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.

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.

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.

Liquid anti-solvent recrystallization to enhance dissolution of CRS 74, a new antiretroviral drug.

This study concerns a new compound named CRS 74 which has the property of inhibiting Human Immunodeficiency Virus (HIV) protease, an essential enzyme involved in HIV replication process. It is proved in this study that the original CRS 74 exhibits poor aqueous solubility and a very low dissolution rate, which can influence its bioavailability and clinical response. In an attempt to improve the dissolution rate, CRS 74 was recrystallized by liquid anti-solvent (LAS) crystallization.

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.

Development and characterization of coated-microparticles based on whey protein/alginate using the Encapsulator device.

The aim of this study is to prepare whey protein (WP)-based microparticles (MP) using the Encapsulator(®) device. The viscosity dependence of the extrusion device required to mix WP with a food-grade and less viscous polymer. Mixed WP/ALG MP were obtained with the optimized WP/alginate (ALG) ratio (62/38).

Enteric polymers as acidifiers for the pH-independent sustained delivery of a weakly basic drug salt from coated pellets.

Weakly basic drugs and their salts exhibit a decrease in aqueous solubility at higher pH, which can result in pH-dependent or even incomplete release of these drugs from extended release formulations. The objective of this study was to evaluate strategies to set-off the very strong pH-dependent solubility (solubility: 80 mg/ml at pH 2 and 0.02 mg/ml at pH 7.

Selection of the most suitable dissolution method for an extended release formulation based on IVIVC level A obtained on cynomolgus monkey.

Objective: The purpose of this study is primarily to identify the most suitable in vitro dissolution method(s) for their ability to predict the in vivo performance of extended release prototype tablet formulations designed for a new chemical entity, Biopharmaceutic Classification System class II drug, weak base, based on the data collected in cynomolgus monkey.

Materials And Methods: Different types of buffer at different pH were selected as dissolution medium resulting in a broad variety of release patterns (slow to fast). The in vivo and in vitro data were put in relation.

Coated whey protein/alginate microparticles as oral controlled delivery systems for probiotic yeast.

Viable Saccharomyces boulardii, used as a biotherapeutic agent, was encapsulated in food-grade whey protein isolate (WP) and alginate (ALG) microparticles, in order to protect and vehicle them in gastrointestinal environment. Yeast-loaded microparticles with a WP/ALG ratio of 62/38 were produced with high encapsulation efficiency (95%) using an extrusion/cold gelation method and coated with ALG or WP by a simple immersion method. Swelling, yeast survival, WP loss and yeast release in simulated gastric and intestinal fluids (SGF and SIF, pH 1.

Investigation of coated whey protein/alginate beads as sustained release dosage form in simulated gastrointestinal environment.

Aim: The biopharmaceutical behavior of new formulations based on both food-grade polymers, whey protein (WP) and alginate (ALG) was studied using different in vitro methods. The Biopharmaceutical Classification System (BCS) class I drug Theophylline was chosen as drug model.

Method: Drug release was studied (i) at pH 1.

Immunoadsorption of alloantibodies onto erythroid membrane antigens encapsulated into polymeric microparticles.

Purpose: Classical immunoadsorbents used for the removal of deleterious molecules in blood such as auto-antibodies are prepared by covalent coupling of antigens onto previously chemically activated supports. Such a chemical treatment may induce a potential toxicity which can be reduced if new immunoadsorbents are prepared by encapsulating erythrocytes-ghosts carrying antigens inside polymeric and porous microparticles.

Materials And Methods: Erythrocyte-ghosts obtained by hemolysis in hypotonic buffer were encapsulated into ethylcellulose microparticles by w/o/w emulsification.

Oral bioavailability of a low molecular weight heparin using a polymeric delivery system.

Low molecular weight heparins (LMWHs) are the standards of anticoagulant for the prevention of deep vein thrombosis (DVT) in patients undergoing arthroplasty and abdominal surgery. However, LMWHs are so far only administered by parenteral route. Thus, they are usually replaced by oral warfarin for outpatient therapy.

Anticoagulant activity of heparin following oral administration of heparin-loaded microparticles in rabbits.

Heparin-loaded microparticles, prepared according to the double emulsion method with biodegradable (PCL and PLGA) and nonbiodegradable (Eudragit RS and RL) polymers used alone or in combination, with or without gelatin, were characterized in vitro and in vivo after oral administration in rabbits. The entrapment efficiency and the release of heparin were determined by a colorimetric method with Azure II. The antifactor Xa activity of heparin released in vitro after 24 h was assessed.