Poly(2-ethyl-2-oxazoline) (PEOX), a biocompatible polymer considered as pseudopolypeptide, was introduced as a potential alternative to the commonly used polymer, poly(vinylpyrrolidone) (PVP) for the preparation of solid dispersion with a poorly soluble drug. Glipizide (GPZ), a Biopharmaceutical Classification System class II model drug, was selected for solubility and dissolution rate study. GPZ-polymer solid dispersions and physical mixtures were characterized and investigated by X-ray diffractometry, differential scanning calorimetry, scanning electron microscopy, and FTIR spectroscopy. The impact of polymers on crystal nucleation kinetics was studied, and PEOX exhibited strong inhibitory effect compared with PVP. Solubility and dissolution behavior of the prepared solid dispersions and their physical blends were in vitro examined and evaluated. A significant enhancement in GPZ solubility was obtained with PEOX compared with the pure drug and solid dispersion with PVP. A big improvement in the intrinsic dissolution rate (45 times) and dissolved amount of GPZ (58 times) was achieved with PEOX in fasted state simulated intestinal fluid, against comparable enhancement observed with PEOX and PVP in phosphate buffer at pH 6.8. Lower molecular weight of PEOX-5K (5000 g/mol) was found to be superior to higher molecular weight PEOX-50K (50,000 g/mol) in the improvement of dissolution behavior. The findings of this study with GPZ as a model drug introduce lower molecular weight PEOX as a promising polymeric carrier toward better oral bioavailability of poorly soluble drugs.

A new cocrystal of Norfloxacin, a poorly soluble fluoroquinolone antibiotic, has been synthetized by a solvent-mediated transformation experiment in toluene, using resorcinol as a coformer. The new cocrystal exists in both anhydrous and monohydrate forms with the same (1:1) Norfloxacin/resorcinol stoichiometry. The solubility of Norfloxacin and the hydrated cocrystal were determined by the shake-flask method. While Norfloxacin has a solubility of 0.32 ± 0.02 mg/mL, the cocrystal has a solubility of 2.64 ± 0.39 mg/mL, approximately 10-fold higher. The dissolution rate was tested at four biorelevant pH levels of the gastrointestinal tract: 2.0, 4.0, 5.5, and 7.4. In a first set of comparative tests, the dissolution rate of Norfloxacin and the cocrystal was determined separately at each pH value. Both solid forms showed the highest dissolution rate at pH 2.0, where Norfloxacin is totally protonated. Then, the dissolution rate decreases as pH increases. In a second set of experiments, the dissolution of the cocrystal was evaluated by a unique dissolution test, in which the pH dynamically changed from 2.0 to 7.4, stepping 30 min at each of the four biorelevant pH values. Results were quite different in this case, since dissolution at pH 2 affects the behavior of Norfloxacin at the rest of the pH values.

Nisin/polyanion Layer-by-Layer (LbL) films are reported to exhibit different mechanisms in antimicrobial efficacy depending on the type of polyanion. LbL films consisting of nisin as the polycationic component were prepared using two different polyanionic constituents: poly acrylic acid (PAA) and dextran sulfate (DX). Due to the weaker interaction strength of carboxylate groups with nisin compared to sulfate/nisin, a larger molecular weight of PAA was needed to achieve LbL assembly. PAA-100K/nisin and DX-15K/nisin multilayer films exhibited significantly different properties. PAA–nisin films grew faster compared to DX–nisin films and showed, for 60 bilayer films, an average bilayer thickness of 21.6 nm compared to that of 6.1 nm in DX–nisin films. The total amount of nisin was found to be 17.1 ± 2.2 μg cm⁻² in (PAA–nisin)₆₀ and 6.8 ± 0.4 μg cm⁻² in (DX–nisin)₆₀ films. The stability of the films was investigated at three different pH values of 6.0, 7.4 and 9.5. (PAA–nisin)₆₀ films exhibited the release of nisin into the solution which resulted in the disintegration of the film over several hours. A burst release was observed in the first hour followed by a slower release and disintegration over 24 hours with a complete release at pH 9.5. The bacterial growth inhibition test against Staphylococcus epidermidis confirmed the antimicrobial activity of nisin released from PAA–nisin films. PAA was found to stabilize nisin and the film-released nisin retained its antimicrobial activity in the neutral and alkaline pH values. Unlike PAA–nisin films, (DX–nisin)₆₀ films were stable at the physiological conditions up to 14 days with no release of nisin. DX–nisin films were found to inhibit the attachment of Staphylococcus epidermidis and prevent biofilm formation. These results clearly demonstrate the effect of different polyanions on nisin LbL films to achieve different mechanisms in antimicrobial efficacy and show the potential of PAA–nisin multilayer films as promising local delivery systems for treatment of burns and wounds, while DX–nisin multilayer films can be employed as stable coatings against bacterial attachment and biofilm formation.

Background: Perindopril erbumine is an antihypertensive, which belongs to the category of angiotensin-converting enzyme inhibitors (ACE inhibitors) that inhibit the conversion of angiotensin I to angiotensin II. Methods: A new, selective, and sensitive spectrofluorimetric method was developed for the determination of perindopril erbumine based on the reaction with dansyl chloride in alkaline medium to give a highly fluorescent derivative which was measured at 496 nm after excitation at 340 nm in dichloromethane. The reaction conditions were studied and optimized. Results: Under the optimum conditions, the fluorescence intensity was linear over a concentration range of 1.0 to 21.0 μg/mL (R ² = 0.9997) with a detection limit of 0.242 μg/mL. In order to validate the method, the results were compared with those obtained by a high performance liquid chromatography method. Conclusions: The proposed method was successfully applied to the analysis of perindopril erbumine in pure form and tablets with good precision and accuracy as revealed by t- and F tests. The mechanism of the reaction has also been discussed.