Nanoemulsão fotoprotetora e processo de produção de nanoemulsão fotoprotetora

DepositadaA invenção se refere a uma nanoemulsão óleo em água fotoprotetora e antioxidante que compreende entre 10 e 25% (m/m) de compostos fotoprotetores, ao menos um antioxidante, quitosana e tensoativos não-iônicos; e ainda a invenção trata do processo de produção destas nanoemulsões

Development and validation of an analytical method using High Performance Liquid Chromatography (HPLC) to determine ethyl butylacetylaminopropionate in topical repellent formulations

Diseases caused by insects are frequent in poor countries, leading to epidemic scenarios in urban areas; e.g., Dengue, Zika and Chikungunya. For this reason, the development of a safe and efficient topical formulation is essential. Ethyl butylacetylaminopropionate (EB) is a mosquito repellent developed by Merck, which is used in products for adults, children and especially babies, due to its low allergenic potential. The aim of this work was to validate an analytical methodology to quantify EB in a new poloxamer-based formulation by high-performance liquid chromatography (HPLC). The quantification methodology was performed at 40 ºC using a Kromasil reverse-phase column (C18), with the dimensions of 250 x 4.6 mm. The mobile phase was acetonitrile:water (1:1) at a 1.0 mL/min flow-rate. The detector wavelength was set at 218 nm to detect EB. The methodology was considered validated since the results indicated linearity (R2>;0.99), specificity, selectivity, precision and accuracy (active recovery between 98% and 102%). It also presented limits of detection and quantification of 0.255 µg/mL and 0.849 µg/mL, respectively. The present study demonstrated the EB vehiculated in poloxamer gel is promising as a new insect repellent formulation, since it could be quantified and quality control evaluated

Drug metabolism: Comparison of biodistribution profile of holmium in three different compositions in healthy Wistar rats

Radioisotope holmium is a candidate to be used in cancer treatment and diagnosis. There are different holmium salts and they present distinct solubility and consequently different biodistribution profiles. In this work, we aimed to evaluate the biodistribution profiles of two holmium salts (chloride and sulfate) and holmium nanoparticles (oxide) through an in vivo biodistribution assay using animal model. Samples were labeled with technetium-99m and administered in Wistar rats by retro-orbital route. Holmium chloride is highly soluble in water and it was quickly filtered by the kidneys while holmium sulfate that presents lower solubility in water was mainly found in the liver and the spleen. However, both the salts showed a similar biodistribution profile. On the other hand, holmium oxide showed a very different biodistribution profile since it seemed to interact with all organs. Due to its particle size range (approximately 100 nm) it was not intensively filtered by the kidneys being found in high quantities in many organs, for this reason its use as a nanoradiopharmaceutical could be promising in the oncology field. (C) 2016 Elsevier Ltd. All rights reserved.The authors would like to thank the National Scientific and Technological Research Council (CNPQ) (CNPq: 303594/2015-2) and the Rio de Janeiro State Research Foundation (FAPERJ) for funding.Cerqueira-Coutinho, C.; Pascual Vidal, L.; Pinto, SR.; Santos-Oliveira, R. (2016). Drug metabolism: Comparison of biodistribution profile of holmium in three different compositions in healthy Wistar rats. Applied Radiation and Isotopes. 112:27-30. https://doi.org/10.1016/j.apradiso.2016.02.015S273011

Development and validation of an analytical method using High Performance Liquid Chromatography (HPLC) to determine ethyl butylacetylaminopropionate in topical repellent formulations

ABSTRACT Diseases caused by insects are frequent in poor countries, leading to epidemic scenarios in urban areas; e.g., Dengue, Zika and Chikungunya. For this reason, the development of a safe and efficient topical formulation is essential. Ethyl butylacetylaminopropionate (EB) is a mosquito repellent developed by Merck, which is used in products for adults, children and especially babies, due to its low allergenic potential. The aim of this work was to validate an analytical methodology to quantify EB in a new poloxamer-based formulation by high-performance liquid chromatography (HPLC). The quantification methodology was performed at 40 ºC using a Kromasil reverse-phase column (C18), with the dimensions of 250 x 4.6 mm. The mobile phase was acetonitrile:water (1:1) at a 1.0 mL/min flow-rate. The detector wavelength was set at 218 nm to detect EB. The methodology was considered validated since the results indicated linearity (R2>0.99), specificity, selectivity, precision and accuracy (active recovery between 98% and 102%). It also presented limits of detection and quantification of 0.255 µg/mL and 0.849 µg/mL, respectively. The present study demonstrated the EB vehiculated in poloxamer gel is promising as a new insect repellent formulation, since it could be quantified and quality control evaluated

Anti-MUC1 nano-aptamers for triple-negative breast cancer imaging by single-photon emission computed tomography in inducted animals: initial considerations

Submitted by Repositório Arca ([email protected]) on 2019-03-07T16:42:10Z No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) F77-ijn-12-053.pdf: 831281 bytes, checksum: e97d0bdfba3436c85de8c7686687cef5 (MD5)Approved for entry into archive by monique santos ([email protected]) on 2019-03-07T17:34:03Z (GMT) No. of bitstreams: 2 F77-ijn-12-053.pdf: 831281 bytes, checksum: e97d0bdfba3436c85de8c7686687cef5 (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5)Made available in DSpace on 2019-03-07T17:34:03Z (GMT). No. of bitstreams: 2 F77-ijn-12-053.pdf: 831281 bytes, checksum: e97d0bdfba3436c85de8c7686687cef5 (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) Previous issue date: 2016Universidade do Estado do Rio de Janeiro. Instituto de Biologia Roberto Alcântara Gomes. Rio de Janeiro, RJ, Brasil / Instituto de Engenharia Nuclear. Comissão Nacional de Energia Nuclear. Rio de Janeiro, RJ, Brasil.Universidade Federal do Rio de Janeiro. Faculdade de Farmácia. Rio de Janeiro, RJ, Brasil.Universidade Federal do Rio de Janeiro. Instituto de Macromoléculas Eloísa Mano. Rio de Janeiro, RJ, Brasil.Universidade do Estado do Rio de Janeiro. Instituto de Biologia Roberto Alcântara Gomes. Rio de Janeiro, RJ, Brasil / Instituto de Pesquisas Energéticas e Nucleares. Centro de Radiofarmácia. São Paulo, SP, Brasil.Instituto de Pesquisas Energéticas e Nucleares. Centro de Radiofarmácia. São Paulo, SP, Brasil.Instituto de Pesquisas Energéticas e Nucleares. Centro de Radiofarmácia. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Imunobiológicos. Rio de Janeiro, RJ, Brasil.Instituto de Engenharia Nuclear. Comissão Nacional de Energia Nuclear. Rio de Janeiro, RJ, Brasil.A detecção precoce e específica de tumores continua sendo uma barreira na oncologia, especialmente em casos como o câncer de mama triplo negativo (TNBC). Para abordar essa lacuna, os aptâmeros encontraram uma importante aplicação no reconhecimento de biomarcadores tumorais, como a mucina 1 (MUC1). No entanto, ainda existem algumas dificuldades no uso do aptâmero, já que sua depuração biológica rápida torna seu uso limitado por drogas. Neste estudo, o aptâmero anti-MUC1 foi usado como um sistema de entrega de drogas (DDS) para uma nanopartícula polimérica radioativa (NP) na geração de imagens de TNBCs. Assim, NPs poli (ácido lático-co-glicólico) carregadas com o aptâmero anti-MUC1 e marcadas com tecnécio-99m foram usadas para um estudo de biodistribuição e geração de imagens de TNBC. Os resultados confirmaram que o NP foi obtido com sucesso, com tamanho médio de 262 nm, de acordo com os dados dinâmicos de espalhamento de luz. O ensaio de biodistribuição em modelos animais induzidos com TNBC mostrou que, embora houvesse uma alta captação pelo intestino (> 30%), o DDS desenvolvido teve uma alta captação tumoral (5%) e com ótimas propriedades de imagem in vivo, corroborando a possibilidade de uso deste DDS como um medicamento de imagem para TNBC.The early and specific detection of tumors remains a barrier in oncology, especially in cases such as the triple-negative breast cancer (TNBC). To address this gap, aptamers have found an important application in the recognition of tumor biomarkers such as mucin 1 (MUC1). However, there are still some difficulties in the use of aptamer, as their rapid biological clearance makes their use as drugs limited. In this study, the anti-MUC1 aptamer was used as a drug delivery system (DDS) for a radioactive polymeric nanoparticle (NP) in the imaging of TNBCs. Thus, poly(lactic-co-glycolic acid) NPs loaded with the anti-MUC1 aptamer and labeled with technetium-99m were used for a biodistribution study and imaging of TNBC. The results confirmed that the NP was successfully obtained, with a mean size of 262 nm, according to the dynamic light scattering data. The biodistribution assay in induced animal models with TNBC showed that although there was a high capture by intestine (>30%), the DDS developed had a high tumor uptake (5%) and with great in vivo imaging properties, corroborating the possibility of use of this DDS as an imaging drug for TNBC

Promotion of cutaneous penetration of nifedipine for nanoemulsion

ABSTRACT This article reports the development and characterization of a nanoemulsion (NE) able to improve the cutaneous penetration of nifedipine. NE with nifedipine was development and characterized, presenting droplet size of 20 nm with low polydispersity index (IP<0.1), spherical shape without aggregation, pH compatible with typical skin levels and stability evaluated by seven months. In the permeation studies, a classical formulation based in an oil/water cream containing nifedipine was used for comparison with NE. Nanoemulsion promoted and improved the retention of nifedipine in the epidermis and dermis in relation to classical formulation. This promoting effect is related to the nanometric size of the droplets of the NE (20 nm), which give him a large superficial area, favoring the contact of the nanocarrier with the skin surface. The NE was efficient in promoting accumulation of nifedipine in the dermis, which is the site of vasodilation action. NE was not irritating according to the primary dermal irritation tests. NE is a promising release system to promote cutaneous penetration of nifedipine and can be used in the future in clinical trials to promote healing of lesions caused by peripheral vascular diseases

Characterization and biodistribution of bevacizumab TPGS-based nanomicelles: Preliminary studies

Bevacizumab is an FDA approved monoclonal antibody (anti VEGF) indicated in many cancers, mostly metastatic ones. D-α-tocopheryl polyethylene glycol succinate (TPGS) is the water-soluble form of vitamin E which usually forms micelles. This work aims to report preliminary results of the biodistribution of a TPGS based nano-micelle delivery system for bevacizumab in a gastric cancer xenograft model. Evaluation of the biodistribution of micelles/bevacizumab-99mTc was performed in Balb/c nude mice carrying MKN45 cell line xenograft. The nano-radiopharmaceutical (3.7 MBq/0.2 mL) was administered intraocularly and biodistribution was assesed 1 h post administration. The activity in each organ and blood was determined by a gamma counter. Mean size was 10 ± 1 nm for pure TPGS and 11 ± 1 nm for bevacizumab-TPGS respectively. Biodistribution showed that the highest uptake was found in both lungs and liver. Kidneys had also an important uptake. The tumor accumulated moderate to low radiolabeled nanomicelles, nevertheless tumor/blood ratio was very high. These preliminary results may help as a start point to continue evaluating the potential of radiolabeled bevacizumab-TPGS based nanomicelles to be used as a theranostic agent.Fil: Tesan, Fiorella Carla. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; ArgentinaFil: Cerqueira Coutinho, Cristal. Universidade Federal do Rio de Janeiro; BrasilFil: Salgueiro, María Jimena. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; ArgentinaFil: Albernaz, Marta de Souza. Universidade Federal do Rio de Janeiro; BrasilFil: Pinto, Suyenne Rocha. Universidade Estadual da Zona Oeste; BrasilFil: Reis, Sara Rhaissa Rezende Dos. Universidade Estadual da Zona Oeste; BrasilFil: Bernardes, Emerson Soares. Instituto de Pesquisas Energéticas e Nucleares; BrasilFil: Chiapetta, Diego. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Zubillaga, Marcela Beatriz. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Santos Oliveira, Ralph. Universidade Estadual da Zona Oeste; Brasi

In vitro and in vivo evaluation of efficacy and safety of photoprotective formulations containing antioxidant extracts

ABSTRACT Chronic exposure to solar radiation could contribute to premature skin aging and skin cancer. Skin presents its own antioxidant defense, however when defenses are out of balance, reactive oxygen species could damage biological structures. In the present work, an oil-in-water photoprotective emulsion was developed and Bauhinia microstachya var. massambabensis Vaz, Fabaceae, extracts at 1% (obtained by extraction with different solvents) were added to this emulsion. In vitro and in vivo efficacy and safety of the formulations were evaluated. Spectrophotometric methods and in vivo Colipa test were performed to evaluated efficacy of the formulations, through sun protection factor (SPF) determination and UVA protection factor assessment. To the in vitro safety assessment HET-CAM, CAM-TBS and Red Blood Cell tests were performed. Results showed that both extracts contributed to a higher in vivo photoprotection (SPF 18) when compared to the formulation without extract (SPF 13), this result could be attributed to the antioxidant activity of the plant extracts that act by capturing reactive oxygen species. Concerning safety, all formulations were considered non-irritant according to in vitro tests. Formulations containing extracts could be considered efficient and safe for cosmetic use since they presented higher sun protection factor and passed the toxicity tests