Evaluation of Emulgel and Nanostructured Lipid Carrier-Based Gel Formulations for Transdermal Administration of Ibuprofen: Characterization, Mechanical Properties, and Ex-Vivo Skin Permeation.

In transdermal applications of nonsteroidal anti-inflammatory drugs, the rheological and mechanical properties of the dosage form affect the performance of the drug. The aim of this study to develop emulgel and nanostructured lipid carrier NLC-based gel formulations containing ibuprofen, evaluate their mechanical properties, bioadhesive value and ex-vivo rabbit skin permeability. All formulations showed non-Newtonian pseudoplastic behavior and their viscosity values are suitable for topical application.

Development and pharmacokinetic evaluation of Neusilin® US2-based S-SNEDDS tablets for bosentan: Fasted and fed states bioavailability, IVIS® real-time biodistribution, and ex-vivo imaging.

The study reported here aimed to develop and optimize the S-SNEDDS tablet of bosentan (BOS) and to investigate its pharmacokinetic and biodistribution properties. The BOS-loaded SNEDDS have been developed and characterized in a previous study. The BOS-loaded SNEDDS formulation was converted to S-SNEDDS using Neusilin® US2.

Formulation development, optimization by Box-Behnken design, characterization, in vitro, ex-vivo, and in vivo evaluation of bosentan-loaded self-nanoemulsifying drug delivery system: A novel alternative dosage form for pulmonary arterial hypertension treatment.

This study aimed to develop and optimize a self-nanoemulsifying drug delivery system (SNEDDS) of bosentan (BOS) to solve its poor oral bioavailability due to low water solubility. A pseudo-ternary phase diagram was created based on the solubility and emulsification studies. The major components of the formulation were selected as glyceryl monolinoleate (lipid), polyoxyl 40 hydrogenated castor oil (surfactant), and caprylocaproyl polyoxyl-8 glycerides (co-surfactant).

Development and Validation of an HPLC Method Using an Experimental Design for Analysis of Amlodipine Besylate and Enalapril Maleate in a Fixed-dose Combination.

Objectives: The aim of this study was to develop and optimize a simple, cost-effective, and robust high-performance liquid chromatography (HPLC) method by taking an experimental design approach to the assay and dissolution analysis of amlodipine besylate and enalapril maleate from a fixed-dose combination tablet.

Materials And Methods: The chromatographic analysis was performed on a C18 column (4.6x250 mm id.

Evaluation of improved oral bioavailability of ritonavir nanosuspension.

The main objective of this study was to evaluate the pharmacokinetics of ritonavir (RTV) nanosuspension in rats in both fed and fasted state in comparison with coarse powder, physical mixture and commercial product (Norvir®). The point to point relation model was generated between the results of in vitro dissolution and in vivo pharmacokinetic studies. The oral RTV nanosuspension was prepared with microfluidization method.

Preparation of ritonavir nanosuspensions by microfluidization using polymeric stabilizers: I. A Design of Experiment approach.

The objective of this study was to prepare ritonavir (RTV) nanosuspensions, an anti-HIV protease inhibitor, to solve its poor water solubility issues. The microfluidization method with a pre-treatment step was used to obtain the nanosuspensions. Design of Experiment (DoE) approach was performed in order to understand the effect of the critical formulation parameters which were selected as polymer type (HPMC or PVP), RTV to polymer ratio, and number of passes.

Evaluation of the transport, in vitro metabolism and pharmacokinetics of Salvinorin A, a potent hallucinogen.

Salvinorin A is an unregulated potent hallucinogen isolated from the leaves of Salvia divinorum. It is the only known non-nitrogenous kappa-opioid selective agonist, and rivals synthetic lysergic acid diethylamide (LSD) in potency. The objective of this study was to characterize the in vitro transport, in vitro metabolism, and pharmacokinetic properties of Salvinorin A.

Ion pair-mediated transport of metoprolol across a three lipid-component PAMPA system.

Parallel Artificial Membrane Permeability Assay (PAMPA) is a method to screen drug candidates for membrane permeability. The objective was to characterize the transport of a model weak base, metoprolol, across a three lipid-component PAMPA system (denoted A-PAMPA, for anionic-PAMPA) and challenge ion pairing as a mechanism for metoprolol transport. A-PAMPA was designed to mimic the lipid composition of the enterocyte's plasma membrane and included 1,2-dioleoyl-sn-glycero-3-[phospho-l-serine] (PS18:1) as an anionic lipid-component.

Lipid composition effect on permeability across PAMPA.

The parallel artificial membrane permeability assay (PAMPA) system has promise to rapidly screen drug candidate passive permeability, but has been poorly described in terms of its lipid membrane structure and function. The objective was to investigate the role of PAMPA lipid composition on the permeability of five model compounds. PAMPA was used and employed individual phospholipids that varied in phosphate head group and acyl chain unsaturation.

Comparison of the hematological effects of a sustained release chitosan formulation of pentoxifylline with a commercial formulation.

In the present study the hematological effects of a sustained release chitosan formulation of pentoxifylline (CAS 6493-05-6) were examined and compared with those of a commercial product. The study was carried out on 12 healthy volunteers. Both formulations were tolerated well clinically.