Hasil untuk "Pharmacy and materia medica"

Adriana Correra, Alfredo Mauriello, Valeria Cetoretta et al.

<b>Introduction</b>: Semaglutide, a glucagon-like peptide-1 receptor agonist (GLP-1RA), has demonstrated unprecedented efficacy in the treatment of type 2 diabetes mellitus (T2DM) and obesity. However, its rapid clinical widespread use has ignited a debate regarding long-term safety, particularly concerning the risk of specific neoplasms and its ability to modulate cardiovascular health, not only as primary prevention but also as a potential agent to mitigate cardiotoxicity. <b>Objectives</b>: This narrative review aims to analyze the most recent evidence from clinical trials and post-marketing surveillance to evaluate the correlation between semaglutide use and the incidence of cancer, as well as the drug’s efficacy in reducing cardiotoxicity induced by anticancer therapies. <b>Results and Discussion</b>: While preclinical rodent models suggested a link to medullary thyroid carcinoma, human epidemiological data remain reassuring, though caution is advised in patients with genetic predisposition. Regarding pancreatic cancer, current meta-analyses do not confirm a significant increase in risk, suggesting that metabolic benefits outweigh potential concerns. <b>Conclusions</b>: Semaglutide is confirmed as a therapeutic tool with a highly favorable benefit–risk profile. While oncological monitoring must continue, the drug’s cardioprotective and anti-inflammatory properties open new frontiers not only in metabolic management but also in safeguarding cardiovascular integrity in complex clinical scenarios.

Yuheng Wang, Xiaolu Wei, Huijun Wang et al.

M Gunasekaran, Sonali Sharma, Kolla Lakshmiprasanna et al.

Nanotechnology is revolutionizing prosthodontics by enhancing the aesthetics, durability, and functionality of dental restorations. Nanomaterials can mimic the natural appearance of teeth with unprecedented precision, resulting in lifelike and visually appealing prosthetics. Their superior strength and wear resistance extend the longevity of restorations, reducing the need for replacements and lowering costs. Beyond aesthetics and durability, nanomaterials can be engineered with unique properties, such as antibacterial effects and the ability to deliver therapeutic agents, improving oral health and patient comfort. This review explores the current applications and future opportunities of nanotechnology in prosthodontics, offering valuable insights for dental professionals and researchers interested in its transformative potential.

Vundrala Sumedha Reddy, S. Shiva, Srinidhi Manikantan et al.

Caffeine is the world's most popular stimulant and psychoactive substance. Given the ubiquitous use of caffeine, it is crucial for us to comprehend how our body interacts with caffeine. The pharmacokinetics of caffeine and its action mechanisms have been reviewed in this paper. The safety and recommended dosage of caffeine in healthy adults and vulnerable populations like children and pregnant women are also discussed in this paper. While caffeine consumption is generally safe, this review paper also examines the potential effects that caffeine could have on human health and development. Studies indicated that caffeine exhibits neuroprotective properties, potentially serving as a preventive measure against the onset of neurodegenerative conditions such as Alzheimer's and Parkinson's disease. The article also explores various physiological effects of caffeine on the body, in addition to investigating novel drug delivery techniques, particularly nano-delivery systems designed to efficiently administer caffeine.

Citlali Vázquez, Rusely Encalada, Isabel Jiménez-Galicia et al.

Infection with the protozoan parasite <i>Trypanosoma cruzi</i> causes human Chagas disease. Benznidazole (BNZ) and nifurtimox are the current drugs for the treatment; however, they induce severe adverse side effects in patients; therefore, there is a need to improve the treatment effectiveness and efficiency of these drugs for its safer use. <b>Background/Objective</b>: Glyburide, glipizide, and gliquidone, hypoglycemic drugs for diabetes treatment, were previously predicted to bind to dihydrofolate reductase-thymidylate synthase from <i>T. cruzi</i> by in silico docking analysis; they also showed antiproliferative effects against <i>T. cruzi</i> epimastigotes, the stage of the insect vector. In the present study, the potential parasiticidal effect of these antidiabetic drugs was tested in monotherapy and bi-therapy with BNZ in human cells in vitro and in animals. <b>Methods</b>: Evaluation was performed in (a) a model of in vitro infection of <i>T. cruzi</i> trypomastigotes using human fibroblasts as host cells and (b) in mice infected with <i>T. cruzi</i>. <b>Results:</b> The antidiabetic drugs in monotherapy showed antiparasitic effects in preventing infection progression (trypomastigotes release), with an IC₅₀ of 8.4–14.3 µM in comparison to that of BNZ (0.26 µM) in vitro. However, in bi-therapy, the presence of just 0.5 or 1 µM of the antidiabetics decreased the BNZ IC₅₀ by 5–10 times to 0.03–0.05 µM. Remarkably, the antidiabetic drugs in monotherapy decreased the infection in mice by 40–60% in a similar extent to BNZ (80%). In addition, the combination of BNZ plus antidiabetics perturbed the antioxidant metabolites in epimastigotes. <b>Conclusions</b>: These results identified antidiabetics as potential drugs in combination therapy with BNZ to treat <i>T. cruzi</i> infection.

Andrew Auyeung, Hank C. Wang, Kannan Aravagiri et al.

Chronic pain is a pressing medical and socioeconomic issue worldwide. It is debilitating for individual patients and places a major burden on society in the forms of direct medical costs and lost work productivity. Various biochemical pathways have been explored to explain the pathophysiology of chronic pain in order to identify biomarkers that can potentially serve as both evaluators of and guides for therapeutic effectiveness. The kynurenine pathway has recently been a source of interest due to its suspected role in the development and sustainment of chronic pain conditions. The kynurenine pathway is the primary pathway responsible for the metabolization of tryptophan and generates nicotinamide adenine dinucleotide (NAD⁺), in addition to the metabolites kynurenine (KYN), kynurenic acid (KA), and quinolinic acid (QA). Dysregulation of this pathway and changes in the ratios of these metabolites have been associated with numerous neurotoxic and inflammatory states, many of which present simultaneously with chronic pain symptoms. While further studies utilizing biomarkers to elucidate the kynurenine pathway’s role in chronic pain are needed, the metabolites and receptors involved in its processes nevertheless present researchers with promising sources of novel and personalized disease-modifying treatments.

Dongsik Park, Su Jin Lee, Dong Kyu Choi et al.

Tissue engineering is a sophisticated field that involves the integration of various disciplines, such as clinical medicine, material science, and life science, to repair or regenerate damaged tissues and organs. To achieve the successful regeneration of damaged or diseased tissues, it is necessary to fabricate biomimetic scaffolds that provide structural support to the surrounding cells and tissues. Fibrous scaffolds loaded with therapeutic agents have shown considerable potential in tissue engineering. In this comprehensive review, we examine various methods for fabricating bioactive molecule-loaded fibrous scaffolds, including preparation methods for fibrous scaffolds and drug-loading techniques. Additionally, we delved into the recent biomedical applications of these scaffolds, such as tissue regeneration, inhibition of tumor recurrence, and immunomodulation. The aim of this review is to discuss the latest research trends in fibrous scaffold manufacturing methods, materials, drug-loading methods with parameter information, and therapeutic applications with the goal of contributing to the development of new technologies or improvements to existing ones.

Xiaoying Zhang, Wenjing Tang, Haoyu Wen et al.

Lung metastasis of colorectal cancer is common in the clinic; however, precise targeting for the diagnosis and therapy purposes of those lung metastases remains challenging. Herein, cholera toxin subunit b (CTB) protein was chemically conjugated on the surface of PEGylated liposomes (CTB-sLip). Both human-derived colorectal cancer cell lines, HCT116 and HT-29, demonstrated high binding affinity and cellular uptake with CTB-sLip. In vivo, CTB-sLip exhibited elevated targeting capability to the lung metastasis of colorectal cancer in the model nude mice in comparison to PEGylated liposomes (sLip) without CTB modification. CTB conjugation induced ignorable effects on the interaction between liposomes and plasma proteins but significantly enhanced the uptake of liposomes by numerous blood cells and splenic cells, leading to relatively rapid blood clearance in BALB/c mice. Even though repeated injections of CTB-sLip induced the production of anti-CTB antibodies, our results suggested CTB-sLip as promising nanocarriers for the diagnosis of lung metastasis of colorectal cancer.

Hudson Polonini, Sarah Taylor, Clark Zander

The wide variety of potential pathogeneses for alopecia and the wide variety of active pharmaceutical ingredients (APIs) to treat and manage those pathogeneses highlight the importance of the development of stable and effective topical treatments. Topical options for alopecia on the market remain limited and oral products may result in unwanted systemic adverse effects. This study is meant to fill the gap by determining compatibility in terms of beyond-use date (BUD) of APIs with theoretical or demonstrated benefits for topical use for alopecia. The compatibility of seven formulations was tested: F1 = clobetasol 0.05% in TrichoWash^TM; F2 = ketoconazole 2% in TrichoWash^TM; F3 = spironolactone 1% in TrichoWash^TM; F4 = latanoprost 0.1% in TrichoCream^TM; F5 = pyridoxine HCl 0.5%, vitamin A acetate 1%, and vitamin E succinate 12.1 IU in TrichoCond^TM; F6 = Caffeine 2%, menthol 1%, and pyridoxine HCl 0.5% in TrichoWash^TM; F7 = Latanoprost 0.1%, minoxidil 5%, and finasteride 0.25% in TrichoSol^TM. All formulations presented a BUD of 6 months, except for F4 and F7, which showed compatibility for 3 months. This validates the compatibility of the APIs with the Trichotech^TM vehicles, and that they are highly convenient for compounding pharmacies.

Radosław Balwierz, Dawid Bursy, Paweł Biernat et al.

Silica nanoparticles were applied as the carrier of chloramphenicol (2,2-dichloro-<i>N</i>-[(1<i>R</i>,2<i>R</i>)-1,3-dihydroxy-1-(4-nitrophenyl)propan-2-yl]acetamide), and were loaded in a 1% carbopol-based gel (poly(acrylic acid)), which allowed obtainment of an upgraded drug form. The samples of silica materials were obtained by means of modified Stöber synthesis, and their morphological properties were analyzed using Fourier transform infrared spectroscopy (FTIR), Brunauer–Emmett–Teller (BET) method, elemental analysis (EA), thermogravimetric analysis (TGA), analysis of the specific surface properties, X-ray diffraction study (XRD), scanning electron microscope (SEM), and dynamic light scattering (DLS) methods, which permitted the selection of the drug carrier. The two obtained silica carriers were coated with chloramphenicol and loaded into 1% carbopol gel. The release studies were then performed. The release results were evaluated using mathematical models as well as model-independent analysis. It was found that the modification of the synthesis of the silica by the sol-gel method to form a product coated with chloramphenicol and further grinding of the silica material influenced the release of the active substance, thus allowing the modification of its pharmaceutical availability. The change in the parameters of silica synthesis influenced the structure and morphological properties of the obtained silica carrier. The grinding process determined the way of adsorption of the active substance on its surface. The studies showed that the proper choice of silica carrier has a considerable effect on the release profile of the prepared hydrogel formulations.

Tomoaki Kurosaki, Hiroki Kanda, Junya Hashizume et al.

In a previous study, we constructed a lung-targeting lipopolyplex containing polyethyleneimine (PEI), 1,2-di-<i>O</i>-octadecenyl-3-trimethylammonium propane (DOTMA), and <i>N</i>-lauroylsarcosine (LS). The lipopolyplex exhibited an extremely high gene expression in the lung after intravenous administration. Here, we optimized the lipopolyplex and used it to deliver a TGF-β1 shRNA to treat refractory pulmonary fibrosis. We constructed several lipopolyplexes with pDNA, various cationic polymers, cationic lipids, and LS to select the most effective formulation. Then, the pDNA encoding shRNA against mouse TGF-β1 was encapsulated in the lipopolyplex and injected into mice with bleomycin-induced pulmonary fibrosis. After optimizing the lipopolyplex, dendrigraft poly-L-lysine (DGL) and DOTMA were selected as the appropriate cationic polymer and lipid, respectively. The lipopolyplex was constructed with a pDNA, DGL, DOTMA, and LS charge ratio of 1:2:2:4 showed the highest gene expression. After intravenous administration of the lipopolyplex, the highest gene expression was observed in the lung. In the in vitro experiment, the lipopolyplex delivered pDNA into the cells via endocytosis. As a result, the lipopolyplex containing pDNA encoding TGF-β1 shRNA significantly decreased hydroxyproline in the pulmonary fibrosis model mice. We have successfully inhibited pulmonary fibrosis using a novel lung-targeting lipopolyplex.

David J. Lundy, Helen Nguyễn, Patrick C. H. Hsieh

Treatment of brain tumors is challenging since the blood–brain tumor barrier prevents chemotherapy drugs from reaching the tumor site in sufficient concentrations. Nanomedicines have great potential for therapy of brain disorders but are still uncommon in clinical use despite decades of research and development. Here, we provide an update on nano-carrier strategies for improving brain drug delivery for treatment of brain tumors, focusing on liposomes, extracellular vesicles and biomimetic strategies as the most clinically feasible strategies. Finally, we describe the obstacles in translation of these technologies including pre-clinical models, analytical methods and regulatory issues.

Anthony Martin Mena, Morgane Masse, Laura Négrier et al.

Background: In neonatal intensive care units (NICUs), the simultaneous administration of drugs requires complex infusion methods. Such practices can increase the risk of drug incompatibilities resulting in the formation of a particulate load with possible clinical consequences. Methods: This paper evaluates strategies to reduce the particulate load of a protocol commonly used in NICUs with a potential medical incompatibility (vancomycin/cefepime combination). The protocol was reproduced in the laboratory and the infusion line directly connected to a dynamic particle counter to evaluate the particulate matter administered during infusion. A spectrophotometry UV assay of cefepime evaluated the impact of filters on the concentration of cefepime administered. Results: A significant difference was observed between the two infusion line configurations used in the NICU, with higher particulate load for cefepime infused via the emergency route. There was no change in particulate load in the absence of vancomycin. A filter on the emergency route significantly reduced this load without decreasing the cefepime concentration infused. Preparation of cefepime seemed to be a critical issue in the protocol as the solution initially contained a high level of particles. Conclusion: This study demonstrated the impact of a reconstitution method, drug dilution and choice of infusion line configuration on particulate load.

Dawid Groth, Izabela Poplawska, Marlena Tynecka et al.

The management of hard-to-heal wounds is a significant clinical challenge. Acellular dermal matrices (ADMs) have been successfully introduced to enhance the healing process. Here, we aimed to develop protocol for the preparation of novel ADMs from abdominoplasty skin. We used three different decellularization protocols for skin processing, namely, 1M NaCl and sodium dodecyl sulfate (SDS, in ADM1); 2M NaCl and sodium dodecyl sulfate (SDS, in ADM1); and a combination of recombinant trypsin and Triton X-100 (in hADM 3). We assessed the effectiveness of decellularization and ADM’s structure by using histochemical and immunochemical staining. In addition, we evaluated the therapeutic potential of novel ADMs in a murine model of wound healing. Furthermore, targeted transcriptomic profiling of genes associated with wound healing was performed. First, we found that all three proposed methods of decellularization effectively removed cellular components from abdominoplasty skin. We showed, however, significant differences in the presence of class I human leukocyte antigen (HLA class I ABC), Talin 1/2, and chondroitin sulfate proteoglycan (NG2). In addition, we found that protocols, when utilized differentially, influenced the preservation of types I, III, IV, and VII collagens. Finally, we showed that abdominoplasty skin-derived ADMs might serve as an effective and safe option for deep wound treatment. More importantly, our novel dressing (ADM1) improves the kinetics of wound closure and scar maturation in the proliferative and remodeling phases of wound healing. In conclusion, we developed a protocol for abdominoplasty skin decellularization suitable for the preparation of biological dressings. We showed that different decellularization methods affect the purity, structure, and therapeutic properties of ADMs.

Nurain Thomas, Agus Rusdin, Madania Tulsyahra et al.

Jatropha sap (JTS), an important fluid carried in xylem and phloem tubes of Jatropha multifida L. plant, has good wound healing property. However, physicochemical stability of JTS needs to be improved in order for it to be useful as a topical wound-healing agent. In this study, we developed an iota carrageenan-polyvinyl alcohol (IC-PVA) hydrogel film (HF) as a carrier of JTS and evaluated its wound-healing ability. The characterization of JTS secondary metabolites by ultraviolet-Vis spectrophotometry suggested presence of flavonoid, saponin, and alkaloids in the sap. We successfully extracted IC from Euchima spinosum using alkaline solvent at 80°C–90°C with calcium chloride as the precipitator. The result of computer simulation using Discovery Studio software and Autodock Tools showed the presence of hydrogen bonding interaction of IC-PVA. IC-PVA/JTS HF with excellent physical properties including high swelling ratio (246.32%) and high gel fraction (16.75%). In addition, irritation test in mice confirmed the absence of hypersensitivity reaction, redness, and allergic reactions. Interestingly, IC-PVA/JTS HF significantly accelerated wound healing when compared to the nontreated group/control with 98% wound closure by 10 days. These results suggest that IC-PVA HF has improves wound-healing ability of JTS.

Dominique Jasmin Lunter, Rolf Daniels

Already in ancient times, semisolid preparations for cutaneous application, popularly known as ointments, played an important role in human society [...]

E. K. Mikhal’chenko, K. V. Аleksandrova, S. V. Levich et al.

Introduction. Synthetic research of new biologically active compounds occupies an important place in modern pharmaceutical science.Thus it is important to develop techniques for the biologically active substances functionalization. Esters and amides take special place among the variety of functional derivatives of organic acids,. These fragments are well-known pharmacophores and could be found in a wide range of drugs. Thus, the nootropic agent pyracetam is 2-oxo-1-pyrolidineacetamide, and is the selective antagonist of β-adrenoreceptores; atenolol is a derivative of benzeneacetamide. Substituted acetamide and ester fragments are also present in the structures of aprofen, spasmolitin, acetylidine and β-lactam cephalosporins and penicillins antibiotics.Aim of our research was the synthetic method development for functional derivatives of 3-benzyl-8-propylxanthinyl-7-acetic acid and the study of their physical-chemical properties. Materials and methods. Melting points were determined using capillary method on DMP (M). 1Н NMR-spectra were recorded by Varian Mercury VX-200 device (company «Varian» – USA) solvent – (DMSO-d6), internal standard – ТМS. Elemental analysis of obtained compounds was produced on device Elementar Vario L cube. Chemical shifts were reported in ppm (parts per million) values. Infrared (IR) spectra were measured on a Bruker Alpha instrument using a potassium bromide (KBr) disk, scanning from 400 to 4000 cm-1. Results and discussion. We selected 3-benzyl-8-propylxanthinyl-7-acetic acid as initial compound for our study. For synthesis of hexyl, heptyl, octyl, nonyl, decyl and benzyl esters of 3-benzyl-8-propylxanthinyl-7-acetic acid we used alternative method, that included alkylation of sodium salts of acids with alkyl halogens. Reaction was made at DMF medium by reflux of reagents. Next stage of our research was the synthesis of amides of 3-beznyl-8-propylxanthinyl-7-acetic acid by the reaction of ethyl or propyl esters with butylamine, benzylamine, p-methylbenzylamine or p-fluorobenzylamine. It should be noted that we conducted reaction without solvent in the medium of amine and reagents were not reflux but heated at 80 оС. The structures of all obtained compounds were proved by the elemental analysis, IR- and 1H NMR-spectroscopy. Conclusions. Obtained results of our work can be used for further search of biological active compounds among functional derivatives of xanthinyl-7-alkanyl acids xanthines; organic synthesis; IR-spectroscopy; NMR-spectroscopy

Galla Narsing Rao

Stevia leaf powder (SLP) and a commercial stevioside powder (CSP) were analysed for their polyphenol content, isothermal sorption behavior and their antioxidant activity was evaluated by DPPH radical scavenging activity, ferric reducing power and ABTS assay. Polyphenol contents were higher (5.6%) in SLP than in CSP (2.3%). It was observed that the SLP was non-hygroscopic and CSP was hygroscopic in nature as seen from sorption isotherms. The equilibrium relative humidity of SLP and CSP respectively was 62 and 24%. The antioxidant activity of the methanolic extracts were determined and DPPH radical scavenging activity for SLP showed 30.33% for 20 µg/ml and 52.46% inhibition at 100 µg/ml, which were slightly higher compared to CSP stevioside, which showed 29.5% and 47.64% inhibition for similar concentrations.Higher ferric reducing power was seen in CSP (0.632) than SLP (0.166) for 100 µg.The antioxidant activity measured by ABTS assay also indicated higher activity (37.5% inhibition for10 µg/ml) for SLP than CSP (39.66% for 40 µg/ml).