Solubility enhancement of a poorly water soluble drug / Mohamed Ahmed Naseef Soliman ; Supervised Samia Abdelkader Nour , Howida Kamal Ibrahim

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

The aim of this work was to improve the poor water solubility of diacerein via drug inclusion into self-nanoemulsifying granules, and drug inclusion into solid dispersions to be compressed into tablets to increase drug efficacy and patient compliance. The current work was to prepare 12 systems consisting of the following oils (Capryol 90, isopropyl myristate IPM and Miglyol), surfactants (Tween 80 and Tween 20) and cosurfactants (PEG 200 and PEG 300). Ternary phase diagrams were constructed using the water dilution method. Only 5 systems showed visual clarity on dilution, namely; systems I, III, IV, V and VI. Seventeen formulae out of 432 combinations tried were prepared and used for further investigations. Diacerein showed higher solubilities in Miglyol-based nanoemulsions (F9 and F10) compared to other oils. DSC, PXRD and SEM of the SNEG indicated that drug was molecularly dispersed within the formulae. FTIR of SNEG indicated the absence of an interaction between diacerein and Aeroperl 300. All SNEG formulae showed higher DE(0-30), Q5 and DR5 and lower MDT than diacerein powder. Formula SNEG3 composed of 10% Miglyol 812, 70% Tween 80 and 20% PEG 200 adsorbed to Aeroperl 300 with a ratio of 2:1 preconcentrate: carrier had the highest desirability value based on saturation solubility in water, Q5, D.E.(0-30), DR₅, MDT and Carr{u2019}s index. A 4¹x3¹x2¹ full factorial design was adopted to prepare 24 formulae using pluronic® F68, pluronic® F127, Gelucire® 50/13 and trehalose as carriers at drug to carrier ratios of 1:3,1:5 and 1:10, by solvent evaporation techniques

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