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The global focus on incorporating natural ingredients into the diet for health improvement encompasses ω-3 polyunsaturated fatty acids (PUFAs) derived from plant sources, such as flaxseed oil. ω-3 PUFAs are susceptible to oxidation, but oil-in-water (O/W) emulsions can serve to protect PUFAs from this phenomenon. This study aimed to create O/W emulsions using flaxseed oil and either soy lecithin or Quillaja saponins, thickened with modified starch, while assessing their physical properties (oil droplet size, ζ-potential, and rheology) and physical stability. Emulsions with different oil concentrations (25% and 30% w/w) and oil-to-surfactant ratio (5:1 and 10:1) were fabricated using high-pressure homogenization (800 bar, five cycles). Moreover, emulsions were thickened with modified starch and their rheological properties were measured. The physical stability of all emulsions was assessed over a 7-day storage period using the TSI (Turbiscan Stability Index). Saponin-stabilized emulsions exhibited smaller droplet diameters (0.11-0.19 µm) compared to lecithin (0.40-1.30 µm), and an increase in surfactant concentration led to a reduction in droplet diameter. Both surfactants generated droplets with a high negative charge (-63 to -72 mV), but lecithin-stabilized emulsions showed greater negative charge, resulting in more intense electrostatic repulsion. Saponin-stabilized emulsions showed higher apparent viscosity (3.9-11.6 mPa·s) when compared to lecithin-stabilized ones (1.19-4.36 mPa·s). The addition of starch significantly increased the apparent viscosity of saponin-stabilized emulsions, rising from 11.6 mPa s to 2117 mPa s. Emulsions stabilized by saponin exhibited higher stability than those stabilized by lecithin. This study confirms that plant-based ingredients, particularly saponins and lecithin, effectively produce stable O/W emulsions with flaxseed oil, offering opportunities for creating natural ingredient-based food emulsions.

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Cyclodextrins (CDs) are cyclic oligosaccharides that contain a relatively hydrophobic central cavity and a hydrophilic outer surface. They are widely used to form non-covalent inclusion complexes with many substances. Although such inclusion complexes typically exhibit higher aqueous solubility and chemical stability than pure drugs, it has been shown that CDs can promote the degradation of some drugs. This property of stabilizing certain drugs while destabilizing others can be explained by the type of CD used and the structure of the inclusion complex formed. In addition, the ability to form complexes of CDs can be improved through the addition of suitable auxiliary substances, forming multicomponent complexes. Therefore, it is important to evaluate the effect that binary and multicomponent complexes have on the chemical and physical stability of complexed drugs. The objective of this review is to summarize the studies on the stabilizing and destabilizing effects of complexes with CDs on drugs that exhibit stability problems.

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The freeze-thaw (F/T) method is commonly employed during the processing and handling of drug substances to enhance their chemical and physical stability and obtain pharmaceutical applications such as hydrogels, emulsions, and nanosystems (e.g., supramolecular complexes of cyclodextrins and liposomes). Using F/T in manufacturing hydrogels successfully prevents the need for toxic cross-linking agents; moreover, their use promotes a concentrated product and better stability in emulsions. However, the use of F/T in these applications is limited by their characteristics (e.g., porosity, flexibility, swelling capacity, drug loading, and drug release capacity), which depend on the optimization of process conditions and the kind and ratio of polymers, temperature, time, and the number of cycles that involve high physical stress that could change properties associated to quality attributes. Therefore, is necessary the optimization of F/T conditions and variables. The current research regarding F/T is focused on enhancing the formulations, the process, and the use of this method in pharmaceutical, clinical, and biological areas. The present review aims to discuss different studies related to the impact and effects of the F/T process on the physical, mechanical, and chemical properties (porosity, swelling capacity) of diverse pharmaceutical applications with an emphasis on their formulation properties, the method and variables used, as well as challenges and opportunities in developing. Finally, we review the experimental approach for choosing the standard variables studied in the F/T method applying the systematic methodology of quality by design.

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In the present investigation, yam mucilage was evaluated as a stabilizer and emulsifier in the formulation of vanilla flavored ice cream; physicochemical, rheological, and stability characteristics were determined. A completely randomized bifactorial design was used (yam mucilage: Carboxymethylcellulose ratio with the following levels: 100:0, 80:20, 50:50, and 20:80, and stabilizers concentration with levels of 0.4 and 0.8%). Results showed an increase in the protein content present in ice cream mixture as the amount of mucilage increases. Rheologically, it was found that ice cream has the characteristic behavior of a pseudoplastic fluid, presenting a viscoelastic structure where elastic behavior predominates. In addition, ratios with a higher content of mucilage incorporated a greater volume of air and presented the longest melting times, delaying drops falling time; in the same way mucilage gives ice cream a freezing temperature between -6.1 to -2.8 °C, indicating that the application of mucilage in food industry is possible due to its nutritional value, and it gives ice cream stability properties.

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BACKGROUND: Salad dressing formulations include a pH within 3.2-4.1, salt and other solutes to depress water activity. The interaction between hydrocolloids and other components such as humectants determines their physical and microbiological stability. To our knowledge, the effect of commonly used solutes on physical stability and rheological characteristics of oil-in-water emulsions stabilized by xanthan gum has not been reported, and neither has the effect of a spoilage yeast on physical stability been evaluated. RESULTS: The effect of different humectants (sodium chloride, glucose and xylitol) and Zygosaccharomyces bailii inoculation on the stability of oil-in-water emulsions containing different levels of xanthan gum to emulate different types of salad dressings was investigated by means of droplet size, zeta potential, rheological measurements and confocal laser scanning microscopy (CLSM). Generally, the addition of humectants strengthened the weak or strong emulsion structure, especially xylitol. Glucose or xylitol acted as stabilizers since they decreased Sauter and De Broucker diameter. On the contrary, NaCl destabilized the emulsions since it increased droplet size and exhibited the lowest absolute values of zeta potential. Inoculation with Z. bailii destabilized some emulsions since it increased Sauter and De Broucker diameter. Emulsion droplet size, polydispersity, and xanthan gum and yeast location were confirmed by CLSM imaging. CONCLUSION: This study highlights the key role of humectants and xanthan gum level on physical characteristics and stability of oil-in-water emulsions. Addition of xylitol leads to an enhancement in emulsion rheology and physical stability, suggesting that it is a potential low-calorie multifunctional additive for salad dressings. © 2022 Society of Chemical Industry.

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The utilization of astaxanthin in food processing is considered to be narrow because of its substandard solubility in aqueous matrices and the instability of chemical compounds during the processing of food and the instability of chemical compounds during the processing of food. The investigation sought to evaluate multilayer emulsions stabilized by ionic interfacial layers of lupin protein isolate (LPI), ι-carrageenan (CA), and chitosan (CHI) on the physical stability of the emulsion as well as the retention of astaxanthin during the spray drying process. Primary emulsion (Pr-E) was prepared by adding LPI on oil droplet surfaces containing astaxanthin. The homogenization pressure and cycles to obtain the Pr-E were investigated. The secondary emulsion (Se-E) and tertiary emulsion (Te-E) were elaborated by mixing CA/Pr-E and CHI/Se-E, respectively. Emulsion stability was assessed under different environmental stresses (pH and NaCl). Astaxanthin retention of emulsions was determined immediately after finishing the spray-drying process. The results showed that Pr-E was stabilized with 1.0% (w/v) of LPI at 50 MPa and three cycles. Se-E and Te-E were obtained with CA/Pr-E and Se-E/CHI of 70/30 and 50/50% (w/w), respectively. The Se-E was the most stable compared to the Pr-E and Te-E when subjected to different pHs; nevertheless, once the NaCl concentration rose, no variations in the ζ-potential of all emulsions studied or destabilization were observed. The Se-E and Te-E derived provided higher astaxanthin retention (>95%) during the spray-drying process compared to Pr-E (around 88%). The results indicated that these astaxanthin multilayer emulsions show considerable potential as a functional ingredient in food products.

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This study was done to determine the time while the binary admixtures with midazolam and haloperidol drugs are administered by perfusion to the patients in the clinical routine. Samples with different concentrations of both drugs were prepared following the usual clinical practice. Solvents used were 0.9 % sodium chloride solution and 5% dextrose, and viaflo plastic bags were used as the containers of the admixtures. Samples were not protected from light and were stored at 20 ºC or at 4 ºC. Compatibility and physicochemical stability were studied by visual inspection, turbidity measurement, pH determination and ultraviolet detection high performance liquid chromatography (UV-HPLC) was used to determine midazolam and haloperidol concentrations. The assay was validated following the FDA and EMA guidelines. Darunavir was used as internal standard (IS). For the studied admixtures, turbidity measurements and pH determinations showed little changes in function of the time. Haloperidol and midazolam concentrations determined by HPLC are within the acceptable range of drug concentrations, which are considered stable for four days in case of admixtures stored at 20 ºC and for seven days for refrigerated admixtures. Taking into account the microbiological risk matrix, the compatibility and the chemical and microbiological stability of the midazolam and haloperidol in the co-administered admixtures in viaflo plastic bags with 0.9 % sodium chloride solution and 5% dextrose can be set as 48 hours when samples are stored at 20 ºC and one week if they are refrigerated.

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The aim of this research was to determine the physicochemical properties, microbial counts and aflatoxin M1 (AFM1) levels of thermoultrasonicated, pasteurized and untreated milk (control) at days 1, 7 and 14 of storage. Thermoultrasound treatment was performed at a rate of 20 kHz for 10 or 15 min and 95% amplitude on homogenized and non-homogenized milk samples. Results showed that most physicochemical parameters were within the Mexican norms established for milk. Ultrasound treatment for 15 min reduced solids precipitation (p < 0.05) in unhomogenized milk during storage as compared to the pasteurized milk. All samples complied with aerobic mesophilic counts limits set by the Mexican norm except the control and the homogenized milk sample which was thermoultrasonicated for 10 min. Enterobacteriaceae counts of pasteurized and 15 min-thermoultrasound homogenized milks complied with the norm. The lowest levels of AFM1 were found in the 10 min-thermoultrasound unhomogenized milk (0.15 ±â€¯0.05 pg AFM⁠1E/mL) one day after storage. Thermoultrasound did not affect the color of samples but homogenized milk treated for 10 min exhibited less total color difference. A high phenolic content was found in thermoultrasound and pasteurized milks on day 1. Thermoultrasound could be an alternative to milk pasteurization that preserves the physicochemical and microbiological quality of milk while reducing AFM1 levels.

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Norfloxacin, an antibiotic that exists in different solid forms, has very unfavorable properties in terms of solubility and stability. Binary complexes of norfloxacin, in the solid form C, and ß-cyclodextrin were procured by the kneading method and physical mixture. Their effect on the solubility, the dissolution rate, and the chemical and physical stability of norfloxacin was evaluated. To perform stability studies, the solid samples were stored under accelerated storage conditions, for a period of 6 months. Physical stability was monitored through powder X-ray diffraction, high-resolution 13C solid-state nuclear magnetic resonance, and scanning electron microscopy. The results showed evidence that the kneaded complex increased and modulated the dissolution rate of norfloxacin C. Furthermore, it was demonstrated that the photochemical stability was increased in the complex, without affecting its physical stability. The results point to the conclusion that the new kneading complex of norfloxacin constitutes an alternative tool to formulate a potential oral drug delivery system with improve oral bioavailability.

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Ganciclovir (GCV; systematic name: 2-amino-9-{[(1,3-dihydroxypropan-2-yl)oxy]methyl}-6,9-dihydro-1H-purin-6-one), C9H13N5O4, an antiviral drug for treating cytomegalovirus infections, has two known polymorphs (Forms I and II), but only the structure of the metastable Form II has been reported [Kawamura & Hirayama (2009). X-ray Struct. Anal. Online, 25, 51-52]. We describe a successful preparation of GCV Form I and its crystal structure. GCV is an achiral molecule in the sense that its individual conformers, which are generally chiral objects, undergo fast interconversion in the liquid state and cannot be isolated. In the crystalline state, GCV exists as two inversion-related conformers in Form I and as a single chiral conformer in Form II. This situation is similar to that observed for glycine, also an achiral molecule, whose α-polymorph contains two inversion-related conformers, while the γ-polymorph contains a single conformer that is chiral. The hydrogen bonds are exclusively intermolecular in Form I, but both inter- and intramolecular in Form II, which accounts for the different molecular conformations in the two polymorphs.

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Chloramphenicol is an old antibiotic agent that is re-emerging as a valuable alternative for the treatment of multidrug-resistant pathogens. However, it exhibits suboptimal biopharmaceutical properties and toxicity profiles. In this work, chloramphenicol was combined with essential amino acids (arginine, cysteine, glycine, and leucine) with the aim of improving its dissolution rate and reduce its toxicity towards leukocytes. The chloramphenicol/amino acid solid samples were prepared by freeze-drying method and characterized in the solid state by using Fourier transform infrared spectroscopy, powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and solid-state nuclear magnetic resonance. The dissolution properties, antimicrobial activity, reactive oxygen species production, and stability of the different samples were studied. The dissolution rate of all combinations was significantly increased in comparison to that of the pure active pharmaceutical ingredient. Additionally, oxidative stress production in human leukocytes caused by chloramphenicol was decreased in the chloramphenicol/amino acid combinations, while the antimicrobial activity of the antibiotic was maintained. The CAP:Leu binary combination resulted in the most outstanding solid system makes it suitable candidate for the development of pharmaceutical formulations of this antimicrobial agent with an improved safety profile.

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A new in vitro mechanical gastric system (IMGS) was fabricated which incorporates: a J-shaped stomach, a mechanical system with realistic peristaltic frequency and force magnitude, and a reproduction of the gastric pH curve. To evaluate the impact of a more realistic gastric peristalsis on the intestinal lipolysis of protein-stabilized O/W emulsions, the emulsions were subjected to two different in vitro digestion methodologies: (i) gastric digestion in the IMGS and intestinal digestion in a stirred beaker (SB), and (ii) gastric and intestinal digestion assays carried out in SBs. At the end of the intestinal digestion, the total amount of free fatty acids released was significantly higher for the first methodology (IMGS-SB) in comparison with the second one (27.5% vs. 23.0%), probably due to the higher physical instability induced by the IMGS in the gastric contents. These results reaffirm that O/W emulsion stability plays a crucial role in controlling the final extent of lipolysis of this kind of food-grade emulsions.

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Infectious diseases are a heterogeneous group of maladies that represent a serious burden to healthcare systems worldwide. Most of the available antimicrobial drugs display poor biopharmaceutical properties that compromise their effectiveness. Cyclodextrins (CDs) are cyclic oligosaccharides of glucopyranose formed by a variable number of repeating units that combine a hydrophilic surface with a hydrophobic cavity. The production of drug/CD complexes has become one of the most extensively investigated technology approaches to improve the stability, solubility, dissolution rate and bioavailability of drugs. The present work overviews the applications of CDs for the formulation of anti-infective agents along with the most relevant administration routes. Finally, an update on the complexes with CDs available on the market to treat infectious diseases is presented.

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In this work two systems based on a carbohydrate polymer were studied: inulin as model system and inulin-orange juice as complex system. Both system were stored at different water activity conditions and subsequently characterized. Water adsorption isotherms type II were fitted by the GAB model and the water monolayer content was determined for each system. From thermal analyzes it was found that at low water activities (aw) systems were fully amorphous. As aw increased, crystallinity was developed. This behavior was corroborated by X-ray diffraction. In the inulin-orange juice system, crystallization appears at lower water activity caused by the intensification of the chemical interaction of the low molecular weight species contained in orange juice. Glass transition temperature (Tg), determined by modulated differential scanning calorimeter, decreased with aw. As water is adsorbed, the physical appearance of samples changed which could be observed by optical microscopy and effectively related with the microstructure found by scanning electron microscopy.

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