Electron Spin Resonance Evaluation of Buccal Membrane Fluidity Alterations by Sodium Caprylate and L-Menthol

The ability of sodium caprylate and l-menthol to fluidize phospholipid bilayers composed of lipids simulating the buccal epithelium was investigated using electron spin resonance (ESR) to evaluate the action of these agents as permeation enhancers. 5-Doxyl stearic acid (5-DSA) and 16-doxyl stearic acid (16-DSA) were used as spin labels to identify alterations in membrane fluidity near the polar head groups or inner acyl regions of the lipid bilayer, respectively. The molecular motion of both 5-DSA and 16-DSA showed increased disorder near the polar and inner hydrophobic regions of the bilayer in the presence of sodium caprylate suggesting fluidization in both the regions, which contributes to its permeation enhancing effects. L-menthol decreased the order parameter for 16-DSA, showing membrane fluidization only in the inner acyl regions of the bilayer, which also corresponded to its weaker permeation enhancing effects. The rapid evaluation of changes in fluidity of the bilayer in the presence of potential permeation enhancers using ESR enables improved selection of effective permeation enhancers and enhancer combinations based on their effect on membrane fluidization.

COMPLEX OF ELUXADOLINE WITH SODIUM CAPRYLATE FOR IMPROVED SOLUBILITY AND DISSOLUTION RATE

In the present research, newly developed complex with sodium caprylate was investigated for solubility and dissolution enhancement of eluxadoline. Complexes were prepared in different ratios by solvent evaporation method and characterised solubility study, Infrared spectroscopy (IR), Diffrential scanning calorimetry (DSC), X-Ray Diffraction (XRD), drug content analysis and in vitro Drug release. The solubility and dissolution rate revealed most suitable ratio of eluxadoline and sodium caprylate (1:4). The IR, DSC and X-RD data also confirmed the results. It was concluded that complex prepared with (1:4 drug:sodium caprylate ratio) using solvent evaporation method showed significant improvement in solubility and drug dissolution.

Sodium caprylate improved intestinal mucosa barrier function and antioxidant capacity by altering gut microbial metabolism

Short-chain fatty acids (SCFAs) produced by gut microbial metabolisms have been proven to regulate intestinal health by activating G protein-coupled receptors (GPRs). There has been unclear if medium-chain fatty acids...

Formulation and development of fast dissolving oral film of a poorly soluble drug, frusemide with improved drug loading using mixed solvency concept and its evaluation

The aim of the present research work is to explore the application of mixed solvency concept to formulate and develop a fast dissolving oral film of furosemide with improved drug loading. In the present study, poorly soluble drug, furosemide was tried to be solubilized by employing the combination of physiologically compatible water-soluble additives (solubilizers) to formulate its fast dissolving formulations. For the development of fast dissolving oral film, firstly, different film forming polymers were tested for their film properties. The second fast dissolving layer was also formed and optimized. Solubility studies were conducted to select water-soluble additives for formulation of fast dissolving drug layer. Keeping the total concentration less than 40 % w/v of mixed blends, different aqueous blends were prepared employing solubilizers from among sodium benzoate, sodium acetate, sodium citrate, urea, niacinamide, glycerin, propylene glycol, polyethylene glycol 200, polyethylene glycol 400, polyethylene glycol 600, and PVP K 30. Maximum solubility of furosemide was found in blends- F5 (10% sodium caprylate +2.5%sodium benzoate+ 2.5% niacinamide) and in blend F7 (10% sodium caprylate +2.5%sodium benzoate +2.5% sodium citrate + 2.5% niacinamide). Prepared films were evaluated for drug content, thickness, folding endurance, tensile strength and hydration ratio. Keywords: Furosemide, fast dissolving oral film, mixed solvency concept.

Efficacy of Antimicrobials Applied Individually and in Combination for Controlling Listeria monocytogenes as Surface Contaminants on Queso Fresco

ABSTRACT Outbreaks of listeriosis are continually attributed to the consumption of Hispanic-style soft cheeses contaminated with Listeria monocytogenes postpasteurization. Once contaminated, L. monocytogenes can grow rapidly in cheeses like Queso Fresco (QF) even when stored at refrigeration temperatures. Several antimicrobials, including acidified calcium sulfate with lactic acid (ACSL), ɛ-polylysine (EPL), hydrogen peroxide (HP), lauric arginate ethyl ester (LAE), and sodium caprylate (SC), have demonstrated antilisterial activity in food. The objectives of this study were to determine the efficacy of these antimicrobials used individually and in combination to control L. monocytogenes as surface contaminants on QF and to identify additive and synergistic interactions. Cheeses were surface inoculated at ∼4 log CFU/g, dipped in antimicrobial solutions, vacuum packaged, and then stored at 7°C for 35 days. L. monocytogenes counts were determined 24 h after application of the antimicrobials and then weekly throughout storage. Dip treatments in a 5% (v/v) HP solution reduced L. monocytogenes counts to <0.5 log CFU/g within 24 h with no increase in counts through day 35. Dip treatments in LAE at 2 and 5% alone and in combination with EPL at 10% produced initial reductions in pathogen counts (1.5 to 1.8 CFU/g) but did not inhibit pathogen growth compared with the sterile water control. Dip applications of ACSL at 25% also produced an initial ∼1.5-log reduction in L. monocytogenes counts followed by regrowth. Application of SC at 10% alone and in combination with either EPL or LAE inhibited growth to <1 log CFU/g through 21 days of storage. The combination of ACSL+SC worked synergistically to inhibit the growth of L. monocytogenes on QF to <1 log CFU/g through 35 days. These data indicate that HP alone and treatments containing EPL, LAE, or ACSL in combination with SC are promising postlethality treatments and process controls for L. monocytogenes on QF through a 21-day shelf life.