Formulações micelares proteicas e respectivo método de produção

The present invention describes micellar protein formulations for the controlled release of active ingredients, and method for preparing the same. The invention describes a new micelle composition for use in pharmaceuticals, cosmetics and detergents. In particular, it describes micelle formation formulations that comprise: an aqueous phase containing a protein or a natural or synthetic peptide; a lipophilic phase containing a hydrophobic compound; an adjuvant dissolved in the aqueous phase to regulate the size and stability of the micelles; the size of the micelles varying from 30 to 5000 nm, preferably from 30 to 100 nm, wherein the micelles can be obtained by two different methods, namely using ultrasound or a high-pressure homogeniser. The preparation method involves two distinct phases: an aqueous phase and a lipophilic phase. The aqueous phase can be water or any buffer that is best suitable for a given use, such as an aqueous solution of bovine serum albumen (BSA); human serum albumen (HSA); silk fibroin or a polypeptide fibroin.A presente invenção descreve em formulações micelares proteicas para libertação controlada de agentes e respetivo método de produção. A invenção descreve numa nova composição de micelas para aplicações farmacêuticas, cosméticas e 0 o0 detergência. Nomeadamente, formulações para a formação de micelas que compreendem: · uma fase aquosa contendo uma proteína ou um péptido natural ou sintético; · uma fase lipofílica que compreende um composto hidrofóbico; · um agente adjuvante dissolvido na fase aquosa que regula o tamanho e estabilidade das micelas; em que os tamanhos das referidas micelas varia entre 30 a 5000 nm, de preferência de 30-100 nm, as referidas micelas podem ser obtidas a partir de duas metodologias diferentes, nomeadamente ultra-sons ou homogeneizador de alta pressão. O método de preparação envolve duas fases distintas: fase aquosa e fase lipofílica. A fase aquosa pode ser água ou qualquer tampão que mais se adeque para uma determinada aplicação, como por exemplo uma solução aquosa de albumina sérica bovina (BSA); albumina sérica humana (HSA); fibroína da seda ou de um polipéptido.Universidade do Minh

Assessment of a Formulation Containing a Castanea sativa Shells Extract on Skin Face Parameters: In Vivo Evaluation

In the last years, the demand for new eco-friendly ingredients has increased on the cosmetic market. Consumers are more aware of sustainable principles and, simultaneously, more conscious regarding the skin aging process. Chestnut (Castanea sativa) shells are a food by-product produced in high quantities in Europe. This waste has been described as a rich source of phenolic compounds with skin biological effects, such as antioxidant, antiradical, and anti-inflammatory activities. Despite the huge number of assays reporting the richness of chestnut shell extracts in bioactive compounds as well as the development of cosmetic formulations containing these extracts, no in vivo assays have assessed their clinical efficacy in human volunteers. The aim of this study was to evaluate the effect on skin face parameters of a formulation containing a chestnut shell extract in human volunteers (n = 22) who applied the product twice per day, for 56 days. For that, biophysical techniques, including Corneometer®, Cutometer®, and PrimosPremium, were employed, allowing the quantification of skin hydration and firmness, as well as of wrinkles’ depth and volume and wrinkles’ skin roughness. The results demonstrated that the formulation led to a slight decrease in roughness and wrinkles’ depth, although no significant differences with respect to a placebo were observed. In addition, a clear improvement of skin hydration was achieved (t0 = 54.00 Arbitrary Units (A.U.) and t56 = 58.62 A.U.). In contrast to the placebo, the active formulation increased skin firmness up to 31.76% in 50.00% of the volunteers, but without significant differences with respect to the placebo, probably due to the short period of treatment. A long-term use of the product is recommended to possibly observe significant differences in all parameters.This research was funded by the project PTDC/ASP-AGR/29277/2017—Castanea sativa shells as a new source of active ingredients for Functional Food and Cosmetic applications: a sustainable approach, supported by national funds by FCT/MCTES and co-supported by the Fundo Europeu de Desenvolvimento Regional (FEDER) throughout COMPETE 2020—Programa Operacional Competitividade e Internacionalização (POCI-01-0145-FEDER-029277). It was also funded by the projects UIDB/50006/2020 and UIDP/50006/2020 through national funds. This work was also financed by national funds from FCT—Fundação para a Ciência e a Tecnologia, I.P., in the scope of the project UIDP/04378/2020 and UIDB/04378/2020 of the Research Unit on Applied Molecular Biosciences—UCIBIO and the project LA/P/0140/2020 of the Associate Laboratory Institute for Health and Bioeconomy—i4HB. The authors are thankful to Sortegel for the chestnut samples and their availability during this work. The authors are thankful to Evonik for the samples. Ana Margarida Silva is thankful for the Ph.D. grant (SFRH/BD/144994/2019) financed by POPH-QREN and subsidized by the European Science Foundation and Ministério da Ciência, Tecnologia e Ensino Superior. Francisca Rodrigues (CEECIND/01886/2020) is thankful for her contract financed by FCT/MCTES—CEEC Individual Program Contractinfo:eu-repo/semantics/publishedVersio

Protein microspheres as suitable devices for piroxicam release

Bovine serum albumin-piroxicam (BSA-piroxicam) and human serum albumin-piroxicam (HSA-piroxicam) microspheres were sonochemically prepared and characterized. The use of polyvinyl alcohol (PVA) lead to an improvement of formulation characteristics, including smaller size, lower polydispersity index (PDl), higher entrapment efficiency and higher stability. The release kinetics of these proteinaceous microspheres was determined in presence of protease, indicating an anomalous drug transport mechanism (diffusion and polymer degradation). In presence of higher protease concentration, BSA microspheres exhibit Case II transport, leading to zero order release (protein degradation). These proteinaceous devices did not show cytotoxicity against human skin fibroblasts in vitro, for range concentrations below to 300 mg L−1, greatly supporting their potential application in the treatment of inflammatory diseases.We would like to acknowledge the financial support of European project Lidwine (contract no. NMP2-CT-2006-026741), and to POPH/FSE for co-financing and FCT for fellowship SFRH/BPD/38939/2007

Development of clozapine tablets by direct compression - analysis of pharmaceutical equivalence by dissolution profiles

The aim of this work was to develop clozapine tablets that can be classified as a pharmaceutical equivalent to a reference brand product. Tablets were produced by direct compression and dissolution tests were realized in order to evaluate the dissolution profiles. The results show that the tablets can be classified as immediate release dosage forms due to clozapine fast release, and such release was dependent on the amount of sodium croscarmelose in the formulation. Analysis of f1 and f2 factors was frustrated due to the fast drug release; the tablets were analyzed by the dissolution efficiency and the dissolution curve shape. The dissolution efficiency was higher than 98 % and the analysis of the dissolution shape curve showed that the tablets from one batch of the developed formulations were similar to the reference brand product. The clozapine tablets obtained in this study can be considered as pharmaceutically equivalent to the reference brand product.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Development of clozapine tablets by direct compression - analysis of pharmaceutical equivalence by dissolution profiles

The aim of this work was to develop clozapine tablets that can be classified as a pharmaceutical equivalent to a reference brand product. Tablets were produced by direct compression and dissolution tests were realized in order to evaluate the dissolution profiles. The results show that the tablets can be classified as immediate release dosage forms due to clozapine fast release, and such release was dependent on the amount of sodium croscarmelose in the formulation. Analysis of f1 and f2 factors was frustrated due to the fast drug release; the tablets were analyzed by the dissolution efficiency and the dissolution curve shape. The dissolution efficiency was higher than 98 % and the analysis of the dissolution shape curve showed that the tablets from one batch of the developed formulations were similar to the reference brand product. The clozapine tablets obtained in this study can be considered as pharmaceutically equivalent to the reference brand product.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Assessment of a protease inhibitor peptide for anti-ageing

Ageing and skin exposure to UV radiation induces production and activation of matrix metalloproteinases (MMPs) and human neutrophil elastase (HNE). These enzymes are known to break down the extracellular matrix (ECM) which leads to wrinkle formation. Here, we demonstrated the potential of a solid-in-oil nanodispersion containing a competitive inhibitor peptide of HNE mixed with hyaluronic acid (HA), displaying 158 nm of mean diameter, to protect the skin against the ageing effects. Western blot analysis demonstrated that activation of MMP-1 in fibroblasts by HNE treatment is inhibited by the solid-in-oil nanodispersion containing the peptide and HA. The results clearly demonstrate that solid-in-oil nanodispersion containing the HNE inhibitor peptide is a promising strategy for anti-ageing effects. This effect can be seen particularly by ECM regulation by affecting fibroblasts. The formulation also enhances the formation of thicker bundles of actin filaments.We thank Matadouro - Central Carnes de Entre Douro e Minho, Lda for their support on pig samples. The histological studies were supported by the Department of Histology from Life and Health Sciences Research Institute (ICVS), University of Minho. The authors thank the Fundação para a Ciência e Tecnologia the strategic funding of ID/BIO/04469/ 2013 unit

Valorization of Kiwiberry Leaves Recovered by Ultrasound-Assisted Extraction for Skin Application: A Response Surface Methodology Approach

This study aims to evaluate the optimal ultrasound-assisted extraction (UAE) conditions of antioxidants polyphenols from Actinidia arguta (Siebold & Zucc.) Planch. Ex Miq. (kiwiberry) leaves using a response surface methodology (RSM). The effects of solid:liquid ratio (2.5–10.0% w/v), time (20–60 min), and intensity (30–70 W/m2) on the total phenolic content (TPC) and antioxidant/antiradical activities were investigated. The optimal UAE conditions were achieved using a solid:liquid ratio of 10% (w/v) and an ultrasonic intensity of 30 W/m2 for 31.11 min. The results demonstrated that the optimal extract showed a high TPC (97.50 mg of gallic acid equivalents (GAE)/g dw) and antioxidant/antiradical activity (IC50 = 249.46 µg/mL for ABTS assay; IC50 = 547.34 µg/mL for DPPH assay; 1440.13 µmol of ferrous sulfate equivalents (FSE)/g dw for ferric reducing antioxidant power (FRAP)) as well as a good capacity to scavenge superoxide and hypochlorous acid (respectively, IC50 = 220.13 μg/mL and IC50 =10.26 μg/mL), which may be related with the 28 phenolic compounds quantified. The in vitro cell assay demonstrated that the optimal extract did not decrease the keratinocytes’ (HaCaT) viability, while the fibroblasts’ (HFF-1) viability was greater than 70.63% (1000 µg/mL). This study emphasizes the great potential of kiwiberry leaves extracted by UAE for skin application.Ana Margarida Silva (SFRH/BD/144994/2019) and Diana Pinto (SFRH/BD/144534 /2019) are thankful for their Ph.D. grants financed by POPH-QREN and subsidized by the European Science Foundation and Ministério da Ciência, Tecnologia e Ensino Superior. Manuela M. Moreira (CEECIND/02702/2017) and Francisca Rodrigues (CEECIND/01886/2020) are thankful for their contracts financed by FCT/MCTES—CEEC Individual Program Contract. The authors also thank the project SYSTEMIC “An integrated approach to the challenge of sustainable food systems: adaptive and mitigatory strategies to address climate change and malnutrition”. The Knowledge hub on Nutrition and Food Security has received funding from national research funding parties in Belgium(FWO), France (INRA), Germany (BLE), Italy (MIPAAF), Latvia (IZM), Norway (RCN), Portugal (FCT) and Spain (AEI) in a joint action of JPI HDHL, JPI-OCEANS and FACCE-JPI launched in 2019 under the ERA-NET ERA-HDHL (no. 696295).info:eu-repo/semantics/publishedVersio

Poloxamer 407 based-nanoparticles for controlled release of methotrexate

Poloxamer 407 (P407)-based nanoparticles were produced by the high pressure homogenization method for the encapsulation and delivery of methotrexate (MTX), aiming intravenous therapeutic applications. The surface of these nanoparticles was functionalized by conjugation of P407 with folic acid (FA) or with MTX, which served as targeting ligand agents. MTX-P407 conjugate was also developed to increase the final drug cargo. Two hydrophobic derivatives of MTX, MTX di-ethylated ester (MTX-OEt) and the ionic complex MTX-dimethyldioctadecylammonium bromide (MTX-DODAB) were produced and entrapped onto P407-based nanoparticles. All formulations developed revealed a monodisperse character comprising small and narrow nanoparticles (<100 nm). P407 nanoparticles (functionalized with FA) and MTX-P407 nanoparticles, both loaded with MTX-OEt, demonstrated a slow drug release profile. The effect of lipase from Aspergillus oryzae on the hydrolysis of the linkage between the P407 and MTX, and consequent MTX release profile, was also evaluated. We observed a controlled and slow release of MTX (<50% of release after 11 days) in the presence of enzyme. These MTX-P407 nanoparticles loaded with MTX-OEt induced a great effect against Caco-2 cancer cells (40% of cell death after 72 h of incubation), demonstrating higher efficiency than the free MTX at the same concentration.This study was supported by the Portuguese Foundation for Science and Technology (FCT) under the scope of the strategic funding of UID/BIO/04469/2019 unit and BioTecNorte operation (NORTE-01-0145-FEDER-000004) funded by the European Regional Development Fund under the scope of Norte2020 - Programa Operacional Regional do Norte. The authors also thanks to FCT for funding their scholarship: Jennifer Noro (SFRH/BD/121673/2016) and Carla Silva (SFRH/IF/00186/2015). This work has also received funding from the European Union Horizon 2020 research and innovation program under grant agreement NMP-06-2015-683356 FOLSMART.info:eu-repo/semantics/publishedVersio

New recycling approaches for thermoset polymeric composite wastes – an experimental study on polyester based concrete materials filled with fibre reinforced plastic recyclates

In this study, a new waste management solution for thermoset glass fibre reinforced polymer (GFRP) based products was assessed. Mechanical recycling approach, with reduction of GFRP waste to powdered and fibrous materials was applied, and the prospective added-value of obtained recyclates was experimentally investigated as raw material for polyester based mortars. Different GFRP waste admixed mortar formulations were analyzed varying the content, between 4% up to 12% in weight, of GFRP powder and fibre mix waste. The effect of incorporation of a silane coupling agent was also assessed. Design of experiments and data treatment was accomplished through implementation of full factorial design and analysis of variance ANOVA. Added value of potential recycling solution was assessed by means of flexural and compressive loading capacity of GFRP waste admixed mortars with regard to unmodified polymer mortars. The key findings of this study showed a viable technological option for improving the quality of polyester based mortars and highlight a potential cost-effective waste management solution for thermoset composite materials in the production of sustainable concrete-polymer based products

The MOVE.TE Falls Prevention and Management Program: lessons learnt in the Portuguese context

MOVE.TE is a non-profit participatory physiotherapy platform that aims at translating knowledge in the field of physiotherapy and developing freely available evidence-based physiotherapy programmes targeting the primary care services of the Portuguese National Health service. A group of volunteer academics and clinicians collaborated at different stages and time points to create the first ever falls prevention and management programme and guidance for Physiotherapy in primary care, in Portugal. This report describes this seven-step process. In spite of many challenges, this project constitutes an example of advocacy in physiotherapy for the promotion of better healthcare for older adults.info:eu-repo/semantics/publishedVersio