Assessment of solubility and intestinal absorption in vitro of praziquantel in solid dispersions of polyethylene glycol 6000

The aim of this study was to investigate the impact of solid dispersions of polyethylene glycol 6000 (PEG 6000), using the co-precipitation method, on the in vitro solubility and intestinal absorption of praziquantel (PZQ). The solubility of PZQ in solid dispersions and physical mixtures was assessed in purified water and TC-199 buffer. The everted intestinal sac model was employed to assess, in vitro, intestinal absorption of PZQ. A significant enhancement in both in vitro solubility and intestinal absorption of PZQ was found in solid dispersions compared to pure PZQ and physical mixtures. This positive series of preliminary results showed that solid dispersion of PEG 6000 is a valuable strategy for increasing bioavailability of PZQ and could also prove useful for other poorly water-soluble drugs.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Anti-inflammatory choline based ionic liquids: Insights into their lipophilicity, solubility and toxicity parametrites

The impact on in vivo efficacy and safety of two novel ionic liquids based on the association of choline with nonsteroidal anti-inflammatory drugs, ketoprofen and naproxen forming IL-APIs, was evaluated. Their lipophilicity, solubility and toxicity were assessed aiming the illustration of the pharmaceutical profile and potential toxic impact. Partition coefficientwas determined usingmicelles of hexadecylphosphocholine and UV–Vis derivative spectroscopy. Additionally, solubility in phosphate buffer pH 7.4 wasmeasured using amodified shake flaskmethod and UV–Vis spectroscopy as detection technique. Ultimately, toxicity was considered resorting to a fully automated cytochrome c oxidase assay based onmicrofluidics. The obtained results demonstrated that the IL-APIs' drug format has the ability to interact with biological membranes and also improves solubility up to 58 times. Moreover, it was evidenced that, although being a nutrient, choline influences the IL-APIs' toxicity. The studied anti-inflammatory IL-APIs exhibited promising properties regarding their incorporation in pharmaceutical formulations

Conservation units in the core area of the Cerrado domain: an overview on the small nonvolant mammals (Rodentia and Didelphimorphia)

A review of small non-volant mammal species of the APA Gama e Cabeça de Veado was carried out, including new surveys in the "Estação Ecológica do Jardim Botânico" (EEJBB) and "Reserva Ecológica do Instituto Brasileiro de Geografia e Estatí­stica" (REIBGE). Thirty-one small mammal's species are registered for the APA Gama and Cabeça de Veado, including one exotic species. Didelphis albiventris, Hylaeamys megacephalus, and Oxymycterus delator were collected for the first time in EEJBB. The APA Gama-Cabeça de Veado has a central position in the Cerrado domain sharing six species with the Amazon domain, five with Atlantic Forest, and 13 with Caatinga. The APA Gama-Cabeça de Veado encompasses the home range of at least six non-volant small mammal species endemic of Cerrado domain, and it has an important role in the protection of these endemic species and species that occurs in those four South America morphoclimatic domains

Histological and ultrastructural feature and nitrite production of caprine preantral follicles in vitro cultured in the presence or absence of serum

Avaliou-se o efeito da adição de diferentes tipos e concentrações de soro sobre o desenvolvimento e a sobrevivência de folículos ovarianos pré-antrais (FOPA) caprinos in vitro. Além disso, verificou-se a relação entre as concentrações de nitrito presentes no meio de cultivo e a viabilidade folicular. Cada par ovariano foi dividido em 29 fragmentos, sendo um destinado ao controle. Os fragmentos foram cultivados por um ou sete dias em meio essencial mínimo suplementado (MEM+) ou MEM+ com diferentes concentrações (10 ou 20%) de soro fetal bovino (SFB), soro de cabra em estro (SCE) ou soro de cabra em diestro (SCD). Na análise morfológica após sete dias, apenas o tratamento com 10% de SFB apresentou percentual de FOPA normais similar ao MEM+ (P>0,05). A análise ultra-estrutural dos folículos cultivados por sete dias com MEM+ ou MEM+ com 10% de SFB mostrou danos oocitários, porém células da granulosa normais. A análise do meio de cultivo revelou correlação positiva entre a viabilidade folicular e a produção de nitrito. A suplementação com soro não melhorou a viabilidade de FOPA e a concentração de nitrito no meio de cultivo funcionou como um indicador da viabilidade das células da granulosa de FOPA caprinos cultivados in vitro. ______________________________________________________________________________________________________________ ABSTRACTThe effect of the addition of different types and concentrations of sera on the viability and development of caprine preantal follicles (PAF) in vitro cultured was analyzed. In addition, it was evaluated the correlation between nitrite concentrations in culture medium and folicular viability. Each ovarian pair was divided in 29 fragments and one was used as control. The fragments were cultured for one or seven days in minimal essential medium (MEM+) or MEM+ with different concentrations of (10 or 20%) bovine fetal serum (BFS), estrous goat serum (EGS), or diestrous goat serum (DGS). After seven days, the morphological analysis showed that only the treatment with 10% BFS maintained the percentage of normal PAF similar to MEM+ (P>0.05). The ultrastructural analysis of follicles cultured for seven days in MEM+ or MEM+ with 10% BFS showed some oocyte damage, although the granulosa cells were normal. Analysis of culture medium revealed a positive correlation between follicular viability and nitrite production. Supplementation with serum did not improve the viability of PAF and nitrite levels in culture medium served as an indicator of viability of granulose cells from caprine PAF in vitro cultured

APOIO À DECISÃO PARA A PROTEÇÃO INTEGRADA NO COMBATE A Tuta absoluta EM TOMATE HORTOINDUSTRIAL

A traça-do-tomateiro é atualmente uma praga-chave do tomate para indústria, na região do Ribatejo. A sua presença foi detectada em 2010, tendo causado prejuízos significativos na campanha de 2011. O objetivo deste projeto é criar ferramentas para a tomada de decisão no âmbito da proteção desta cultura contra esta praga. Durante o ano de 2013, procedeu-se à monitorização semanal de adultos de T. absoluta com recurso a armadilhas com feromona sexual, e à observação visual em 25 a 50 plantas, de acordo com o estado fenológico da cultura. O material entomológico foram analisadas, posteriormente, em laboratório para deteção de parasitismo. Além de avaliar a intensidade de ataque, identificaram-se fatores de risco prévio, para construção de mapas de risco de apoio à tomada de decisão para a limitação da praga como culturas vizinhas e respetivas datas de colheita. Os dados preliminares não apresentaram uma correlação entre o número de machos adultos capturados e o número de larvas presentes na cultura, pelo que a estimativa de risco baseada apenas na contagem de machos adultos não parece ser suficiente para a tomada de decisão. Verificaram-se dificuldades no combate à praga devido a razões de ordem estrutural (e.g. posse da terra, hospedeiros alternativos na vizinhança) e a lacunas no conhecimento da sua bioecologia

role of female sex hormone receptors

Funding Information: Funding: This study was supported by grant IECT-FAPEMA-05796/18 and FAPEMA IECT 30/2018-IECT Saúde, by the Research Center of the Portuguese Oncology Institute of Porto (project no. PI86-CI-IPOP-66-2017); by European Investment Funds by FEDER/COMPETE/POCI—Operational Competitiveness and Internationalization Program, and national funds by FCT—Portuguese Foundation for Science and Technology under projects UID/AGR/04033/2020, UIDB/CVT/00772/2020 and by Base Funding-UIDB/00511/2020 of the Laboratory for Process Engineering, Environment, Biotechnology, and Energy—LEPABE—funded by national funds through the FCT/MCTES (PID-DAC); Project 2SMART-engineered Smart materials for Smart citizens, with reference NORTE-01-0145-FEDER-000054, supported by Norte Portugal Regional Operational Programme (NORTE 2020), under the PORTUGAL 2020 Partnership Agreement, through the European Regional Development Fund (ERDF). Publisher Copyright: © 2021 by the authors. Licensee MDPI, Basel, Switzerland.A growing proportion of oropharyngeal squamous cell carcinomas (OPSCC) are associated with infection by high-risk human papillomavirus (HPV). For reasons that remain largely unknown, HPV+OPSCC is significantly more common in men than in women. This study aims to determine the incidence of OPSCC in male and female HPV16-transgenic mice and to explore the role of female sex hormone receptors in the sexual predisposition for HPV+ OPSCC. The tongues of 30-weeks-old HPV16-transgenic male (n = 80) and female (n = 90) and matched wild-type male (n = 10) and female (n = 10) FVB/n mice were screened histologically for intraepithelial and invasive lesions in 2017 at the Centre for the Research and Technology of Agro-Environmental and Biological Sciences (CITAB), Por-tugal. Expression of estrogen receptors alpha (ERα) and beta (ERβ), progesterone receptors (PR) and matrix metalloproteinase 2 (MMP2) was studied immunohistochemically. Collagen remodeling was studied using picrosirius red. Female mice showed robust ERα and ERβ expression in intraepithelial and invasive lesions, which was accompanied by strong MMP2 expression and marked collagen remodeling. Male mice showed minimal ERα, ERβ and MMP2 expression and unaltered collagen patterns. These results confirm the association of HPV16 with tongue base cancer in both sexes. The higher cancer incidence in female versus male mice contrasts with data from OPSCC patients and is associated with enhanced ER expression via MMP2 upregulation.publishersversionpublishe

Assessment of solubility and intestinal absorption in vitro of praziquantel in solid dispersions of polyethylene glycol 6000

The aim of this study was to investigate the impact of solid dispersions of polyethylene glycol 6000 (PEG 6000), using the co-precipitation method, on the in vitro solubility and intestinal absorption of praziquantel (PZQ). The solubility of PZQ in solid dispersions and physical mixtures was assessed in purified water and TC-199 buffer. The everted intestinal sac model was employed to assess, in vitro, intestinal absorption of PZQ. A significant enhancement in both in vitro solubility and intestinal absorption of PZQ was found in solid dispersions compared to pure PZQ and physical mixtures. This positive series of preliminary results showed that solid dispersion of PEG 6000 is a valuable strategy for increasing bioavailability of PZQ and could also prove useful for other poorly water-soluble drugs.Colegio de Farmacéuticos de la Provincia de Buenos Aire