Objective: The objective of this study was to formulate and evaluate of the poorly soluble drug, azilsartan medoxomil into nanosuspension to increase the solubility and enhance the dissolution rate and then improve its bioavailability.Methods: Nanosuspension of azilsartan medoxomil was prepared using solvent-antisolvent precipitation method using PVP-K30 as a stabilizer. Eight formulations were prepared to show the effect of different parameters in which four formulations show the effect of stabilizer concentration, three formulations show the effect of stirring speed and two formulations prepare to show the effect of the addition of co-stabilizer such as sodium lauryl sulphate (SLS) and tween 80. All these formulation are evaluated for their particle size and entrapment efficiency. The selected one was evaluated for zeta potential, scanning electron microscope (SEM), saturation solubility, and in vitro drug release.Results: All the prepared formulations were in the nano size. The optimum concentration of the stabilizer was in the formulation when the drug: stabilizer ratio 1:1 and optimum stirring speed was 300 rpm. Dramatic effect on the particle size reduction was found by the addition of costabilizer (SLS) in formulation F3 that has P. S 157±0.0 nm. The selected formula F3 showed an enhanced dissolution profile compared to the pure drug at all-time intervals. Conclusion:The results show that the formulation that contain drug: PVP-K30: SLS in ratio 1:0.75:0.25 is the best one and can be utilized to formulate azilsartan medoxomil nanosuspension.

Nanosponges (NS) of etodolac(ETO) was prepared using the emulsion solvent diffusion method ; the effects of drug: polymer ratio, the effect of level concentration of internal phase and stirring time and other variables that effect on the physical characteristics of NS were investigated and characterized, The selected formula was lyophilized then incorporated into hydrogel ; which also evaluated .The results show that the formulation that contain Drug: PVA:EC in ratio 1:3:2 is the best with smallest particle size 40.2±0.098 with polydispersibility0.005 and in vitro release 97.6±0.11%, , ETO NS Carbopol hydrogel produced a significant(p<0.05) improvement of the in vitro release than pure ETO hydrogel.

This study designed to prepare ultrafine apixaban (APX) o/w nanoemulsion (NE) based gel with droplet size below 50 nm as a good method for transdermal APX delivery without using permeation enhancer, alternatively, the formulation components itself act as permeation enhancer. APX, a potent oral anticoagulant drug that selectively and directly inhibit coagulation factor Xa, was selected as a good candidate for transdermal delivery as it displays poor water solubility (0.028 mg/mL) and low bioavailability (50%). APX-NE gel was prepared using triacetin, triton-x-100 and carbitol as oil phase, surfactant and cosurfactant respectively, while Carbopol 940 used as a gelling agent. Ex vivo permeation of APX-NE gel through human stratum corneum reveal

Objective: The aim of the present study was to prepare a new liquid-solid tablet to enhance the dissolution and bioavailability of a poor water soluble calcium channel blocker lacidipine.Methods: Firstly, solubility study of lacidipine in different media of water-miscible non-volatile solvents as tween 20, tween 80, propylene glycol, liquid paraffin, PEG200, PEG400, and PEG600 was investigated to select the most suitable solvent. A mathematical model was applied to calculate the appropriate amount of carrier and coating material.Four liquid-solid tablets of 6 mg lacidipine were prepared by dissolving the drug in the previously chosen water miscible non-volatile solvents, then a binary mixture of the carrier (Avicel PH 102) and coating material (Aerosil 200) at a ratio of 45:1 was used in all preparation since it gave the optimal flow property. Croscarmellose and magnesium stearate were incorporated in all prepared formulas as super disintegrant and lubricant respectively. On the other hand, directly compressed lacidipine tablet of the same previous composition without the addition of any non-volatile solvent was prepared for comparism study. Both characterizations of powder mixture and post-compression tablet evaluations were done. Differential scanning calorimetry (DSC) and fourier transform infrared spectroscopy (FTIR) were investigated for the pure drug, physical mixture, and selected liquid-solid tablet to exclude any drug-excipients interaction. Results:The obtained results indicated that PEG 200 was the most suitable solvent with lacidipine solubility of 2.81 mg/ml. Flowability of all the prepared formulas was found to be within the specification limits. The liquid-solid tablet formula with PEG 200 at 10% w/w lacidipine was the most suitable one in the term of disintegration time (21±0.2 second), 100% of drug release within 10 min, and with accepted other tablet properties.DSC thermograms for both physical mixture of selected liquisolid system and its tablets illustrated the formation of lacidipine amorphous solid solution. The absence of chemical interaction between drug and other formula components was confirmed by remaining all characteristic peaks of lacidipine in all investigated FTIR spectra. Conclusion:Liquid-solid tablet was considered as a promising system to enhance solubility and dissolution rate of poor-water soluble lacidipine.

Bromocriptine mesylate is a semisynthetic ergot alkaloid derivative with a potent dopaminergic activity, used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinemia, neuroleptic malignant syndrome, and type 2 diabetes, the oral bioavailability is approximately 6%.Therefore, the aim is the preparation and evaluation of bromocriptine mesylate as a liquid self-nano emulsifying drug delivery system to enhance its solubility, dissolution and thermodynamic stability of the formulation. Solubility study was made in different vehicles to select the best one for dissolving bromocriptine mesylate. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1ratios of surfactant and co-surfactant. Four formulations were prepared, using various concentrations of castor oil, tween 80 and ethanol. All the prepared formulations were evaluated for particle size distribution, polydispersity index, drug content, thermodynamic stability, dispersibility and emulsification time, robustness to dilution and in vitro drug dissolution. It was found that, the rate and extent of release for all prepared formulations were significantly higher (p ≤ 0.05) than that in crude drug powder. From the study, it was concluded that self-Nano emulsifying drug delivery system is a promising approach to improve solubility, dissolution and stability of the formulation.