Νιοσώματα κετοκοναζόλης : παρασκευή, χαρακτηρισμός και in-vitro αξιολόγηση

• Κύριος συγγραφέας: Χαμπίμπη, Ευαγγελία
• Άλλοι συγγραφείς: Κλεπετσάνης, Παύλος
• Μορφή: Thesis
• Γλώσσα: Greek
• Έκδοση: 2019
• Θέματα: Niosomes; Ketoconazole; Drug delivery systems; Νιοσώματα; Κετοκοναζόλη; Συστήματα χορήγηση φαρμάκων

Recent research work on the field of Pharmaceutical Technology is mainly carried out on drug formulation in sustained and controlled release dosage form. Thus, a lot of carriers have been designed in order to transport the active substance and release it to the site of action. One category of such carriers is niosomes. Niosomes are a closed bilayer vesicular structures formed by self-assembled non-ionic surfactants in the aqueous phase with or without the incorporation of cholesterol as a stabilizer. Niosomes are chemically stable to oxidative degradation thus they can be an effective drug delivery system with the ability to load both hydrophilic and lipophilic drugs. Ketoconazole is a broad spectrum antifungal agent active against a wide variety of fungi and yeasts. It is readily but incompletely absorbed after oral dosing. Topically it is used in the treatment of infections of the skin, mainly caused by candida. The encapsulation of ketoconazole in niosomes may increase the half-life providing prolonged drug delivery and minimize the commonly occurring side effects. The goal of this study was the development and characterization of a promising formulation of ketoconazole. The effect of surfactant and cholesterol concentration in the formulation of ketoconazole loaded niosomes was studied by employing 32 full factorial design. A reliable model for the desired responses as for the vesicle size, the entrapment efficiency and the drug release was optimized and validated. Ketoconazole loaded niosomes were prepared using thin film hydration method by varying the ratio of surrfactant and cholesterol. It was found that the best surfactant for our experiment was Span 60. Afterwards, the prepared niosomes were evaluated for vesicle size, entrapment efficiency, cumulative drug release and zeta potential. The release kinetics was studied and it was found that it follows Korsmeyer-Peppas kinetics with fickian diffusion controlled mechanism. Stability studies were also performed at 4οC±2oC for 3 months. Finally, equations were developed that correlate each response with the surfactant and cholesterol concentration and according to these, an optimized formulation was developed, which was studied and evaluated as for the responses mentioned above, showing that the developed model is reliable as no significant differences were observed between the theoretical and experimental values.