Benzoic acid complexes with Eudragit E100®: New alternative antimicrobial preservatives.

Given that the use of some preservatives in cosmetics has been restricted, novel alternative preservatives are needed. The aim of this study was to characterize the physicochemical and antimicrobial properties of two polyelectrolyte complexes (EuB and EuBCl), which were developed through hot melt extrusion (HME) using benzoic acid (BA) and Eudragit E100. Based on phase diagrams and an experimental statistical design, the solubility of the acid in the polymer and the HME conditions were established.

Molecular and physical characterization of octenyl succinic anhydride-modified starches with potential applications in pharmaceutics.

Five commercially available starches modified with octenyl succinic anhydride (OSA) are characterized at a molecular, physicochemical and bulk level providing useful data for designing pharmaceutical products. The degree of substitution (DS) of the starches range from 0.017 to 0.

Effect of Roughness on the Dispersion of Dry Powders for Inhalation: a Dynamic Visualization Perspective.

Dry powder inhalers have attracted more interest over the years in every aspect related to them. Interestingly, when focusing on the effects of particle morphology of the active or carrier (excipient), it is generally regarded particle size and shape to influence drug availability of aerosolized particles. However, to date, few studies have examined the effect of texture, i.

Effect of pH and Ionic Strength on the Solubility of Quinoline: Back-to-Basics.

The interest of quinoline as a contaminant agent and as scaffold for the development of new therapeutic agent warrants to revisit the pH-solubility behavior of quinoline (Q) and quinoline derivatives (Q-derivatives) with possible salting-out effect. Q is a weak base with potential hazard upon exposure that may be occupational by inhalation or ingestion of or dermal exposure to particulates in certain industries; or simply by inhalation of cigarette smoke. In contrast, quinoline and its derivatives are useful in diverse therapeutic applications such as anticancer, antiseptic, antipyretic, antiviral, and antimalarial.

Quantifying the surface properties of enzymatically-made porous starches by using a surface energy analyzer.

The behavior of starch during processing and its performance in products is influenced by the surface energetics/structure of the constituent particles. This work investigates the effect of enzymatically-produced porous maize starch particles on their energetic surface properties using inverse gas chromatography-based surface energy analysis (SEA). Three modified maize starch samples treated with amylase (AM), glucoamylase (AMG) and cyclodextrin-glycosyltransferase (CGT), were used for the study.

TPP-dendrimer nanocarriers for siRNA delivery to the pulmonary epithelium and their dry powder and metered-dose inhaler formulations.

The regulation of genes utilizing the RNA interference (RNAi) mechanism via the delivery of synthetic siRNA has great potential in the treatment of a variety of lung diseases. However, the delivery of siRNA to the lungs is challenging due to the poor bioavailability of siRNA when delivered intraveneously, and difficulty in formulating and maintaining the activity of free siRNA when delivered directly to the lungs using inhalation devices. The use of non-viral vectors such as cationic dendrimers can help enhance the stability of siRNA and its delivery to the cell cytosol.

Stain removal effect of novel papain- and bromelain-containing gels applied to enamel.

Objectives: The aims of the study are to prepare novel stain removal gel-based formulations containing papain or bromelain and to investigate their stain removal effect when applied to enamel.

Materials And Methods: Experimental bromelain- and papain-based stain removal gels were prepared. Next, enamel/dentin tooth samples (6 × 6 mm, 4 mm in thickness) were obtained from bovine teeth, stained in coffee solution for 1 week, and measured with a digital spectrophotometer (Easyshade, Vita Zahnfabrik) for color assessment (baseline).

Powder dispersion mechanisms within a dry powder inhaler using microscale particle image velocimetry.

The goal of this work was to evaluate the ability of Particle Image Velocimetry (PIV) to visually assess dry powder dispersion within an inhaler. Herein, the study reports particle movement characterization of entrained low-micron particles within an inhaler to further scheme of potential mechanisms. Carrier based DPI formulations were prepared and placed in a transparent model Rotahaler chamber for the aerosolization experiments.

Nanomechanical testing technique for millimeter-sized and smaller molecular crystals.

Large crystals are used as a control for the development of a mounting and nanoindentation testing technique for millimeter-sized and smaller molecular crystals. Indentation techniques causing either only elastic or elastic-plastic deformation produce similar results in assessing elastic modulus, however, the elastic indents are susceptible to surface angle and roughness effects necessitating larger sample sizes for similar confidence bounds. Elastic-plastic indentations give the most accurate results and could be used to determine the different elastic constants for anisotropic materials by indenting different crystal faces, but not by rotating the indenter about its axis and indenting the same face in a different location.

The influence of API concentration on the roller compaction process: modeling and prediction of the post compacted ribbon, granule and tablet properties using multivariate data analysis.

Objective: While previous research has demonstrated roller compaction operating parameters strongly influence the properties of the final product, a greater emphasis might be placed on the raw material attributes of the formulation. There were two main objectives to this study. First, to assess the effects of different process variables on the properties of the obtained ribbons and downstream granules produced from the rolled compacted ribbons.

Thermal insight of mechanically activated bile acid powders.

Mechanical activation of pharmaceutical materials presents an important but poorly understood phenomenon of milled molecular crystals. In this work, a strategy was followed in an effort to understand this phenomenon, cryo-milled of both crystalline and amorphous counterpart of bile acids materials were characterized by X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). The XRPD results for the 30-min milled crystalline powders displayed a characteristic amorphous halo patterns for all compounds tested.

Determination of the scale of segregation of low dose tablets using hyperspectral imaging.

In this work, near infrared (NIR) hyperspectral imaging was used to quantify the spatial distribution of drug in tablets containing tolmetin sodium dihydrate. Hyperspectral data cubes were generated by imaging the same spatial region of a sample while illuminated by a laser at a different wavelength for each image. Images were generated for wavelengths ranging from 1100 to 2200 nm.

Assessment of milling-induced disorder of two pharmaceutical compounds.

The goal of this study was to provide a better framework for understanding the bulk and surface disorder in milled crystalline materials. The surface and bulk properties of two model compounds, ketoconazole and griseofulvin, were characterized by inverse gas chromatography as a function of cryomilling time. Cryomilling was used to decrease the effect of temperature-induced changes, which commonly occur during milling.

Improvement of the dissolution rate of poorly soluble drugs by solid crystal suspensions.

We present a novel extrusion based approach where the dissolution rate of poorly soluble drugs (griseofulvin, phenytoin and spironolactone) is significantly accelerated. The drug and highly soluble mannitol are coprocessed in a hot melt extrusion operation. The obtained product is an intimate mixture of the crystalline drug and crystalline excipient, with up to 50% (w/w) drug load.

Investigating the effect of dehydration conditions on the compactability of glucose.

Hydrates are commonly found in pharmaceutical ingredients either in excipients or in the active pharmaceutical ingredient form. There is always the possibility that the processing involved in manufacturing can result in the dehydration of the hydrate components. It has been seen that different dehydration conditions can have an effect on the behavior of the final product; however this area has not been fully investigated.

Vibrational imaging of tablets by epi-detected stimulated Raman scattering microscopy.

Proper chemical imaging tools are critical to the pharmaceutical industry due to growing regulatory demand for intermediate and end-product content uniformity testing. Herein we demonstrate stimulated Raman scattering (SRS) imaging of active pharmaceutical ingredient (API) and four excipients within tablets. Tablets from six manufactures were imaged with a speed of 53 s per frame of 512 × 512 pixels (i.

A novel method to measure the glass and melting transitions of pharmaceutical powders.

A method to measure thermo-mechanical properties of pharmaceutical and polymeric powders was developed. The measurements are conducted by characterizing the material's response to applied acoustic waves. Measurements were performed using griseofulvin, felodipine and indomethacin as model drugs and polyethylene oxide (MW=200,000, 900,000, 2,000,000Da) as model polymers.

Assessment of Thermal Transitions by Dynamic Mechanical Analysis (DMA) Using a Novel Disposable Powder Holder.

Foods and pharmaceuticals materials are exposed to various environmental conditions during processing and while in storage; therefore, stability and quality are key attributes of concern. The properties of foods and pharmaceutical materials that define their quality are affected by conditions such as temperature, humidity and time. Glass transition is considered a key material property to understand how these external conditions affect the stability and quality of foods and pharmaceuticals.

The effect of dehydration conditions on the functionality of anhydrous amorphous raffinose.

The purpose of this investigation is to study the effect of dehydration conditions of raffinose pentahydrate (RF.5H2O) on the physical properties and functionality of the resulting material. Crystalline RF.

Elucidating raw material variability--importance of surface properties and functionality in pharmaceutical powders.

The purpose of this study is to illustrate, with a controlled example, the influence of raw material variability on the excipient's functionality during processing. Soluble starch was used as model raw material to investigate the effect of variability on its compaction properties. Soluble starch used in pharmaceutical applications has undergone a purification procedure including washing steps.

Interactions between bovine serum albumin and alginate: an evaluation of alginate as protein carrier.

The intermolecular interactions between the model protein, bovine serum albumin (BSA) and a biocompatible polysaccharide, sodium alginate, have been investigated. Both the native BSA and the heat pre-denatured BSA were utilized to study, in parallel, the effect of protein conformational change during the protein-alginate complex formation. In this work, a comparison was performed between the native BSA and the heat-denatured BSA incubated sodium alginate mixtures by using zeta potential analyzer, dynamic light scattering (DLS) and turbidimetric analysis of the systems in combination with protein conformational tools, Fourier transform infrared spectroscopy (FT-IR) and size exclusion chromatography (SE-HPLC).

Toward understanding the evolution of griseofulvin crystal structure to a mesophase after cryogenic milling.

The purpose of this research is to investigate the response of crystalline griseofulvin to mechanically induced stress through cryogenic milling. Crystalline griseofulvin was subjected to cryogenic milling for two different lengths of time. Following cryo-milling, the samples were immediately analyzed by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD).

Utility of multivariate analysis in modeling the effects of raw material properties and operating parameters on granule and ribbon properties prepared in roller compaction.

This article aimed to model the effects of raw material properties and roller compactor operating parameters (OPs) on the properties of roller compacted ribbons and granules with the aid of principal component analysis (PCA) and partial least squares (PLS) projection. A database of raw material properties was established through extensive physical and mechanical characterization of several microcrystalline cellulose (MCC) and lactose grades and their blends. A design of experiment (DoE) was used for ribbon production.

Investigation of the variability of NIR in-line monitoring of roller compaction process by using Fast Fourier Transform (FFT) analysis.

The purpose of this research was to investigate the variability of the roller compaction process while monitoring in-line with near-infrared (NIR) spectroscopy. In this paper, a pragmatic method in determining this variability of in-line NIR monitoring roller compaction process was developed and the variability limits were established. Fast Fourier Transform (FFT) analysis was used to study the source of the systematic fluctuations of the NIR spectra.

Preparation of calcium alginate microgel beads in an electrodispersion reactor using an internal source of calcium carbonate nanoparticles.

An electrodispersion reactor has been used to prepare calcium alginate (Ca-alginate) microgel beads in this study. In the electrodispersion reactor, pulsed electric fields are utilized to atomize aqueous mixtures of sodium alginate and CaCO3 nanoparticles (dispersed phase) from a nozzle into an immiscible, insulating second liquid (continuous phase) containing a soluble organic acid. This technique combines the features of the electrohydrodynamic force driven emulsion processes and externally triggered gelations in microreactors (the droplets) ultimately to yield soft gel beads.