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1.
J Cosmet Laser Ther ; 25(5-8): 95-101, 2023 Nov 17.
Artículo en Inglés | MEDLINE | ID: mdl-38032251

RESUMEN

This study evaluated the effects of laser application of diverse wavelengths applied simultaneously and on different skins. The sample included two participants, a woman with light skin with abdominal hair and a woman with dark skin and hair on the inner part of the lower limbs, who received a laser therapy session. After 45 days from laser application, abdominoplasty and thigh dermolipectomy surgery were performed. In the control sample, the hair follicles were in the anagen phase, showing the presence of Bcl-2 expression. In the treated areas, follicles were observed in an advanced phase (telogen), with the presence of CK-18 and negativity of Bcl-2, highlighting the phase of hair loss at that moment and the complete apoptosis of the investigated follicle. Significant difference was observed in the comparison of the anagen phase (p = .00) and it similarly occurred in the comparison of the telogen phase (p = .00). The presence of a greater amount of follicles in the anagen phase in the control area and follicles in the telogen phase in the treated area demonstrates the efficiency of the laser at different wavelengths when reaching different skin phototypes and hair thickness, being reinforced by apoptosis and cell proliferation markers. Therefore, the hair-removal process has been optimized with various laser wavelengths.


Asunto(s)
Remoción del Cabello , Femenino , Humanos , Cabello , Piel , Folículo Piloso , Rayos Láser , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo
2.
Curr Neuropharmacol ; 2023 Sep 20.
Artículo en Inglés | MEDLINE | ID: mdl-37811654

RESUMEN

Zolpidem is a non-benzodiazepine hypnotic drug that works as a positive modulator of Gamma-Amino Butyric Acid-A (GABA-A) receptors, with high selectivity for α1 subunits. Given this selective binding, the drug has a strong hypnotic activity. Social isolation during the SARS-CoV-2 pandemic has contributed to increased rates of anxiety, depression, and insomnia. As a result, studies have pointed to a possible increase in the indiscriminate use of drugs with sedative effects, such as Zolpidem, during the pandemic. The aim of this work was to present prospective evidence that warns of the possibility of the abusive use of Zolpidem even after the pandemic. High rates of addiction to this drug have been reported around the world after the emergence of the coronavirus. Data from the National Survey on Drug Use and Health and from Medicaid support the continuing growth in prescription and indiscriminate use of Zolpidem during the pandemic and afterward. Therefore, there is enough evidence to support the indiscriminate use of this drug since the beginning of the pandemic. Rates of indiscriminate use of sedatives may continue to increase in the post-pandemic period, especially if strict control measures are not taken by health authorities.

3.
Int J Mol Sci ; 24(13)2023 Jul 07.
Artículo en Inglés | MEDLINE | ID: mdl-37446369

RESUMEN

With the advancement of in vivo studies and clinical trials, the pathogenesis of neurodegenerative diseases has been better understood. However, gaps still need to be better elucidated, which justifies the publication of reviews that explore the mechanisms related to the development of these diseases. Studies show that vitamin E supplementation can protect neurons from the damage caused by oxidative stress, with a positive impact on the prevention and progression of neurodegenerative diseases. Thus, this review aims to summarize the scientific evidence of the effects of vitamin E supplementation on neuroprotection and on neurodegeneration markers in experimental models. A search for studies published between 2000 and 2023 was carried out in the PubMed, Web of Science, Virtual Health Library (BVS), and Embase databases, in which the effects of vitamin E in experimental models of neurodegeneration were investigated. A total of 5669 potentially eligible studies were identified. After excluding the duplicates, 5373 remained, of which 5253 were excluded after checking the titles, 90 articles after reading the abstracts, and 11 after fully reviewing the manuscripts, leaving 19 publications to be included in this review. Experiments with in vivo models of neurodegenerative diseases demonstrated that vitamin E supplementation significantly improved memory, cognition, learning, motor function, and brain markers associated with neuroregeneration and neuroprotection. Vitamin E supplementation reduced beta-amyloid (Aß) deposition and toxicity in experimental models of Alzheimer's disease. In addition, it decreased tau-protein hyperphosphorylation and increased superoxide dismutase and brain-derived neurotrophic factor (BDNF) levels in rodents, which seems to indicate the potential use of vitamin E in preventing and delaying the progress of degenerative lesions in the central nervous system.


Asunto(s)
Enfermedad de Alzheimer , Enfermedades Neurodegenerativas , Humanos , Vitamina E/farmacología , Vitamina E/uso terapéutico , Enfermedades Neurodegenerativas/tratamiento farmacológico , Enfermedad de Alzheimer/tratamiento farmacológico , Cognición/fisiología , Modelos Teóricos
4.
Nutrients ; 15(11)2023 May 27.
Artículo en Inglés | MEDLINE | ID: mdl-37299465

RESUMEN

INTRODUCTION: Neurodegenerative diseases are characterized by neuronal dysfunction and death. Studies suggest that some seed extracts have a neuroprotective effect. Considering the increased incidence of these diseases and the need for new effective therapies with fewer side effects, this review aimed to assess the evidence of the efficacy and safety of seed extracts in experimental models of neurodegeneration. MATERIAL AND METHOD: The search was carried out through studies published between 2000 and 2021 in Science Direct, PubMed, Scientific Electronic Library Online (SciELO), and Latin American Literature in Health Sciences (LILACS) databases, in which the effects of seed extracts in in vitro and in vivo experimental models of neurodegeneration were investigated. Based on the eligibility criteria, 47 studies were selected for this review. RESULTS: In the in vitro models, the neuroprotection of the seed extracts was a result of their antioxidant, anti-inflammatory, and anti-apoptotic properties. In the in vivo models, neuroprotection resulted from the antioxidant and anti-inflammatory properties, a decrease in motor deficits, an improvement in learning and memory, as well as the increased release of neurotransmitters. The results show promise for the future of clinical research on new therapies for neurodegenerative diseases. However, the studies are still limited, which does not allow us to extrapolate the results to human beings with ND. CONCLUSIONS: Therefore, clinical trials are needed in order to prove the results of the in vitro and in vivo studies, as well as to assess the ideal, safe, and effective dose of these seed extracts in patients with neurodegenerative diseases.


Asunto(s)
Enfermedades Neurodegenerativas , Fármacos Neuroprotectores , Humanos , Neuroprotección , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/uso terapéutico , Antiinflamatorios , Enfermedades Neurodegenerativas/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
5.
Front Glob Womens Health ; 2: 602572, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34816177

RESUMEN

The new coronavirus (SARS-Cov-2) was first identified in late 2019 as the new RNA virus in the coronaviridae family responsible for causing COVID-19 in the residents of China's Hubei province. In mid-March 2020 WHO declared the pandemic caused by this virus as a result of thousands of people infected all over the world. Epidemiological evidence obtained from other pandemics, such as influenza and ebola, suggest that pregnant women are more susceptible to serious complications and death from viral infection. Physiological changes in the anatomical structure of the respiratory system as well as in the immune system during the pregnancy-puerperal period seem to contribute to this greater risk. Thus, pregnant women are more susceptible to be infected by the SARS-COV-2 or other viruses and to have serious COVID-19 disease. In fact, COVID-19 can alter immune responses at the maternal-fetal interface, affecting the well-being of both mother and her fetus. There is still no sufficient evidence in the literature to support the occurrence of vertical transmission and through breastfeeding, but the prevalence of prematurity was high among pregnant women infected by SARS-Cov-2. In this review, the changes in the immune system that may increase susceptibility to SARS-Cov-2 are discussed as well as the possible mechanisms involved in the transmission of the virus to the fetus by vertical transmission and during breastfeeding.

6.
Front Nutr ; 8: 685317, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34150830

RESUMEN

This review covers current knowledge of selenium in the dietary intake, its bioavailability, metabolism, functions, biomarkers, supplementation and toxicity, as well as its relationship with diseases and gut microbiota specifically on the symbiotic relationship between gut microflora and selenium status. Selenium is essential for the maintenance of the immune system, conversion of thyroid hormones, protection against the harmful action of heavy metals and xenobiotics as well as for the reduction of the risk of chronic diseases. Selenium is able to balance the microbial flora avoiding health damage associated with dysbiosis. Experimental studies have shown that inorganic and organic selenocompounds are metabolized to selenomethionine and incorporated by bacteria from the gut microflora, therefore highlighting their role in improving the bioavailability of selenocompounds. Dietary selenium can affect the gut microbial colonization, which in turn influences the host's selenium status and expression of selenoproteoma. Selenium deficiency may result in a phenotype of gut microbiota that is more susceptible to cancer, thyroid dysfunctions, inflammatory bowel disease, and cardiovascular disorders. Although the host and gut microbiota benefit each other from their symbiotic relationship, they may become competitors if the supply of micronutrients is limited. Intestinal bacteria can remove selenium from the host resulting in two to three times lower levels of host's selenoproteins under selenium-limiting conditions. There are still gaps in whether these consequences are unfavorable to humans and animals or whether the daily intake of selenium is also adapted to meet the needs of the bacteria.

7.
Curr Neuropharmacol ; 19(10): 1738-1759, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33882807

RESUMEN

BACKGROUND: Neural cells undergo functional or sensory loss due to neurological disorders. In addition to environmental or genetic factors, oxidative stress is a major contributor to neurodegeneration. In this context, there has been a growing interest in investigating the effects of EOs (EOs) in recent years, especially in the treatment of neuropathologies. The chemical and biological effects of EOs have led to important treatment tools for the management of various neurological disorders. OBJECTIVE: In the present study we performed a systematic review that sought to comprehend the neuroprotective effects of different EOs. METHOD: This work is a systematic review where an electronic search was performed on PubMed, ScienceDirect, Cochrane Library and SciELO (Scientific Electronic Library Online) databases, covering the last 10 years, using "Essential oil" and "Neuroprotective effect" as reference terms. RESULTS: A total of 9 articles were identified, in which the efficacy of EOs was described in experimental models of anxiety, dementia, oxidative stress, cerebral ischemia, Alzheimer's disease, and oxidative toxicity. CONCLUSION: EOs from different species of medicinal plants have shown positive responses in neurological disorders such as anxiety, dementia, oxidative stress, cerebral ischemia, and oxidative toxicity. Thus, EOs emerges with the potential to be used as alternative agents in the treatment of neurological disorders.


Asunto(s)
Enfermedad de Alzheimer , Fármacos Neuroprotectores , Aceites Volátiles , Enfermedad de Alzheimer/tratamiento farmacológico , Humanos , Modelos Teóricos , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/uso terapéutico , Aceites Volátiles/farmacología , Estrés Oxidativo
8.
Front Med (Lausanne) ; 7: 546, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33043030

RESUMEN

The pandemic caused by the new coronavirus (SARS-Cov-2) has encouraged numerous in vitro studies and clinical trials around the world, with research groups testing existing drugs, novel drug candidates and vaccines that can prevent or treat infection caused by this virus. The urgency for an effective therapy is justified by the easy and fast viral transmission and the high number of patients with severe respiratory distress syndrome who have increasingly occupied intensive care hospital beds, leading to a collapse in health systems in several countries. However, to date, there is no sufficient evidence of the effectiveness of any researched therapy. The off-label or compassionate use of some drugs by health professionals is a reality in all continents, whose permission by regulatory agencies has been based on the results of some clinical trials. In order to guide decision-making for the treatment of COVID-19, this review aims to present studies and guidelines on the main therapies that have been and are currently being tested against SARS-CoV-2 and to critically analyze the reported evidences.

9.
Carbohydr Polym ; 248: 116724, 2020 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-32919548

RESUMEN

In this study, the ability of different beta-cyclodextrins to facilitate homogeneous dispersion of triamcinolone acetonide (TA) into chitosan membranes is assessed. Drug loading was assessed through atomic force microscopy (AFM), scanning electron microscopy (MEV-FEG), and X-ray diffraction analyses. Drug interactions with the co-polymer were investigated with Fourier transform infrared spectroscopy, thermal analyses. Swelling assay, and in vitro drug release experiment were used to assess TA release behavior. Undispersed particles of drug were observed to remain in the simple chitosan membranes. Hydroxypropyl-ß-cyclodextrin enabled the dispersion of TA into chitosan membranes and subsequent sustained drug release. In addition, the membrane performance as a drug delivery device is improved by adding specified amounts of the co-solvent triethanolamine. The experimental data presented in this study confirm the utility of our novel and alternative approach for obtaining a promising device for slow and controlled release of glucocorticoids, such as triamcinolone acetonide, for topical ulcerations.


Asunto(s)
Corticoesteroides/administración & dosificación , Quitosano/química , Preparaciones de Acción Retardada/administración & dosificación , Sistemas de Liberación de Medicamentos/métodos , Liberación de Fármacos , beta-Ciclodextrinas/química , Corticoesteroides/química , Corticoesteroides/farmacocinética , Química Farmacéutica/métodos , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética , Glucocorticoides/administración & dosificación , Glucocorticoides/química , Glucocorticoides/farmacocinética , Membranas Artificiales , Microscopía de Fuerza Atómica , Microscopía Electrónica de Rastreo , Polímeros/química , Solubilidad , Solventes/química , Espectroscopía Infrarroja por Transformada de Fourier , Triamcinolona/administración & dosificación , Triamcinolona/química , Triamcinolona/farmacocinética , Difracción de Rayos X
10.
Pharmaceutics ; 12(4)2020 Apr 21.
Artículo en Inglés | MEDLINE | ID: mdl-32326277

RESUMEN

A variety of neuroactive flavonoids can be found in the species of the Passiflora genus; however, their difficulty in crossing the blood-brain barrier limits their in vivo neuropharmacological activity. In this study, cationic nanoparticles were developed as a novel nanocarrier for improving the antidepressant activity of Passiflora edulis f. flavicarpa leaf extract. Formulations obtained using Eudragit E PO polymethylmethacrylate copolymer, as polymeric matrix had their physicochemical properties investigated. The analytical content of the flavonoids vicenin-2, orientin, isoorientin, vitexin, and isovitexin was determined in the plant extract. Small-sized and spherical nanoparticles loaded with Passiflora edulis f. flavicarpa were obtained with positive zeta potential and high encapsulation efficiency. In addition, the nanosystems were shown to be stable for at least 6 months. The antidepressant activity of P. edulis extract (50 and 100 mg/kg) as well as the extract-loaded nanoparticles (5 mg/kg) were investigated in mice using the forced swimming test, where the latter increased the potency of the former by 10-fold. In addition, histopathological and biochemical analysis confirmed the biocompatibility of the extract-loaded nanoparticles. This study demonstrated that the Eudragit cationic nanoparticles were able to improve the antidepressant activity of P. edulis in the central nervous system of mice.

11.
Polymers (Basel) ; 11(7)2019 Jul 02.
Artículo en Inglés | MEDLINE | ID: mdl-31269671

RESUMEN

Cellulose is among the top 5 excipients used in the pharmaceutical industry. It has been considered one of the main diluents used in conventional and modern dosage forms. Therefore, different raw materials of plant origin have been evaluated as potential alternative sources of cellulose. In this context, Opuntia ficus-indica L. Miller (palma forrageira), a plant of the cactus family that has physiological mechanisms that provide greater productivity with reduced water requirements, is an interesting and unexplored alternative for extracting cellulose. By using this source, we aim to decrease the extraction stages and increase the yields, which might result in a decreased cost for the industry and consequently for the consumer. The aim of this work was to investigate the use of Opuntia ficus-indica L. Miller as a new source for cellulose extraction, therefore providing an efficient, straight forward and low-cost method of cellulose II production. The extraction method is based on the oxidation of the lignins. The obtained cellulose was identified and characterized by spectroscopic methods (FTIR and NMR), X-ray diffraction, thermal analysis (TGA-DTG and DSC) and scanning electron microscopy. The results confirmed the identity of cellulose and its fibrous nature, which are promising characteristics for its use in the industry and a reasonable substrate for chemical modifications for the synthesis of cellulose II derivatives with different physicochemical properties that might be used in the production of drug delivery systems and biomaterials.

12.
Biomolecules ; 9(6)2019 06 21.
Artículo en Inglés | MEDLINE | ID: mdl-31234312

RESUMEN

α, ß amyrin (ABAM) is a natural mixture of pentacyclic triterpenes that has a wide range of biological activities. ABAM is isolated from the species of the Burseraceae family, in which the species Protium is commonly found in the Amazon region of Brazil. The aim of this work was to develop inclusion complexes (ICs) of ABAM and ß-cyclodextrin (ßCD) and hydroxypropyl-ß-cyclodextrin (HPßCD) by physical mixing (PM) and kneading (KN) methods. Interactions between ABAM and the CD's as well as the formation of ICs were confirmed by physicochemical characterization in the solid state by Fourier transform infrared (FTIR), scanning electron microscopy (SEM), X-ray diffraction (XRD), thermogravimetry (TG) and differential scanning calorimetry (DSC). Physicochemical characterization indicated the formation of ICs with both ßCD and HPßCD. Such ICs were able to induce changes in the physicochemical properties of ABAM. In addition, the formation of ICs with cyclodextrins showed to be an effective and promising alternative to enhance the anti-inflammatory activity and safety of ABAM.


Asunto(s)
2-Hidroxipropil-beta-Ciclodextrina/química , 2-Hidroxipropil-beta-Ciclodextrina/farmacología , Antiinflamatorios/química , Antiinflamatorios/farmacología , Ácido Oleanólico/análogos & derivados , Animales , Línea Celular , Supervivencia Celular/efectos de los fármacos , Lipopolisacáridos/farmacología , Macrófagos/citología , Macrófagos/efectos de los fármacos , Ratones , Ácido Oleanólico/química , Solubilidad
13.
Toxicon ; 164: 1-9, 2019 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-30902683

RESUMEN

Scorpion envenomation has been considered a public health issue around the world. Tityus serrulatus represents a specie of major medical importance in Brazil due to mortality rates of approximately 1% among children and elderly populations. The aim of this work was to evaluate the in vivo anti-inflammatory potential of aqueous extract from Hancornia speciosa fruits, its fractions and its phenolic compounds against T. serrulatus envenomation. After receiving the T. serrulatus venom (TsV, 0.8 mg/kg) intraperitoneally, the animals were treated intravenously with the aqueous extract (20, 30 and 40 mg/kg), the arachnid antivenom (50 µL/animal), the dichloromethane, ethyl acetate and n-butanol fractions (20 mg/kg) as well as rutin and chlorogenic acid (2, 2.5 and 5 mg/kg). The treatment with the aqueous extract, fractions and phenolic compounds decreased the migration of leukocytes to the peritoneal cavity and reduced the levels of IL-1ß, IL-6 and IL-12. Moreover, the pulmonary histopathologic analysis showed a reduction in both interstitial and alveolar edema, as well as in the leukocytes infiltration and vascular ectasia in the mice's lungs, which evidences a protective effect attributed to H. speciosa. This is the first study that demonstrates the inhibitory potential of the aqueous extract from H. speciosa fruits against inflammation induced by TsV. These findings suggest that the bioactive compounds from the aqueous extract, especially chlorogenic acid and rutin, are responsible for the reported anti-inflammatory activity of H. speciosa.


Asunto(s)
Antiinflamatorios/farmacología , Apocynaceae/química , Fenoles/farmacología , Extractos Vegetales/farmacología , Neumonía/tratamiento farmacológico , Venenos de Escorpión/toxicidad , Animales , Antiinflamatorios/uso terapéutico , Antivenenos/farmacología , Movimiento Celular , Ácido Clorogénico/farmacología , Femenino , Frutas/química , Leucocitos/efectos de los fármacos , Leucocitos/fisiología , Pulmón/efectos de los fármacos , Pulmón/patología , Masculino , Ratones Endogámicos BALB C , Fenoles/uso terapéutico , Extractos Vegetales/uso terapéutico , Neumonía/inducido químicamente , Neumonía/patología , Edema Pulmonar/inducido químicamente , Edema Pulmonar/tratamiento farmacológico , Edema Pulmonar/patología , Rutina/farmacología
14.
Curr Neuropharmacol ; 17(5): 406-421, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-29338678

RESUMEN

BACKGROUND: The formation of senile plaques and neurofibrillary tangles of the tau protein are the main pathological mechanism of Alzheimer's disease (AD). Current therapies for AD offer discrete benefits to the clinical symptoms and do not prevent the continuing degeneration of neuronal cells. Therefore, novel therapeutic strategies have long been investigated, where curcumin (Curcuma longa) has shown some properties that can prevent the deleterious processes involved in neurodegenerative diseases. OBJECTIVE: The aim of the present work is to review studies that addressed the effects of curcumin in experimental models (in vivo and in vitro) for AD. METHOD: This study is a systematic review conducted between January and June 2017, in which a consultation of scientific articles from indexed periodicals was carried out in Science Direct, United States National Library of Medicine (PubMed), Cochrane Library and Scielo databases, using the following descriptors: "Curcuma longa", "Curcumin" and "Alzheimer's disease". RESULTS: A total of 32 studies were analyzed, which indicated that curcumin supplementation reverses neurotoxic and behavioral damages in both in vivo and in vitro models of AD. CONCLUSION: The administration of curcumin in experimental models seems to be a promising approach in AD, even though it is suggested that additional studies must be conducted using distinct doses and through other routes of administration.


Asunto(s)
Enfermedad de Alzheimer/tratamiento farmacológico , Curcumina/administración & dosificación , Fármacos Neuroprotectores/administración & dosificación , Extractos Vegetales/administración & dosificación , Enfermedad de Alzheimer/metabolismo , Enfermedad de Alzheimer/patología , Enfermedad de Alzheimer/prevención & control , Péptidos beta-Amiloides/metabolismo , Animales , Curcuma/química , Curcumina/farmacología , Suplementos Dietéticos , Humanos , Ovillos Neurofibrilares/metabolismo , Fármacos Neuroprotectores/farmacología , Extractos Vegetales/farmacología , Ensayos Clínicos Controlados Aleatorios como Asunto
15.
Molecules ; 23(12)2018 Nov 29.
Artículo en Inglés | MEDLINE | ID: mdl-30501061

RESUMEN

The novel 2-aminothiophene derivative 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile (6CN) has shown potential anti-proliferative activity in human cancer cell lines. However, the poor aqueous solubility of 6CN impairs its clinical use. This work aimed to develop binary 6CN-ß-cyclodextrin (ßCD) systems with the purpose of increasing 6CN solubility in water and therefore, to improve its pharmacological activity. The 6CN-ßCD binary systems were prepared by physical mixing, kneading and rotary evaporation methods and further characterized by FTIR, XRD, DSC, TG and SEM. In addition, molecular modeling and phase solubility studies were performed. Finally, MTT assays were performed to investigate the cytostatic and anti-proliferative effects of 6CN-ßCD binary systems. The characterization results show evident changes in the physicochemical properties of 6CN after the formation of the binary systems with ßCD. In addition, 6CN was associated with ßCD in aqueous solution and the solid state, which was confirmed by molecular modeling and the aforementioned characterization techniques. Phase solubility studies indicated that ßCD forms stable 1:1 complexes with 6CN. The MTT assay demonstrated the cytostatic and anti-proliferative activities of 6CN-ßCD binary systems and therefore, these might be considered as promising candidates for new anticancer drugs.


Asunto(s)
Tiofenos/farmacología , beta-Ciclodextrinas/química , Rastreo Diferencial de Calorimetría , Muerte Celular/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Humanos , Simulación del Acoplamiento Molecular , Transición de Fase , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier , Termogravimetría , Difracción de Rayos X
16.
Drug Dev Ind Pharm ; 44(5): 750-756, 2018 May.
Artículo en Inglés | MEDLINE | ID: mdl-29206496

RESUMEN

ß-lapachone (ßlap) has shown potential use in various medical applications. However, its poor solubility has limited its systemic administration and clinical applications. The aim of this work is to develop solid dispersions of ßlap using poly (ethylene glycol) (PEG 6000) and polyvinylpyrrolidone (PVP K30) as hydrophilic polymers and evaluate the dissolution rate in aqueous medium. Solid dispersions were prepared by solvent evaporation method using different weight ratios of ßlap and hydrophilic polymer (1:1, 1:2, and 1:3). Characterization performed by differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy showed that ßlap was molecularly dispersed within the polymer matrix. The in vitro dissolution tests showed an enhancement in the dissolution profile of ßlap as solid dispersions prepared in both PVP and PEG, although the former showed better results. The drug:polymer ratio influenced ßlap dissolution rate, as higher amounts of hydrophilic polymer led to enhanced drug dissolution. Thus, this study demonstrated that solid dispersions of ßlap in PVP offers an effective way to overcome the poor dissolution of ßlap.


Asunto(s)
Naftoquinonas/química , Naftoquinonas/síntesis química , Polietilenglicoles/química , Polímeros/química , Povidona/química , Rastreo Diferencial de Calorimetría , Interacciones Hidrofóbicas e Hidrofílicas , Microscopía Electrónica de Rastreo , Solubilidad , Solventes , Espectroscopía Infrarroja por Transformada de Fourier , Difracción de Rayos X
17.
Biomed Pharmacother ; 97: 870-879, 2018 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-29136763

RESUMEN

Hecogenin acetate (HA) is an acetylated sapogenin that has shown potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors. However, HA exhibits poor aqueous solubility, which may limit its application. This study aims to develop amorphous solid dispersions (ASD) using five hydrophilic polymers, to characterize them and to evaluate their antihyperalgesic activity. Physicochemical characterization was performed by X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and Fourier Transformed Infrared (FTIR) spectroscopy. In order to evaluate the hyperalgesia of the ASD, sciatic nerve crush injury (NCI) was induced in mice followed by administration of the ASD, where three parameters were evaluated: mechanical and thermal hyperalgesia as well as grip strength. XRD and SEM showed that ASD of HA with HPMC obtained by kneading (KND) presented an amorphous profile, unlike the others polymers, indicating interaction between HA and HPMC. FTIR analysis evidenced the strong interaction between HA and HPMC. Although the results of mechanical hyperalgesia were slightly improved on the groups treated with ASD of HA with HPMC, the thermal hyperalgesia showed that the incorporation of HA into HPMC matrix significantly improved its antinociceptive activity.


Asunto(s)
Analgésicos/farmacología , Hiperalgesia/tratamiento farmacológico , Neuralgia/tratamiento farmacológico , Compuestos de Espiro/farmacología , Esteroides/farmacología , Analgésicos/administración & dosificación , Analgésicos/química , Animales , Química Farmacéutica/métodos , Modelos Animales de Enfermedad , Interacciones Hidrofóbicas e Hidrofílicas , Masculino , Ratones , Microscopía Electrónica de Rastreo , Polímeros/química , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier , Compuestos de Espiro/administración & dosificación , Compuestos de Espiro/química , Esteroides/administración & dosificación , Esteroides/química , Difracción de Rayos X
18.
Molecules ; 22(10)2017 Sep 30.
Artículo en Inglés | MEDLINE | ID: mdl-28973960

RESUMEN

Chagas disease is an endemic parasitic infection that occurs in 21 Latin American countries. New therapies for this disease are urgently needed, as the only two drugs available (nifurtimox and benznidazol) have high toxicity and variable efficacy in the disease's chronic phase. Recently, a new chemical entity (NCE) named Pyranaphthoquinone (IVS320) was synthesized from lawsone. We report herein, a detailed study of the physicochemical properties and in vitro trypanocidal activity of IVS320. A series of assays were performed for characterization, where thermal, diffractometric, and morphological analysis were performed. In addition, the solubility, permeability, and hygroscopicity of IVS320 were determined. The results show that its poor solubility and low permeability may be due to its high degree of crystallinity (99.19%), which might require the use of proper techniques to increase the IVS320's aqueous solubility and permeability. The trypanocidal activity study demonstrated that IVS320 is more potent than the reference drug benznidazole, with IC50/24 h of 1.49 ± 0.1 µM, which indicates that IVS320 has potential as a new drug candidate for the treatment of Chagas disease.


Asunto(s)
Enfermedad de Chagas/tratamiento farmacológico , Naftoquinonas/química , Tripanocidas/química , Trypanosoma/efectos de los fármacos , Sitios de Unión , Humanos , Modelos Moleculares , Estructura Molecular , Naftoquinonas/farmacología , Permeabilidad , Unión Proteica , Solubilidad , Tripanocidas/farmacología
19.
Molecules ; 22(9)2017 Sep 09.
Artículo en Inglés | MEDLINE | ID: mdl-28891943

RESUMEN

α,ß Amyrin (ABAM) is a natural mixture of pentacyclic triterpenes that has shown a variety of pharmacological properties, including anti-inflammatory effect. ABAM is isolated from Burseraceae oilresins, especially from the Protium species, which is commonly found in the Brazilian Amazon. This work aimed to develop solid dispersions (SD) of ABAM with the following hydrophilic polymers: polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG-6000) and hydroxypropylmethylcellulose (HPMC). The SDs were prepared by physical mixture (PM), kneading (KND) and rotary evaporation (RE) methods. In order to verify any interaction between ABAM and the hydrophilic polymers, physicochemical characterization was performed by Fourier transform infrared (FTIR), scanning electron microscopy (SEM), powder X-ray diffraction (XRD), thermogravimetry (TG) and differential scanning calorimetry (DSC) analysis. Furthermore, an in vitro anti-inflammatory assay was performed with ABAM alone and as SDs with the hydrophilic polymers. The results from the characterization analysis show that the SDs were able to induce changes in the physicochemical properties of ABAM, which suggests interaction with the polymer matrix. In vitro anti-inflammatory assay showed that the SDs improved the anti-inflammatory activity of ABAM and showed no cytotoxicity. In conclusion, this study showed the potential use of SDs as an efficient tool for improving the stability and anti-inflammatory activity of ABAM without cytotoxicity.


Asunto(s)
Antiinflamatorios no Esteroideos/química , Burseraceae/química , Lipopolisacáridos/antagonistas & inhibidores , Óxido Nítrico/antagonistas & inhibidores , Ácido Oleanólico/análogos & derivados , Antiinflamatorios no Esteroideos/aislamiento & purificación , Antiinflamatorios no Esteroideos/farmacología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Humanos , Derivados de la Hipromelosa/química , Inflamación , Lipopolisacáridos/farmacología , Macrófagos/citología , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Óxido Nítrico/biosíntesis , Ácido Oleanólico/química , Ácido Oleanólico/aislamiento & purificación , Ácido Oleanólico/farmacología , Aceites de Plantas/química , Polietilenglicoles/química , Povidona/química , Resinas de Plantas/química , Suspensiones
20.
Phytother Res ; 31(7): 959-970, 2017 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-28544038

RESUMEN

Parkinson's disease (PD) consists of a neurodegenerative pathology that has received a considerable amount of attention because of its clinical manifestations. The most common treatment consists of administering the drugs levodopa and biperiden, which reduce the effectiveness of the disease and the progress of its symptoms. However, phytotherapy treatment of PD has shown great potential in retarding the loss of dopaminergic neurons and minimizing the behavioral abnormalities. The aim of this study is to systematically review the use of supplemental herbal plants with cellular protective effect and behavioral activity in in vivo and in vitro experimental models. A total of 20 studies were summarized, where the effectiveness of herbal extracts and their isolated bioactive compounds was observed in animal models for PD. The main neurochemical mechanisms found in these studies are schematically represented. The herbal extracts and their biocompounds have antioxidant, anti-apoptotic, and antiinflammatory properties, which contribute to avoiding neuronal loss. Reports show that besides acting on the biosynthesis of dopamine and its metabolites, these compounds prevent D2 receptors' hypersensitivity. It is suggested that further studies need be conducted to better understand the mechanisms of action of the bioactive compounds distributed in these plants. Copyright © 2017 John Wiley & Sons, Ltd.


Asunto(s)
Fármacos Neuroprotectores/farmacología , Enfermedad de Parkinson/tratamiento farmacológico , Fitoterapia , Extractos Vegetales/farmacología , Animales , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Apoptosis/efectos de los fármacos , Modelos Animales de Enfermedad , Dopamina/biosíntesis , Antagonistas de los Receptores de Dopamina D2/farmacología , Neuronas Dopaminérgicas/efectos de los fármacos , Humanos
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