Diacerein solid dispersion loaded tablets for minimization of drug adverse effects: statistical design, formulation, , and evaluation.

Diacerein is a BCS class II drug employed in osteoarthritis management. The acid/base hydrolysis of the unabsorbed diacerein in the colon is responsible for its laxative effect. Therefore, this work aimed to enhance the solubility, dissolution, and oral bioavailability of diacerein.

Formulation of sustained release bioadhesive minitablets containing solid dispersion of levofloxacin for once daily ocular use.

This study aimed to increase ocular residence time of levofloxacin by formulation into zero-order sustained release mucoadhesive minitablets for once daily administration using a hydrophobic-hydrophilic polymeric matrix. Levofloxacin was first formulated into solid dispersion with different ratios of Eudragit RS then the resulting solid dispersion was mixed with different concentrations of Carbopol and other excipients to be finally compressed into minitablets. A 2 full factorial design was employed to estimate the effects and interactions of two formulation factors, and to establish their relationships with selected responses in the developed minitablets.

Solid Form of Lipid-Based Self-Nanoemulsifying Drug Delivery Systems for Minimization of Diacerein Adverse Effects: Development and Bioequivalence Evaluation in Albino Rabbits.

This work aimed to enhance the oral bioavailability of diacerein. The drug was incorporated in self-nanoemulsifying drug delivery system. Ternary phase diagrams were constructed using Capryol™90, Miglyol®812 and isopropyl myristate as oils, Tween®80 and Tween®20 as surfactants and PEG 200 and PEG 300 as co-surfactants.

Effects of different combinations of nanocrystallization technologies on avanafil nanoparticles: in vitro, in vivo and stability evaluation.

The study investigated the effects of different combined top-down and bottom-up nanocrystallization technologies on particle size and solid state of avanafil nanoparticles. Combined antisolvent precipitation-ultrasonication (sonoprecipitation) technique was adopted to prepare 18 formulas according to 3.2 factorial design using 3 stabilizers; Tween 80, polyvinyl alcohol (PVA) and Pluronic F68 at different concentrations with different cryoprotectants.

Formulation of avanafil in a solid self-nanoemulsifying drug delivery system for enhanced oral delivery.

Avanafil was incorporated into solid self-nanoemulsifying systems with the aim of improving its oral bioavailability. Labrafil, Labrafac, and Miglyol 812 N were investigated as oils, Tween 80 and Cremophor EL as surfactants, and Transcutol HP as a co-surfactant. Nine formulations produced clear solutions of 13.

Effect of different polymers on avanafil-β-cyclodextrin inclusion complex: in vitro and in vivo evaluation.

In this study, we examined the effect of different polymers on the chemical, physical and pharmacokinetic properties of avanafil-β-cyclodextrin (β-CD) inclusion complex. Equimolar mixtures of drug and β-CD were used to prepare 25 ternary drug-β-CD-polymer inclusion complexes using five different polymers, polyethylene glycol (PEG 4000), polyvinyl pyrrolidone (PVP K-30), chitosan, hydroxypropylmethyl cellulose, and hydroxyethyl cellulose, each in five different concentrations, 1, 3, 5, 7, and 10% (w/w). The addition of 10% (w/w) PEG 4000 resulted in a significant decrease of drug solubility, where the infrared spectra and differential scanning thermograms revealed an interaction between PEG 4000 and avanafil which hindered drug inclusion.

Formulation of venlafaxine for once daily administration using polymeric material hybrids.

Objective: Controlled release venlafaxine for once daily administration.

Methods: Drug resin complexation followed by polymer encapsulation. A 4(1).

Localized rosuvastatin via implantable bioerodible sponge and its potential role in augmenting bone healing and regeneration.

Objective: Statins proved potential bone healing properties. Rosuvastatin is a synthetic, hydrophilic, potent and highly efficacious statin. In the current work, an attempt was investigated to develop, evaluate various bioerodible composite sponges enclosing rosuvastatin and explore their potential in augmenting bone healing and regeneration.

Effervescent tablet formulation for enhanced patient compliance and the therapeutic effect of risperidone.

Risperidone is a poorly water soluble atypical antipsychotic drug. This work investigated the potential of developing risperidone effervescent tablets to facilitate drug administration and mask drug taste. The solid dispersion technique was selected to improve drug solubility due to its ease of scaling up, reproducibility and affordable cost.

In vitro and in vivo evaluation of indomethacin nanoemulsion as a transdermal delivery system.

Nanoemulsions were investigated as transdermal delivery systems for indomethacin. Six formulae were prepared using Triacetin, capryol 90 and labrafil as oils; Tween 80 and pluronic F127 as surfactants and transcutol and propylene glycol as co-surfactants. The continuous phase was that one with the larger volume fraction regardless of the hydrophile-lipophile balance of the surfactant/co-surfactant mixture.

Fast-dissolving sublingual films of terbutaline sulfate: formulation and in vitro/in vivo evaluation.

Terbutaline sulfate fast dissolving sublingual films were prepared using seven drug compatible film formers in different combinations and proportions. The film polymers are maltodextrin, Na alginate, Carpabol 430, xanthan gum, HPMC E5, PVP K-25, and Na CMC. Propylene glycol and sorbitol were used as plasticizers and mannitol as filler.

Microemulsions as vehicles for topical administration of voriconazole: formulation and in vitro evaluation.

This work was undertaken to investigate microemulsion (ME) as a topical delivery system for the poorly water-soluble voriconazole. Different ME components were selected for the preparation of plain ME systems with suitable rheological properties for topical use. Two permeation enhancers were incorporated, namely sodium deoxycholate or oleic acid.

Enhancement of the intranasal delivery of insulin via a novel mucoadhesive Carbopol gel.

Objectives: The objectives of this study were to develop an intranasal insulin gel using Carbopol homogenization rather than neutralization and to examine the effectiveness of the gel compared with a subcutaneous injection.

Methods: Four factors, namely the molecular weight of polyethylene glycol (PEG), the concentration of Carbopol, the temperature of preparation and the type of absorption enhancer, were evaluated for their effect on viscosity and in-vitro insulin release. Bioavailability of insulin from selected formulations was compared with an intranasal solution and subcutaneous injection in rabbits.

Mucoadhesive nanoparticles as carrier systems for prolonged ocular delivery of gatifloxacin/prednisolone bitherapy.

A fluoroquinolone/glucocorticoid combination for the treatment of bacterial keratitis in the form of mucoadhesive nanoparticle suspensions was developed to prolong the release and improve patient compliance. Gatifloxacin/prednisolone loaded nanoparticles were prepared using Eudragit RS 100 and RL 100 and coated with the bioadhesive polymer, hyaluronic acid. FT-IR and DSC studies revealed no interaction between gatifloxacin and prednisolone.

Valsartan orodispersible tablets: formulation, in vitro/in vivo characterization.

Valsartan orodispersible tablets have been developed at 40-mg dose, with the intention of facilitating administration to patients experiencing problems with swallowing and hopefully, improving its poor oral bioavailability. Work started with selecting drug compatible excipients depending on differential scanning calorimetric analysis. A 3(3) full factorial design was adopted for the optimization of the tablets prepared by freeze-drying technique.