Formulation of nanocarrier systems for improvement of bioavailability of a certain anti-gout drug / Hala Nehad Hassan Ali Elshagea ; Supervised Emad B. Basalious , Rania Hassan Fahmy , Nermeen Adel Ahmed Elkasabgy

Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutics

Febuxostat suffers from relatively low bioavailability owing to the poor drug solubility and hepatic {uFB01}rst-pass effect. This study aimed to prepare highly drug-loaded self-nanoemulsifying self-nanosuspension (SNESNS) drug delivery systems. SNESNS were designed to improve febuxostat{u2019}s oral bioavailability by enhancing its solubility and lymphatic uptake. Different oil and surfactant/co-surfactant mixtures were used for the preparation of SNESNS. The prepared SNESNS were estimated for their particle size, in vitro drug release and transmission electron microscopy (TEM). Results revealed that the oil mixture of Capryol{u2122} 90: Miglyol® 812 (1:1 w/w) with surfactant/co-surfactant mixture of Cremophor® RH 40/Transcutol® HP loaded with drug in 4-fold greater concentration than its saturated solubility, resulted in the formation of SNESNS by dilution under the effect of magnetic stirring. SNESNS were freeze-dried using trehalose as a cryoprotectant.TEM images and the bimodal particle size curve con{uFB01}rmed the formation of the biphasic nanosystems after dilution (nanoemulsion and nanosuspension). Freeze-dried SNESNS were then prepared and filled in enteric coated hard gelatin capsules to avoid drug release in the acidic pH and hence the release of the free form of the drug before reaching the intestinal Peyer{u2019}s patches.Higher Cmax and AUC0{u2013}48 values compared to those of the market product Feburic® tablets con{uFB01}rmed the success of the SNESNS as a promising carrier for drugs suffering from poor water solubility like febuxostat

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