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1.
Pharmaceutics ; 15(4)2023 Mar 24.
Artículo en Inglés | MEDLINE | ID: mdl-37111535

RESUMEN

Plantago major L. is a plant available worldwide that has been traditionally used for several medical applications due to its wound healing, anti-inflammatory, and antimicrobial properties. This work aimed to develop and evaluate a nanostructured PCL electrospun dressing with P. major extract encapsulated in nanofibers for applications in wound healing. The extract from leaves was obtained by extraction in a mixture of water:ethanol = 1:1. The freeze-dried extract presented a minimum inhibitory concentration (MIC) for Staphylococcus Aureus susceptible and resistant to methicillin of 5.3 mg/mL, a high antioxidant capacity, but a low content of total flavonoids. Electrospun mats without defects were successfully produced using two P. major extract concentrations based on the MIC value. The extract incorporation in PCL nanofibers was confirmed using FTIR and contact angle measurements. The PCL/P. major extract was evaluated using DSC and TGA demonstrating that the incorporation of the extract decreases the thermal stability of the mats as well as the degree of crystallinity of PCL-based fibers. The P. major extract incorporation on electrospun mats produced a significant swelling degree (more than 400%) and increased the capacity of adsorbing wound exudates and moisture, important characteristics for skin healing. The extract-controlled release evaluated using in vitro study in PBS (pH, 7.4) shows that the P. major extract delivery from the mats occurs in the first 24 h, demonstrating their potential capacity to be used in wound healing.

2.
Expert Opin Ther Pat ; 33(3): 193-209, 2023 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-36786067

RESUMEN

INTRODUCTION: Chagas disease is a neglected, endemic disease in 21 countries, spreading to non-endemic countries too. Like other neglected diseases affecting primarily low- and middle-income countries, low investment and the absence of new chemical entities from the industry occurred. Increased knowledge about the parasite, drug targets, and vector control has been observed, but this was not translated into new drugs. The partnerships of pharmaceutical companies with academies and consolidated networks to increment the new drugs and treatment research in Chagas disease are shown. The current review analyzes in detail the patents dealing with compounds candidates for new drugs and treatment. The patent search was performed using Orbit Intelligence® software in the 2001-2021 period. AREAS COVERED: The author focused specifically on patents for the treatment, the new candidates disclosed in the patents, and the barriers to innovation. EXPERT OPINION: Patents in Chagas disease have been increasing in the last years, although they do not bring new compounds to an effective treatment.


Asunto(s)
Enfermedad de Chagas , Tripanocidas , Trypanosoma cruzi , Humanos , Patentes como Asunto , Enfermedad de Chagas/tratamiento farmacológico , Enfermedad de Chagas/epidemiología , Enfermedad de Chagas/parasitología , Sistemas de Liberación de Medicamentos , Tripanocidas/farmacología , Tripanocidas/uso terapéutico
3.
Bioorg Med Chem ; 25(5): 1543-1555, 2017 03 01.
Artículo en Inglés | MEDLINE | ID: mdl-28161253

RESUMEN

Trypanosoma cruzi and Leishmania spp. are protozoa of the Trypanosomatidae family, being the etiological agents of two widespread parasitic diseases, Chagas disease and leishmaniasis, respectively. Both parasites are the focus of worldwide research with the aim to find effective and less toxic drugs than the few ones available so far, and for controlling the spread of the diseases. Carbonic anhydrases (CAs, EC 4.2.1.1) belonging to the α- and ß-class were recently identified in these protozoans and several studies suggested that they could be new targets for drug development. Sulfonamide, thiol and hydroxamate inhibitors effectively inhibited the α-CA from T. cruzi (TcCA) and the ß-CA from L. donovani chagasi (LdccCA) in vitro, and some of them also showed in vivo efficacy in inhibiting the growth of the parasites in animal models of Chagas disease and leishmaniasis. As few therapeutic options are presently available for these orphan diseases, protozoan CA inhibition may represent a novel strategy to address this stringent health problem.


Asunto(s)
Antiprotozoarios/farmacología , Anhidrasas Carbónicas/efectos de los fármacos , Leishmania/efectos de los fármacos , Trypanosoma cruzi/efectos de los fármacos , Animales , Anhidrasas Carbónicas/metabolismo , Leishmania/enzimología , Leishmania/crecimiento & desarrollo , Trypanosoma cruzi/enzimología , Trypanosoma cruzi/crecimiento & desarrollo
4.
Am J Primatol ; 68(8): 825-31, 2006 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-16847975

RESUMEN

The purpose of this study was to provide current data on Staphylococcus species from the vaginas of clinically normal captive lion tamarins and to determine the antimicrobial susceptibility of these isolates. Samples were collected from 25 adult lion tamarins, processed to isolate Staphylococcus species, and tested for susceptibility to penicillin G, gentamicin, chloramphenicol, tetracycline, trimethoprim-sulfamethoxazole, streptomycin, ampicillin, and rifampicin. Isolates with the typical characteristics of the genus Staphylococcus were recovered from all 25 samples. Coagulase-negative species were the most common (68% of the isolates), and the most frequently isolated species (10 samples) was S. simulans. Other coagulase-negative species, including S. saprophyticus (n=5), S. epidermidis (n=1), and S. arlettae (n=1), were also recovered. Coagulase-positive Staphylococci were obtained from eight animals (six of from the S. aureus species and two from S. intermedius). Resistance to antibiotics was frequently observed, and 88% of the isolates (23 samples) showed resistance to at least one drug. Resistance to penicillin G was a common finding, and the most active antimicrobial agents were chloramphenicol and gentamicin. Coagulase-positive strains were more frequently resistant to antibiotics (79.7%, average=6.4 drugs) than coagulase-negative strains (38.2%, average=3.0 drugs). The high frequency of resistance observed in those isolates is surprising and very alarming. A detailed history of the use of antimicrobial drugs in these subjects did not reveal any previous exposure to any of the tested antibiotics that could justify the observed resistance rate.


Asunto(s)
Farmacorresistencia Bacteriana Múltiple , Leontopithecus/microbiología , Staphylococcus/efectos de los fármacos , Vagina/microbiología , Ampicilina/farmacología , Animales , Antibacterianos/farmacología , Cloranfenicol/farmacología , Coagulasa/metabolismo , Femenino , Gentamicinas/farmacología , Pruebas de Sensibilidad Microbiana , Penicilina G/farmacología , Rifampin/farmacología , Staphylococcus/clasificación , Staphylococcus/aislamiento & purificación , Estreptomicina/farmacología , Tetraciclina/farmacología , Combinación Trimetoprim y Sulfametoxazol/farmacología
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