Ascorbic acid in skin health

Ascorbic acid (vitamin C) is a water-soluble vitamin and a recognized antioxidant drug that is used topically in dermatology to treat and prevent the changes associated with photoaging, as well as for the treatment of hyperpigmentation. Ascorbic acid has neutralizing properties of free radicals, being able to interact with superoxide, hydroxyl and free oxygen ions, preventing the inflammatory processes, carcinogens, and other processes that accelerate photoaging in the skin. Current research focuses on the search for stable compounds of ascorbic acid and new alternatives for administration in the dermis. Unlike plants and most animals, humans do not have the ability to synthesize our own ascorbic acid due to the deficiency of the enzyme L-gulono-gamma-lactone oxidase, which catalyzes the passage terminal in the ascorbic acid biosynthesis. To deal with this situation, humans obtain this vitamin from the diet and/or vitamin supplements, thus preventing the development of diseases and achieving general well-being. Ascorbic acid is involved in important metabolic functions and is vital for the growth and maintenance of healthy bones, teeth, gums, ligaments, and blood vessels. Ascorbic acid is a very unstable vitamin and is easily oxidized in aqueous solutions and cosmetic formulations. Ascorbic acid is extensively used as an ingredient in anti-aging cosmetic products, as sodium ascorbate or ascorbyl palmitate. This review discusses and describes the potential roles for ascorbic acid in skin health and their clinical applications (antioxidative, photoprotective, anti-aging, and anti-pigmentary effects) of topical ascorbic acid on the skin and main mechanisms of action. Considering the instability and difficulty in administering ascorbic acid, we also discuss the importance of several factors involved in the formulation and stabilization of their topical preparations in this review.Fil: Ravetti, Soledad. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Centro de Investigaciones y Transferencia de Villa María. Universidad Nacional de Villa María. Centro de Investigaciones y Transferencia de Villa María; ArgentinaFil: Clemente, Camila Mara. Universidad Nacional de Villa María. Instituto Académico Pedagógico de Ciencias Básicas y Aplicadas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Brignone, Sofía Gisella. Universidad Nacional de Villa María. Instituto Académico Pedagógico de Ciencias Básicas y Aplicadas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Hergert, Lisandro Yamil. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Villa María. Instituto Académico Pedagógico de Ciencias Básicas y Aplicadas; ArgentinaFil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentin

Validation of UV-Visible and HPLC method for the determination of sodium p-aminosalicylate and m-aminophenol in a new pharmaceutical formulation

Sodium p-aminosalycilate is an orphan drug used in patients affected with multidrug-resistant Tuberculosis. Two methods, high-performance liquid chromatographic and ultraviolet spectrophotometric for the quantitative determination of sodium p-aminosalycilate and its degradation productm-aminophenol in a new pharmaceutical formulation, powder for extemporaneous reconstitution, were developed in the present work. The parameters linearity, precision, accuracy, specificity, robustness, limit of detection, and limit of quantification were also studied. Chromatography was carried out by reverse-phase technique on an RP-18 column with a mobile phase composed of 50 mM monobasic/dibasic phosphate buffer and methanol (42.5:42.5:15 v/v/v) with 1.9 g of hidroxytetrabutyl ammonium ionic pare adjusted to pH 7.0 with orthophosphoric acid. The ultraviolet spectrophotometric method was performed at 254 nm and 280 nm for quantification of sodium p-aminosalycilate and m-aminophenol, respectively. The proposed methods are highly sensitive, precise, and accurate and can be used for the reliable quantification of sodium p-aminosalycilate in the new alternative formulation. High-performance liquid chromatographic approach demonstrated to be a stability-indicating method, therefore suitable for the investigation of the chemical stability of sodium p-aminosalycilate.Fil: Hergert, Lisandro Yamil. Universidad Nacional de Villa María. Instituto Académico Pedagógico de Ciencias Básicas y Aplicadas; Argentina. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; ArgentinaFil: Ravetti, Soledad. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Centro de Investigaciones y Transferencia de Villa María. Universidad Nacional de Villa María. Centro de Investigaciones y Transferencia de Villa María; ArgentinaFil: Mazzieri, Maria Rosa. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentin

Synthesis of N-benzenesulfonylbenzotriazole derivatives, and evaluation of their antimicrobial activity

A series of benzenesulfonyl compounds, 1a-i, containing a BZT moiety was synthesized and characterized, and their antifungal and antibacterial activities were investigated. Compounds la and 1d showed the highest activity against Escherichia coli ATCC 25922; in addition la presented bactericidal activity against E. coli and Staphylococcus aureus at 8.6 mM. The ability of la to generate superoxide anion (O2-) was measured and it showed more stimuli in S. aureus compared to sulfafhiazole, indicating that 1a can be involved in oxidative stress of bacteria. None of the compounds inhibited the growth of the dermatophytes strains at the tested concentration (250 μg/ml). © 2008 Bentham Science Publishers Ltd.Fil: Hergert, Lisandro Yamil. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; ArgentinaFil: Nieto, Marcelo J.. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina. Southern Illinois University; Estados UnidosFil: Becerra, María Cecilia. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto Multidisciplinario de Biología Vegetal. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas Físicas y Naturales. Instituto Multidisciplinario de Biología Vegetal; ArgentinaFil: Albesa, Inés. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; ArgentinaFil: Mazzieri, Maria Rosa. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentin

Challenges in Protein Formulation Focused on Extrusion-Spheronization Process

Biotechnology revolution had led the overcoming of different types of therapeutic protein because of theirchemical structure can perform specific reactions in the body, increasing efficacy and decreasing side effects.Numerous efforts were made to optimize the physicochemical properties of the proteins used for therapeuticand studied different methods for an effective administration of the protein contained in the medicine,evaluating different routes of administration to achieve the desired therapeutic effects. The delivery systemfor oral pharmaceutical proteins and peptides is still in development stage. There are number of limitationsto oral delivery of proteins such as barriers to peptide bioavailability after oral administration, intestinalmembrane permeability, size, intestinal and hepatic metabolism and solubility. Pellets have shown greatpotential in the delivery of proteins/peptidal drugs. Some strategies of development of oral protein andpeptides has always been challenged, optimizing the safety and efficacy while ensuring the ability tomanufacture the drug while maintaining quality and stability. The pelletization techniques have beenreviewed in numerous papers, is a technique that enables the formation of spherical beads or pellets with amean diameter usually ranging from 0.5-2.0 mm. Pellets are prepared by different techniques, such asextrusion and spheronization. This review discusses challenges in protein formulation that have been used toprepare pelletized dosage forms using the extrusion-spheronization process.Fil: Ravetti, Soledad. Universidad Nacional de Villa María; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Hergert, Lisandro Yamil. Universidad Nacional de Villa María; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Sparo, Mónica Delfina. Universidad Nacional del Centro de la Provincia de Buenos Aires; ArgentinaFil: Sanchez Bruni, Sergio Fabian. Universidad Nacional del Centro de la Provincia de Buenos Aires; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentin

Synthesis, In Vitro Antiprotozoal Activity and Cytotoxicity of New Thymol Carbonate Derivatives

Considering the biological properties of thymol and its derivatives and the urgency of effective drugs for neglected tropical diseases, we report the synthesis of a novel series of carbonates of thymol, using N,N-carbonyldiimidazole and several aliphatic alcohols. The in vitro leishmanicidal, trypanocidal, antiplasmodial and cytotoxic activities of thymol and derivatives were also studied together with the in silico physicochemical and pharmacokinetic properties of synthesized compounds. Both, thymol and carbonate derivatives although were cytotoxic to mammal U-937 cells, they were also highly active against Plasmodium falciparum and Trypanosoma cruzi parasites. When relating the cytotoxicity with antiparasitic activity all compounds, except 1 g and 1 i were more selective against parasites than against the mammal cells. Computational analysis indicates good oral bioavailability for all compounds. Results suggest that thymol and their carbonate derivatives have promising therapeutic potential as antiplasmodial, trypanocidal and leishmanicidal agents; nonetheless further studies are needed to validate their efficacy as antiparasitic drugs in in vivo assays.Fil: Clemente, Camila Mara. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Centro de Investigaciones y Transferencia de Villa María. Universidad Nacional de Villa María. Centro de Investigaciones y Transferencia de Villa María; ArgentinaFil: Ravetti, Soledad. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Centro de Investigaciones y Transferencia de Villa María. Universidad Nacional de Villa María. Centro de Investigaciones y Transferencia de Villa María; ArgentinaFil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Hergert, Lisandro Yamil. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Centro de Investigaciones y Transferencia de Villa María. Universidad Nacional de Villa María. Centro de Investigaciones y Transferencia de Villa María; ArgentinaFil: Pineda, Tatiana. Corporación de Innovación CIDEPRO; ColombiaFil: Robledo, Sara M.. Universidad de Antioquia; Colombi

In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms

Chagas disease is still an important health problem in Central and South America. However, the only drugs currently available for specific treatment of this disease may induce toxic side effects in the host. The aim of this work was to determine the activity of N-benzenesulfonylbenzotriazole (BSBZT) against the protozoan parasite Trypanosoma cruzi. The effects of BSBZT and benzotriazole (BZT) were compared to those of benznidazole (BZL) on epimastigote and trypomastigote forms. BSBZT was found to have an in vitro growth inhibitory dose-dependent activity against epimastigotes, with flow cytometry analysis confirming that the treated parasites presented size reduction. BSBZT showed an IC50 of 21.56 μg/mL (81.07 μM) against epimastigotes at 72 h of incubation, whereas BZT did not affect the growth of this parasite form. Furthermore, the toxic effect of BSBZT, was stronger and appeared earlier (at 24 h) in trypomastigotes than in epimastigotes, with the LC50 of this compound being 28.40 μg/mL (106.79 μM) against trypomastigotes. The concentrations of BSBZT used in this study presented low hemolytic activity and cytotoxicity. Consequently, at concentrations near IC50 and LC50 (25 μg/mL), BSBZT caused only 2.4% hemolysis and 15% of RAW 264.7 cell cytotoxicity. These results reveal the potential of BSBZT as a prototype in drug design for developing new anti-T. cruzi compounds.Fil: Becerra, María Cecilia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinario de Biología Vegetal (p); Argentina. Universidad Nacional de Córdoba; ArgentinaFil: Guiñazú, N.. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones en Bioquímica Clínica e Inmunología; ArgentinaFil: Hergert, Lisandro Yamil. Universidad Nacional de Córdoba; ArgentinaFil: Pellegrini, Andrea Vanina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones En Bioquímica Clínica E Inmunología; ArgentinaFil: Mazzieri, M. R.. Universidad Nacional de Cordoba. Facultad de Ciencias Quimicas. Departamento de Farmacia; ArgentinaFil: Gea, Susana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones En Bioquímica Clínica E Inmunología; ArgentinaFil: Albesa, Inés. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinario de Biología Vegetal (p); Argentina. Universidad Nacional de Córdoba; Argentin