after the last dose. We used a highly sensitive HPLC method for simultaneous determination of the two compounds with a quantification limit of 2 ng/ml in plasma and 10 ng/g in total skin (epidermis and dermis). After 10 h, plasma concentrations of Ro 14-6113 were 5-13 times higher than for Ro 15-0778. Ro 14-6113 concentrations in the skin were 4-10 times higher than for Ro 15-0778 within the initial 48 h. The concentrations of both compounds in the skin were higher than concentrations in plasma.