Formulation and biopharmaceutical evaluation of a certain anti-inflammatory drug / Islam Mohamed Adel Mahmoud Hashim ; Supervised Mohamed Farid Elmeligy , Nermeen Adel Elkasabgy

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

This work aimed at improvingthe poor aqueous solubility besides the low oral bioavailability of curcuminalong withevaluatingits anti-inflammatory effect using two different drug delivery systems. A brief review was discussedabout pulmonary drug delivery via different mechanisms and devices while focusing on dry powder inhalers (DPIs).Different techniques for the production of dry powders were carefully mentioned and the pharmacokinetic profile of the inhaled particle was illustrated starting from powder dissolution and up to different elimination modes. Moving on, the benefits of curcumin as an anti-inflammatorywere studied when formulated as inhalable dry curcumin proliposomes and as curcumin topicalscaffolds forinjured skin care. As for curcumin proliposomes, they were prepared using nano-spray drying technique which proved to give sufficiently high % yield and produce free-flowing particles of uniform size distribution.Proliposomes were characterized in terms of particle size (PS), zeta potential (ZP), % entrapment efficiency (% EE), % drug content (% DC),% drug loading (% DL)andin-vitro drug releasein order to screen for the optimized formulations. The selected formulations were evaluated for their aerodynamic particle size measurements;possible ingredients interactions usingFourier transform infrared spectroscopy (FT-IR), thermal behavior usingDifferential scanning calorimetry (DSC) and their morphology using Transmission electron microscopy (TEM) and Scanning electron microscopy(SEM). Cell line studies were carried on human A549 lung carcinomacells to study their cytotoxicity profiles by MTT assay and their inhibitory effects on major proinflammatory cytokines(Tumor necrosis factor-alpha; TNF-Ü, Interleukin-6; IL-6 and Interleukin-10; IL-10).In-vivo study on male Albino rats was conducted to evaluate their pharmacokinetic profiles.The selected formulations proved superior to pure curcumin in reaching deeplung tissues and eliciting better anti-inflammatory and growth inhibitory effect on major cytokines and A549 cells, respectively. The pharmacokinetic profiles showed thatthey exceled in both the rate and extent of absorption into lung tissues as when compared to the pure drug

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