Oral Formulations Research Articles

Personality traits and their relationship with oral health related quality of life among adolescents in Saudi Arabia

BackgroundPersonality traits are linked with different oral health outcomes. However, personality traits and their associations among children are not fully understood. Therefore, this study aimed to investigate the relationship between personality traits and oral health-related quality of life (OHRQoL) among adolescents in Saudi Arabia.MethodsThis cross-sectional study included male and female students aged 12–18 years from different schools in the Eastern Province of Saudi Arabia. The participants responded to a self-administered questionnaire after providing informed consent. The questionnaire included demographic information and Arabic versions of the Big Five Personality Inventory and the Child Oral Health Impact Profile-Short Form to evaluate personality traits and OHRQoL, respectively. Bivariate and multivariable analyses were performed.ResultsThis study included 231 (59.7%) males and 156 (40.3%) females. Regarding personality traits, conscientiousness had the highest mean score (15.31 ± 3.65), followed by agreeableness (14.94 ± 3.96) and openness (14.08 ± 3.98), whereas neuroticism had the lowest mean score (8.86 ± 3.34). Males had significantly higher mean scores for extraversion (14.28 ± 3.30) and conscientiousness (15.69 ± 3.62) compared to females, who had mean scores of 13.02 ± 3.35 and 14.75 ± 3.63, respectively (P < 0.05). Females, on the other hand, scored significantly higher in neuroticism (9.51 ± 3.71) and agreeableness (15.60 ± 3.75) compared to males, who had mean scores of 8.09 ± 2.94 and 14.49 ± 4.04, respectively (P < 0.05). Bivariate analyses showed that neuroticism was negatively correlated with OHRQoL (r = -0.455, P < 0.001), whereas extraversion (r = 0.182, P < 0.001) and conscientiousness (r = 0.110, P = 0.047) were positively correlated with OHRQoL. In multiple linear regression analyses, extraversion (B = 0.696, P = 0.012) and neuroticism (B=-2.229, P < 0.001) were statistically significant predictors of OHRQoL.ConclusionThis study found that neuroticism was significantly and negatively correlated with OHRQoL, whereas extraversion was significantly and positively correlated with OHRQoL. In addition, there were statistically significant differences in personality traits between the male and female adolescents.

Pharmacokinetics and bioequivalence evaluation of two oral formulations of topiramate tablets in healthy Chinese male volunteers under fasting and fed conditions.

Topiramate is an antiepileptic drug (AED) that is effective in treating various types of epilepsy. This study evaluated the bioequivalence and safety of two topiramate tablets in healthy Chinese subjects under fasting and fed conditions. We designed an open-label, randomized, single-dose, two-period, crossover trial protocol. Two independent trials were conducted, each including 26 volunteers. In the fed trial, subjects were randomly assigned to two groups (1:1 ratio) to receive either 100mg of test formulation or reference formulation of topiramate. After a 21-day washout period, crossover administration was implemented. The fasting trial design was similar to that of the fed trial. Plasma concentrations of topiramate were determined using a validated method (high-performance liquid chromatography-tandem mass spectrometry, HPLC-MS/MS). Pharmacokinetic (PK) parameters such as maximum plasma drug concentration (Cmax), time to reach maximum concentration (Tmax), and the area under the plasma concentration-time curve from time 0 to 72h (AUC0-72) were calculated using a non-compartment model to evaluate the bioequivalence of two formulations. The safety of volunteers was monitored during the entire study. In the fasting trial, 90% confidence intervals (CIs) of geometric mean ratios (GMRs) of the test to reference formulations were 101.26-112.94% for Cmax and 98.50-102.69% for AUC0-72, all within the recognized bioequivalence range of 80.00-125.00%. In the fed trial, 90% CIs of GMRs of the test to reference formulations were 92.08-101.54% for Cmax and 95.81-99.79% for AUC0-72, both were within the bioequivalence range of 80.00-125.00%. Research findings indicated that the two topiramate formulations were bioequivalent and had a favorable safety profile.

Bioequivalence and Food Effect Assessment Between 2 Oral Tablet Formulations of Rivaroxaban 20mg in Healthy Chinese Subjects.

To evaluate the bioequivalence and safety of oral rivaroxaban tablets between a test formulation and a reference formulation in healthy Chinese subjects, a randomized, open, 2-formulation, 4-cycle, complete repeat crossover study was conducted under both fasting and fed states. Thirty-six healthy participants were enrolled separately for the fasting and fed groups, and each subject received a single oral dose of 20mg of the test or reference formulation of rivaroxaban tablets per cycle. Blood samples were collected at specified intervals, and rivaroxaban was analyzed using liquid chromatography-tandem mass spectrometry. Under fasting and fed conditions, the 90% confidence intervals (CIs) for the geometric mean ratios of the maximum concentration (Cmax), the area under the plasma concentration-time curve from time 0 to the last measurable time point (AUC0-t), and the area under the curve extrapolated to infinity from time 0 (AUC0-∞) all fell within the 80%-125% CI, and the upper limit of the 90% CIs for the test-to-reference ratio of the within-subject variability was <2.5. This indicated that the test formulation of rivaroxaban is bioequivalent to the reference formulation. Compared to the fasted state, the Cmax, AUC0-t, and AUC0-∞ of rivaroxaban increased significantly by factors of 2, 1.6, and 1.5, respectively, following oral administration of 20mg of rivaroxaban in the fed state. This suggests that a high-fat diet significantly enhances the exposure to rivaroxaban. No serious adverse events were reported under fasting or fed conditions.

The future approach for the management of acute bacterial skin and skin structure infections.

To discuss the new available options for the treatment of acute bacterial skin and skin structure infections (ABSSSIs) and how to implement in the clinical practice innovative approaches for their management. The availability of long-acting antibiotics, including dalbavancin and oritavancin, changed the approach to patients with ABSSSI. Direct discharge from the emergency department and early discharge from the hospital should be considered in patients with ABSSSI. Despite limited data about different bactericidal properties, the choice between dalbavancin and oritavacin is usually based on patients' characteristics and comorbidities. Delafloxacin and omadacycline are other options and have the advantage to be available for both intravenous and oral formulations, allowing a sequential therapy and switch from intravenous to oral treatment in clinically stable patients. Further studies should elucidate the profile of patients who may beneficiate from these drugs. Early discharge from the hospital should be considered in patients with ABSSSI at a high risk of methicillin-resistant Staphylococcus aureus and in vulnerable patients for which hospitalization may have detrimental consequences. In elderly individuals, patients with diabetes mellitus, oncological people who need for continuing their healthcare pathway, this approach may reduce complications and costs related to hospitalization.

Vitamins as excipients in pharmaceutical products.

Excipients are ingredients in pharmaceutical products other than the active ingredient, added to facilitate manufacturing, enhance stability or modulate release and bioavailability. Vitamins are diverse molecules essential for human nutrition that also can fulfil excipient functions. This review focuses on vitamins used as excipients and provides an overview of the functions of vitamins in various pharmaceutical formulations. A thorough search was conducted to understand the current use of vitamins in marketed drug products, concluding that many vitamins are already used as functional excipients. Vitamins are used widely in different dosage forms, including oral, parenteral, and topical formulations, and alongside a broad range of active pharmaceutical ingredients, biologics, and small molecules from different biopharmaceutical classification system classes. Many examples of the use of vitamins to improve the performance of the pharmaceutical formulation in which they are included are presented and the mode of action of vitamins as excipients in the product is reviewed. Furthermore, the potential for future uses of vitamins in pharmaceutical products is highlighted. Lastly, considerations for the use of vitamins as excipients in drug products as well as the regulatory framework are discussed.

Development and in vitro/in vivo evaluation of taste-masked orodispersible films of dapoxetine hydrochloride using ion exchange resins.

Dapoxetine hydrochloride tablets are the most commonly used drug for the treatment of premature ejaculation (PE). However, the tablets must be taken with water 1-3h before sexual activity, which makes the medication intake conspicuous and inconvenient. This study aimed to develop taste-masked orodispersible films (ODFs) of dapoxetine hydrochloride using ion exchange resins. It was found that the based-Kyron T-134 resin complex achieved a high drug loading of 75.9 ± 1.4%, establishing the mass ratio of dapoxetine hydrochloride to Kyron T-134 at 2:1, and adjusting the solution pH to 5.4 ± 0.05. The effect of pH on the drug loading of the resin was initially characterized by SEM, while the binding mechanism between dapoxetine hydrochloride and the resin was investigated by XRD, DSC, and FTIR. The ODFs exhibited favorable mechanical properties and palatability. Meanwhile, the drug release in both the ODFs and commercially available tablets Priligy® could reach 100.8% of the drug over 15min in a simulated gastric fluid with pH 1.2 HCl. Furthermore, pharmacokinetic studies conducted in healthy volunteers demonstrated that the ODFs were bioequivalent to Priligy®. Therefore, this ODFs, characterized by its pleasant taste and water-free administration, offer a novel and convenient oral formulation for patients with PE, thereby enhancing patient compliance.

A comparative study of two data-driven modeling approaches to predict drug release from ER matrix tablets.

The pharmaceutical industry is striving to develop innovative and promising tools, increasingly embracing new data-driven approaches, to understand, improve and accelerate the drug product development process. While extended release (ER) oral formulations offer a number of advantages, including maintenance of therapeutic drug levels, a reduction in dosing frequency, and minimization of side effects, achieving consistent drug release profiles remains a significant challenge. As a critical attribute for drug absorption into systemic circulation, in vitro dissolution testing represents a time-consuming and complex method for the evaluation of such formulations. The main objective of this study was to develop a model for predicting drug dissolution in the quality by design (QbD)-based development of ER oral hydrophilic matrix tablets comprising polyethylene oxide (PEO). Two main modeling approaches are conducted and compared: (i) model screening to fit and compare multiple predictive machine learning (ML) models and then deploy the best model, in this case, artificial neural networks (ANN), and (ii) functional data analysis (FDA) combined with the design of experiments (DoE) that fit a smoothing model to each dissolution curve as a continuous function. A dataset comprising 91 ER matrix tablet formulations was analyzed, with the dissolution data split into training, validation, and test sets (70%, 20%, and 10%, respectively). The results demonstrated that both ANN and functional DoE (FDOE) models achieved high similarity with the experimental dissolution profiles, as indicated by f2 values ranging from 48 to 88 for the FDOE and 52 to 88 for ANN. This work highlights the potential of integrating advanced data-driven modeling techniques into ER drug development to enhance dissolution prediction accuracy and streamline the formulation process, thus reducing time and costs.

Enhanced Vitamin C Delivery: A Systematic Literature Review Assessing the Efficacy and Safety of Alternative Supplement Forms in Healthy Adults.

Vitamin C is an antioxidant and is essential for immune function and infection resistance. Supplementation is necessary when a sufficient amount of vitamin C is not obtained through the diet. Alternative formulations of vitamin C may enhance its bioavailability and retention over traditional ascorbic acid. This systematic review consolidates the evidence on this and the effects on immunity and infection. A systematic literature search was conducted in October 2024 in Embase and Medline, focused on healthy adults (Population); oral forms of liposomal-encapsulated ascorbic acid, liposomal-encapsulated lipid metabolite ascorbic acid, calcium ascorbate, slow-release ascorbic acid, or lipid metabolite ascorbic acid (Intervention); compared to placebo/others (Comparison); in terms of bioavailability, absorption, vitamin C concentration in plasma, serum, and leukocytes, and impacts on tolerability, immunity, and infection (Outcome); and included randomized or non-randomized controlled trials, single-arm trials, and observational studies (Study design). Thirteen studies were included, several evaluating calcium ascorbate in combination with vitamin C metabolites, including L-threonate, referred to here as Calcium ascorbate EC (Ester C®; n = 7). No safety or tolerability concerns were noted with Calcium ascorbate EC vs. placebo or ascorbic acid. Calcium ascorbate EC showed better tolerability and fewer epigastric adverse events, improved quality of life, and induced favorable oxalate changes vs. ascorbic acid. Four studies reported leukocyte vitamin C concentration, some showing higher concentrations with Calcium ascorbate EC vs. ascorbic acid; seven reported more favorable plasma concentrations with the alternative forms over ascorbic acid or placebo; one reported higher serum vitamin C levels with vitamin C lipid metabolites than with Calcium ascorbate EC, calcium ascorbate, and ascorbic acid. No study reported retention in tissues. One study reported a favorable impact of Calcium ascorbate EC on immune parameters, and one found an association of Calcium ascorbate EC with fewer colds and a shorter duration of severe symptoms vs. placebo. Findings suggest that alternative vitamin C forms can improve leukocyte vitamin C, sometimes without affecting plasma levels. Most studies (77%) had a low risk of bias. In conclusion, the type and delivery modality of vitamin C can impact its bioavailability and functionality. Studies highlight the advantages of Calcium ascorbate EC over traditional ascorbic acid in terms of its tolerability and its potential to increase leukocyte vitamin C concentrations, crucial for immune function and protection against infection. However, further research is required to conclusively establish its effects on immune health.

Production, Characterization, and In Vitro Antifungal Evaluation of Itraconazole-Loaded Fibrous Sheets Prepared by Electrospinning with a Factorial Design

Itraconazole (ITZ) is a broad-spectrum triazole antifungal agent suitable for the treatment of superficial and systemic mycoses. This study aimed to formulate, characterize, and evaluate the in vitro antifungal performance of single-jet electrospun itraconazole-loaded polyvinylpyrrolidone-based fibers. Fibrous mats were prepared under the following experimental conditions: 10, 12.5, and 15 cm needle–collector distance, 20 kV tension, and 1, 1.5, and 2 mL/hour flow rate. The fibers were characterized by SEM, DSC, FTIR, assays, disintegration tests, dissolution tests, and in vitro antifungal activity. Using a 22 factorial design, the effects of preparation variables on the characteristics of the fibrous sheets were described. The electrospinning process led to smooth-surfaced, randomly oriented, and bead-free fibers. The average fiber diameter ranged from 887 nm to 1175 nm. The scanning calorimetry of pure ITZ revealed a sharp endothermic melting point at a temperature of 170 °C, not present in the curves of the fibers. After 60 min, between 70 and 100% of ITZ was released. The antifungal assay revealed that the fibers inhibited the growth of Candida albicans and Candida parapyilosis. The obtained fiber mats prepared from the hydrophilic polymer presented almost instantaneous disintegration, with potential applications for rapid antifungal delivery in oral or topical pharmaceutical form.

Next-generation pharmaceuticals: the rise of sildenafil citrate ODF for the treatment of men with erectile dysfunction.

Orodispersible film (ODF) is one of the novel formulations that disintegrate rapidly in the mouth without the requisite for water compared to other conventional oral solid dosage formulations. This delivery system serves as a convenient mode of administration, especially in patients who have dysphagia and fluid restriction, being beneficial to pediatric, geriatric, and bedridden patients. A novel sildenafil ODF containing sildenafil citrate is formulated to be used in patients with erectile dysfunction (ED). This review discusses the advantages of ODF in improving compliance and satisfaction in these patients and describes the manufacturing techniques, evaluation tests, bioequivalence, and stability studies of sildenafil ODF. This formulation offers unique benefit to patients with ED by improving their acceptance and compliance and respecting their privacy and the need for a discreet treatment. Moreover, the comparison of pharmacokinetic parameters between the sildenafil ODF administered with and without water and the conventional film-coated tablet were similar. It also demonstrated reliable performance that yielded a consistent product, meeting all specifications at release and after three weeks of storage under stressed conditions (60°C). Sildenafil ODF warrants improved ease of intake, taste, portability, storage, and compliance among ED patients, making it the potential most preferred formulation and drug of choice.

Exploring the Therapeutic Landscape: A Narrative Review on Topical and Oral Phosphodiesterase-4 Inhibitors in Dermatology.

Phosphodiesterase-4 (PDE4) is involved in the synthesis of inflammatory cytokines that mediate several chronic inflammatory disorders, including psoriasis and atopic dermatitis. In recent years, the therapeutic armamentarium in dermatology has expanded with the introduction of PDE4 inhibitors, both in oral and topical formulations. PDE4 inhibitors have gained increasing interest due to their remarkable safety record and ease of prescription, as evidenced by the recent influx of literature detailing its off-label uses. Apremilast was the first PDE4 inhibitor approved by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for psoriasis, psoriatic arthritis, and oral ulcers of Behcet's disease. Off-label use has been reported in diverse dermatological conditions, including aphthous stomatitis, chronic actinic dermatitis, atopic dermatitis, cutaneous sarcoidosis, hidradenitis suppurativa, lichen planus, and discoid lupus erythematosus. Roflumilast is a PDE4 inhibitor that was approved by the FDA and the EMA as an oral treatment of chronic obstructive pulmonary disease. Since patent expiration, several generic formulations of oral roflumilast have become available, and various studies have documented its off-label use in psoriasis and other dermatological conditions such as hidradenitis suppurativa, recurrent oral aphthosis, nummular eczema, lichen planus, and Behçet's disease. Topical roflumilast has received FDA approval for treatment of plaque psoriasis and seborrheic dermatitis. The favorable safety profile encourages its long-term use as an alternative to corticosteroids, addressing the chronic nature of many dermatological conditions. New oral PDE4 inhibitors are being developed, such as orismilast (LEO-32731), mufemilast (Hemay005), difamilast (OPA-15406) or lotamilast (E6005/RVT-501), among others. This narrative review provides a comprehensive synthesis of the pharmacology, clinical efficacy, safety profile, and practical considerations regarding the oral and topical use of PDE4 inhibitors in dermatology.

Pharmaceutical development of sangviritrin spray for the treatment of inflammatory diseases of the oral cavity

Introduction. One of the most common bacterial infections includes acute and chronic tonsillitis, affecting 10 to 15 % of adults and approximately 20–25 % of children worldwide, according to the World Health Organization. The focus of this study was an original substance, sangviritrin, containing no less than 96.5 % of the sum of bisulfates of two alkaloids: sanguinarine and chelerythrine. Given the high antimicrobial activity of sangviritrin, the research aimed to develop a local delivery system based on this medicinal substance.Aim. The aim of this work was to develop an oral medicinal form of sangviritrin.Materials and Methods. Sangviritrin, produced by the All-Russian Scientific Research Institute of Medicinal and Aromatic Plants, was used as the active pharmaceutical ingredient. The selection of auxiliary components was carried out in accordance with the methodologies specified in the State Pharmacopoeia XV edition. The organoleptic properties of the substance and spray samples were studied using A. I. Tenzova's method. The local irritant action of the spray was assessed using the conjunctival test method on chinchilla rabbits weighing 3.5–4.3 kg. Quantitative determination of sangviritrin in the medicinal form was performed using spectrophotometric methods at a wavelength of 321 ± 2 nm on a spectrophotometer SPECORD® 200 PLUS (Analytik Jena GmbH+Co. KG, Germany).Results and Discussion. Optimal auxiliary component compositions were selected based on measurements of spray technological parameters. A comprehensive approach was justified for correcting the organoleptic properties of the substance, involving the introduction of a minimal amount of sweeteners and additional use of β-cyclodextrin. Examination of the local irritant action indicated a "weak or absent" degree of local irritation.Conclusion. A local delivery system for sangviritrin has been developed for the treatment of infectious and inflammatory diseases of the oral cavity.

Meta-Analysis of the Input and Disposition of Various Dosage Forms of Methylprednisolone in Healthy Subjects Utilizing a Physiologically Based Pharmacokinetic Model.

The study quantitatively analyzes and compares the pharmacokinetics (PK) of methylprednisolone (MPL) in humans upon administration of various dosage forms. The PK parameters and profiles of MPL in healthy subjects were collected from 22 literature sources. A minimal physiologically based pharmacokinetic (mPBPK) model consisting of blood and two tissue (lumped liver and kidney, remainder) compartments with nonlinear tissue partitioning was applied to describe MPL disposition. Overall 18 plasma concentration profiles were well captured and 85% of PK parameters reasonably estimated. The clearance (CL) of MPL averaged 336mL/h/kg and appeared slightly nonlinear across a dosage range of 5 to 800mg, the distribution volume (Vd) averaged 1.17 L/kg, and the model predicted elimination half-life (t1/2) was 2.6h. Rapid prodrug conversion was found for intravenous MPL sodium succinate (MPSS) with a t1/2 of 1.7min, and followed by MPL phosphate (MPPS) 3.8min, MPL hemisuccinate (MPHS) 16min, and MPL suleptanate (MPSP) 2.9h. Their bioavailabilities (F) varied slightly from 60 to 73%. Intramuscular doses showed an absorption rate constant (ka) of 1.5h-1 for MPSS and 96h-1 for MPSP. Oral doses of 5 formulations were examined. Medrol exhibited greatest absorption with F of 74% and ka of 2.1h-1, while one generic product had F of 32.6%. This study demonstrated the utility of a mechanistic mPBPK disposition model for comparing MPL formation from various esters, absorption from several oral dose formulations, and modest variability across numerous PK studies in healthy humans.

A Comparative Analysis of the Pharmacodynamic and Pharmacokinetic Properties of 2 Controlled-Release Formulations Versus a Marketed Orlistat Product.

A new modified-release oral formulation combines acarbose and orlistat (MR-OA) to enhance efficacy and reduce adverse effects through controlled drug release. This study aims to compare the pharmacodynamic properties of the orlistat component of MR-OA (MR-O) with a conventional orlistat product, Xenical (Conv-O), analyzing the percentage of fecal fat excretion. In addition, the pharmacokinetic properties of the complete formulation, MR-OA, were compared with Conv-O. In Part I of the study, 20 healthy volunteers were randomized in a single-blind, crossover trial to take MR-O or Conv-O (120-mg orlistat) 3 times daily for 9 days. Fecal fat was measured at baseline and after each treatment. MR-O and Conv-O similarly increased fecal fat percentage from 3.8% to 13.5%, confirming pharmacodynamic equivalence. Adverse events were few and generally rated as mild. In Part II, participants received MR-OA and then Conv-O, with blood samples collected for 12 hours to measure orlistat and acarbose levels. Orlistat's peak concentration stayed below 5ng/mL, and acarbose plasma levels were mostly undetectable, indicating minimal systemic absorption. This shows that the new weight loss product MR-OA retains the dietary energy loss pathway used in Conv-O. Consistent with previous studies, minimal systemic absorption of orlistat and acarbose was observed for MR-OA, confirming that no significant alteration of the original substances occurs when modifying their release.

In Silico Screening of Phytochemicals as Potential Inhibitors of the JAK/STATs Pathway in Psoriasis.

The skin is a dynamic tissue that consists of different layers such as stratum corneum, the site for keratinocyte development and maturation for the natural changeover of skin. In psoriasis, this natural development of keratinocytes gets disturbed and aggregation of nucleated keratinocytes takes place in the epidermis of the skin, leading to the presence of scaly skin, which makes the patient physically, socially, and psychologically ill. Various natural, semisynthetic, and synthetic treatments are available. Still, semisynthetic or synthetic are mainly used to treat psoriasis with side effects on different parts of the body, which is life threatening. Various molecular target sites are getting upregulated such as Janus kinase/Signal transducer and activator of transcription (JAK/STATs), phosphodiesterase 4 (PDE4), mitogen-activated protein kinase (MAPK), platelet selectin (Pan Selectin), Tumor Necrosis Factor Alpha (TNF-α), Interleukin-23 (IL-23), Interleukin-17 (IL-17), and Tyrosine Kinase 2 (Tyk2) in psoriasis. Plants and their bioactive compounds of flavonoids, alkaloids, resins, tannins, glycosides, and terpenoids category are used in the treatment of psoriasis as topical, oral, and biological forms. Using a computational approach, the inhibition of these molecular targets can be studied and potential molecules can be identified. This research article aims to find out the potential molecules that can inhibit the molecular sites and are effective than synthetic ones.

Selected topics of the 27th IPVS Congress in Leipzig. The impact of changes in swine production and globalization of pig trade on the appearence and spread of transboundary diseases.

Between June 4 and 7 2024, the 27th Congress of the International Pig Veterinary Society (IPVS) took place in Leipzig, Germany. The meeting took place in a modern congress center located on the outskirts of this historic Saxon city with a history of more than a thousand years. Polish practitioners and scientists involved in the field of swine diseases have been participating in IPVS congresses since the beginning. Our delegation is usually one of the most numerous. In Leipzig, the IPVS congress was held for the first time simultaneously with the 15th European Symposium of Porcine Health Management (ESPHM), which has been organized for many years by the European College of Pig Health Management (ECPHM). Hence, IPVS&amp;ESPHM affiliations appear in all materials related to the congress. During the congress, 1,035 reports were presented in oral or poster form. Plenary lectures were of particular interest. The 17 lectures were presented by internationally recognized scientists and practitioners invited by the organizers. Analyzing the subject matter of the papers submitted to the congress, it can be concluded that the most important topics over the last two years have been viral diseases of pigs, including circovirus infections, PRRS, and ASF. Scientists predict that, due to climate change, at least 15,000 viruses will move between different mammalian species in the next 50 years. Human mortality from zoonoses is projected to increase 12-fold between now and 2050.

Manipulated Slow Release of Florfenicol Hydrogels for Effective Treatment of Anti-Intestinal Bacterial Infections.

The difficulty of establishing slow release at intestinal infection sites, weak antibacterial effects, as well as the limited broad use of florfenicol oral formulations are the main targets of the current study. Novel hydrogels derived from sodium alginate were developed using a complexation form for florfenicol delivery to achieve slow release at the site of intestinal infection and enhance its antibacterial activity against Escherichia coli. The optimal formulation, physicochemical properties, stability, pH-responsive performance, antibacterial activity, and in vitro biosafety of the florfenicol hydrogels have been studied systematically. The created hydrogels had a consistent spherical morphology, with an average diameter of 531.9±12.6 nm. Energy dispersive spectroscopy and Fourier transform infrared indicated that florfenicol hydrogels have been successfully prepared through complexation force. Furthermore, it is shown that florfenicol hydrogels hold outstanding stability, excellent sustained release, and faster swelling and release at intestinal pH due to pH-responsiveness. The florfenicol hydrogels had no obvious structural destruction in simulated gastric juice (pH=1.2) for 12 hrs and were highly stable. However, the hydrogels began to be destroyed after 5minutes in simulated intestinal fluid (SIF), and this decomposition was continuous. With the decomposition of the structure of florfenicol hydrogels, the encapsulated florfenicol was also slowly released, and thus, it achieves the slow-release effect. Additionally, the florfenicol hydrogels showed a low hemolytic ratio and greater antibacterial activity compared with florfenicol. The blended formulation creates a promising oral matrix intended for the slow-release of florfenicol along the gastrointestinal tract.

Compounded glucagon-like peptide-1 receptor agonists for weight loss: the direct-to-consumer market in Colorado.

High prices and other access barriers have contributed to the rise of a market for compounded glucagon-like peptide-1 receptor agonists for weight loss in the United States. This market has not been systematically studied. We conducted a pilot study to assess the prevalence, characteristics, and advertising content of direct-to-consumer providers of compounded glucagon-like peptide-1 products for weight loss in Colorado. We conducted a cross-sectional study of websites advertising compounded glucagon-like peptide-1 products for weight loss in Colorado. Websites were identified using Google searches focused on census-defined statistical areas. Searches were conducted between March 21 and April 12, 2024. Data collected from websites included physical addresses, business type, highest reported staff credential, advertised glucagon-like peptide-1 products, whether businesses referred to Food and Drug Administration approval when describing products, and whether businesses referred to products as 'generic'. We identified 93 business websites advertising compounded glucagon-like peptide-1 products for weight loss corresponding to 188 physical locations throughout Colorado. Most businesses were self-categorized as medical/health spas (33/93) or weight loss services (26/93). Advertised products included semaglutide (92/93), tirzepatide (40/93), liraglutide (2/93), and retatrutide (1/93). Advertised combination products included B vitamins (8/93), levocarnitine (1/93), mannitol (1/93), BPC-157 (1/93), and glycine (1/93). Seven websites advertised oral formulations. Additionally, 41/93 websites referred to Food and Drug Administration approval in their descriptions of compounded products and 5/93 referred to products as 'generic'. This study identified several instances of unapproved glucagon-like peptide-1 products being compounded and advertised in Colorado. Additionally, 1 product was advertised as compounded with BPC-157, a substance determined by the Food and Drug Administration to be unsafe for compounding. This study also identified numerous examples of misleading claims regarding the regulatory status of compounded glucagon-like peptide-1 products. Regulatory action is needed to ensure the benefits of compounded GLP-1 products outweigh the risks.

The Role of Intravenous Selexipag in Managing PAH and Bridging Gaps in Oral Treatment: A Narrative Review.

Pulmonary arterial hypertension (PAH) is a rare and potentially fatal condition characterized by progressive increases in blood pressure in the arteries of the lungs. Oral selexipag, approved by the Food and Drug Administration (FDA) in 2015 for the treatment of PAH, targets prostacyclin receptors on pulmonary arterial vascular smooth muscle and endothelial cells to improve blood flow through the lungs and reduce pulmonary vascular resistance. Oral selexipag is effective, but may be discontinued due to factors like side effects, emergency conditions, or inability to take oral medication, potentially leading to severe adverse events, such as rebound pulmonary hypertension and right heart failure. To address treatment interruptions, intravenous (IV) selexipag was introduced as an alternative for patients who are temporarily unable to take oral medications. IV selexipag bypasses hepatic metabolism, requiring a 12.5% higher dose compared to the oral form to achieve similar therapeutic effects. It is administered via IV infusion twice daily over 80minutes, typically for short-term use. However, caution is needed when prescribing selexipag to patients with hepatic or renal issues, and it is contraindicated with strong CYP2C8 inhibitors. A Phase III clinical trial confirmed that switching between oral and IV selexipag was safe, with comparable efficacy and tolerability, though it was limited by small sample size and short duration. Given the risks of treatment interruption and the complexity of managing PAH, this review provides essential insights into the practical use of IV selexipag as a bridging therapy. Furthermore, it calls for larger clinical trials to refine dosing strategies, explore long-term outcomes, and identify patient populations most likely to benefit from IV selexipag.

AMENAMEVIR: A BREAKTHROUGH IN HERPESVIRUS THERAPY

Amenamevir is a promising antiviral agent with strong activity against herpes simplex virus (HSV) and varicella-zoster virus (VZV). This review article aims to explore its pharmacodynamics, therapeutic potential, and safety profile in detail. Amenamevir functions by inhibiting the viral helicase-primase complex, a crucial step in viral DNA replication, distinguishing it from other antiviral drugs. The article examines the results from clinical trials assessing its efficacy in treating recurrent herpesvirus infections, its pharmacokinetic properties, and its suitability for patients with compromised immune systems. We also discuss the drugs safety and tolerability, identifying common side effects, drug interactions, and contraindications. Furthermore, the review highlights Amenamevirs potential role in managing antiviral resistance and its possible broader applications in the treatment of chronic viral infections. Finally, future directions are outlined, including the exploration of combination therapy and the development of more accessible oral formulations, to optimize the clinical use of Amenamevir.