Effect of talc and vitamin E TPGS on manufacturability, stability and release properties of trilaurin-based formulations for hot-melt coating.

This study was focused on one particular case of hot-melt coating with trilaurin - a solid medium-chain monoacid triglyceride. The challenge of using trilaurin as coating agent in melting-based processes is linked to its relatively low melting profile: 15.6 °C (T), 35.

Evaluation of the Antimicrobial Activity of a Formulation Containing Ascorbic Acid and Eudragit FS 30D Microparticles for the Controlled Release of a Curcumin-Boric Acid Solid Dispersion in Turkey Poults Infected with : A Therapeutic Model.

The selection of components within a formulation or for treatment must stop being arbitrary and must be focused on scientific evidence that supports the inclusion of each one. Therefore, the objective of the present study was to obtain a formulation based on ascorbic acid (AA) and Eudragit FS 30D microparticles containing curcumin-boric acid (CUR-BA) considering interaction studies between the active components carried out via Fourier transform infrared spectrometry (FTIR) and differential scanning calorimetry (DSC) to minimize antagonistic effects, and comprehensively and effectively treat turkey poults infected with (). The DSC and FTIR studies clearly demonstrated the interactions between AA, BA, and CUR.

Development and Stability of a New Formulation of Pentobarbital Suppositories for Paediatric Procedural Sedation.

Pentobarbital is a drug of choice to limit motion in children during paediatric procedural sedations (PPSs). However, despite the rectal route being preferred for infants and children, no pentobarbital suppositories are marketed, and therefore they must be prepared by compounding pharmacies. In this study, two suppository formulations of 30, 40, 50, and 60 mg of pentobarbital sodium were developed using hard-fat Witepsol W25 either alone (formulation F1) or with oleic acid (formulation F2).

Characterization, dissolution, and pharmacokinetics of different batches of efavirenz raw materials.

Objective: To perform the solid-state characterization and the - correlation (IVIVC) of three batches of efavirenz (EFV) active pharmaceutical ingredients.

Significance: EFV is an effective anti-HIV drug. Due to the poor aqueous solubility, the rate and extent of EFV absorption deeply depend on its dissolution characteristics.

Organogel Nanoparticles as a New Way to Improve Oral Bioavailability of Poorly Soluble Compounds.

Purpose: The aim of the study was to evaluate organogel nanoparticles as a lipophilic vehicle to increase the oral bioavailability of poorly soluble compounds. Efavirenz (EFV), a Biopharmaceutical Classification System (BCS) Class II, was used as drug model.

Methods: Organogel nanoparticles loaded with EFV were formulated with sunflower oil, 12-hydroxystearic acid (HSA) and polyvinyl alcohol (PVA).

Evaluation of a -Based Direct-Fed Microbial on Aflatoxin B1 Toxic Effects, Performance, Immunologic Status, and Serum Biochemical Parameters in Broiler Chickens.

The aim of the present study was to evaluate the effect of a commercial direct-fed microbial (DFM) on aflatoxin B1 toxic effects, performance, and biochemical and immunologic parameters in broiler chickens. Ninety 1-day-old Cobb 500 male broiler chicks were raised in floor pens for a period of 21 days. Chicks were neck-tagged, individually weighed, and randomly allocated to one of three groups: Negative control (basal feed), aflatoxin B1 (basal feed + 2 ppm AFB1), and DFM (basal feed + 2 ppm AFB1 + direct-fed microbial).

Evaluation of Cellulosic Polymers and Curcumin to Reduce Aflatoxin B1 Toxic Effects on Performance, Biochemical, and Immunological Parameters of Broiler Chickens.

To evaluate the effect of cellulosic polymers (CEL) and curcumin (CUR) on aflatoxin B1 (AFB1) toxic effects on performance, and the biochemical and immunological parameters in broiler chickens, 150 one-day-old male broiler chicks were randomly allocated into five groups with three replicates of 10 chickens per pen: Negative Control (feed); AFB1 (feed + 2 ppm AFB1); CUR (feed + 2 ppm AFB1 + Curcumin 0.2%); CEL (feed + 2 ppm AFB1 + 0.3% Cellulosic polymers); and, CEL + CUR (feed + 2 ppm AFB1 + 0.

Retrograded starch/pectin coated gellan gum-microparticles for oral administration of insulin: A technological platform for protection against enzymatic degradation and improvement of intestinal permeability.

Gellan gum microparticles coated with colon-specific films based on retrograded starch and pectin was developed for enhancing the oral release of insulin (INS). The system developed promoted an impressive protection of INS (80%) after 120 min of incubation with trypsin and alpha-chymotrypsin, while only 3% of free INS remained intact after the same time, possibility due to the calcium chelating activity of the polymers in inhibiting the proteolytic activity. In vitro INS release in media simulating the gastrointestinal portions revealed a pH-dependent behavior, as well as the significance of the coating in lowering the release rates in relation to their counterparts.

Evaluation of Chitosan and Cellulosic Polymers as Binding Adsorbent Materials to Prevent Aflatoxin B1, Fumonisin B1, Ochratoxin, Trichothecene, Deoxynivalenol, and Zearalenone Mycotoxicoses Through an In Vitro Gastrointestinal Model for Poultry.

Mycotoxins are secondary toxic metabolites that are produced by fungi representing threats to human and animal health. The objective of this study was to evaluate the adsorption capacity of Chitosan (CHI), and three cellulosic polymers (HPMC, CMC, and MCC), on six mycotoxins (AFB₁; FUB₁; OTA; T-2; DON; and, ZEA) using an in vitro digestive model for poultry. The adsorbent capacity of the materials in the supernatant of each compartment was evaluated by a non-competitive chemiluminescent assay.

Atomization of denatured whey proteins as a novel and simple way to improve oral drug delivery system properties.

In the sphere of drug delivery, denatured whey protein (DWP) has in recent times gained press. However, to date, no scalable and affordable dosage form has been developed. The objective of our study was to evaluate the potential use of spray-dried DWP as a ready to use excipient for oral drug delivery.

Molecular and biopharmaceutical investigation of alginate-inulin synbiotic coencapsulation of probiotic to target the colon.

Colon targeting, as a site-specific delivery for oral formulation, remains a major challenge, especially for sensitive bioactive components such as therapeutic forms of phages, live attenuated virus and prebiotics-probiotics association. Synbiotics could be used to protect encapsulated probiotics during the gastrointestinal tract and control their release in the colon. To achieve these goals, effective prebiotics, such as inulin, could be combined with alginate - the most exploited polymer used for probiotic encapsulation - in the form of beads.

Denatured Whey Protein Powder as a New Matrix Excipient: Design and Evaluation of Mucoadhesive Tablets for Sustained Drug Release Applications.

Purpose: In earlier study, we proposed denatured whey protein (DWP) powder obtained by atomization as a new excipient to promote oral drug delivery. In this work, we evaluate the possibility to formulate tablets based on DWP powders and to characterize their role as a matrix mucoadhesive excipient.

Methods: Tablets containing increased amount of DWP (10 to 30%) were produced by direct compression after mixing with theophylline, microcrystalline cellulose, Aerosil® and magnesium stearate.

A prebiotic matrix for encapsulation of probiotics: physicochemical and microbiological study.

This work aims to develop an encapsulated oral-synbiotic supplement by studying the effect of adding inulin in alginate beads and observing its ability to protect three probiotic strains: Pediocucus acidilactici, Lactobacillus reuteri and Lactobacillus salivarius. Beads of different inulin concentrations 0%, 5%, 10%, 15% and 20% (w/v) in 2% (w/v) alginate solution were prepared by the extrusion/ionotropic gelation method. Polymer distribution within beads was characterised using confocal laser scanning microscopy.

Development and validation of a new dynamic computer-controlled model of the human stomach and small intestine.

For ethical, regulatory, and economic reasons, in vitro human digestion models are increasingly used as an alternative to in vivo assays. This study aims to present the new Engineered Stomach and small INtestine (ESIN) model and its validation for pharmaceutical applications. This dynamic computer-controlled system reproduces, according to in vivo data, the complex physiology of the human stomach and small intestine, including pH, transit times, chyme mixing, digestive secretions, and passive absorption of digestion products.

Whey protein mucoadhesive properties for oral drug delivery: Mucin-whey protein interaction and mucoadhesive bond strength.

Whey protein is a natural polymer recently used as an excipient in buccoadhesive tablets but its mucoadhesive properties were barely studied. In this work, we characterize mucoadhesion of whey protein in order to determine the mechanisms and optimal conditions for use as excipient in oral drug delivery. Thus, native and denatured whey protein (NWP and DWP) were investigated and the effect of concentration and pH were also studied.

Food protein-based microspheres for increased uptake of vitamin D3.

To protect vitamin D3 during cold storage and exposure to UV-light, vitamin D3 has been entrapped in microspheres formed by bovine protein β-lactoglobulin (βlg) and lysozyme (Lyso) from egg white. The behaviour of the βlg/Lyso microspheres in simulated intestinal fluid and their impact on the kinetic release of D3 were determined. The impact of the D3-loaded βlg/Lyso microspheres on the bioavailability of D3 was evaluated in vivo by force-feeding rats.

Self-assembly of β-lactoglobulin and egg white lysozyme as a potential carrier for nutraceuticals.

Self-assembly structures of β-lactoglobulin (βlg) and egg protein lysozyme (Lyso) were developed, using electrostatic interactions between the two oppositely charged proteins. Different βlg/Lyso concentration ratios were essayed at pH 6.8 to select the optimal ratio for the proteins co-precipitation, which behaviour was then studied at varying pH values.

Improved bioavailability of vitamin D3 using a β-lactoglobulin-based coagulum.

Vitamin D3 (D3) was encapsulated within a water-soluble matrix, formed by promoting the βlg/D3 complex by acidification. The capacity of the βlg-based coagulum to increase the long term stability of D3 in cold storage, upon exposure to intensive UV-light, and in the presence and absence of intestinal proteases, was evaluated. Additionally, the impact of the sequestration of D3 within the matrix of βlg-based coagulum on its bioavailability was determined in vivo with force-fed rats.

Micelle dynamic simulation and physicochemical characterization of biorelevant media to reflect gastrointestinal environment in fasted and fed states.

The characterization of biorelevant media simulating the upper part of the gastrointestinal tract in the fasted and fed states was investigated by classical determination of physicochemical parameters such as pH, osmolality, surface tension and results were compared to in vivo physiological data. Incorporation of fatty material, in order to better simulate the influence of high fat meal was also performed. Stability and characterization of this medium was studied and compared to classical FeSSIF.

Development of a novel drug delivery system: chitosan nanoparticles entrapped in alginate microparticles.

A novel carrier using chitosan nanoparticles entrapped into alginate microparticles is proposed for protecting molecules of interest from degradation in the digestive tract. The effects of polymer concentration, sonication, stirring, pH, and processing conditions on the physical characteristics of the carrier were studied. FITC and RBITC were used to localise the polymers within particles using CLSM.

Increased stability and protease resistance of the β-lactoglobulin/vitamin D3 complex.

The stability of the β-lactoglobulin (βlg)/vitamin D3 (D3) complex at 4°C and upon exposure to UV-C light, and in simulated intestinal fluid, were studied in vitro. Caco-2 cells were used to demonstrate the passage of the βlg/D3 complex across the monolayers. Furthermore, an in vivo experiment was conducted by force-feeding rats with the free D3 and βlg/D3 complex, with subsequent determination of the plasma concentration of 25-hydroxy-D3.

Whey protein and alginate hydrogel microparticles for insulin intestinal absorption: evaluation of permeability enhancement properties on Caco-2 cells.

The evaluation of encapsulated insulin intestinal absorption enhancement was investigated by in vitro methods. Insulin-loaded microparticles (INS-MP) made of whey protein (WP) and alginate (ALG) were prepared by a cold gelation technique. Effect of INS encapsulation toward trypsin and chymotrypsin degradation was performed.

Efficacy of mucoadhesive hydrogel microparticles of whey protein and alginate for oral insulin delivery.

Purpose: To evaluate the efficacy of mucoadhesive insulin-loaded whey protein (WP) /alginate (ALG) microparticles (MP) for oral insulin administration.

Methods: Insulin-loaded microparticles (ins-MP) made of whey protein and alginate were prepared by a cold gelation technique and an adsorption method, without adjunction of organic solvent in order to develop a biocompatible vehicle for oral administration of insulin. In vitro characterization, evaluations of ins-MP in excised intestinal tissues and hypoglycaemic effects after intestinal administration in healthy rats were performed

Results: The release properties and swelling behaviors, investigated in different pH buffers, demonstrated a release based on diffusion mechanism following matrix swelling.

Development and in vitro characterization of insulin loaded whey protein and alginate microparticles.

Insulin was encapsulated into microparticles (MP) made of denaturized whey proteins (WP) and alginate (ALG) using an extrusion/cold gelation process with calcium ions. High encapsulation efficiency of 85% was obtained. Influence of insulin on polymeric viscosity and on microparticle behavior was evaluated.