Currently, there is an increasing interest on the development of topical formulations containing rosmarinic acid (RA) due to its well-documented antioxidant activity. This study aimed to develop and ...validate a stability-indicating ultra-fast liquid chromatography (UFLC) method for the determination of RA in nanoemulsions, porcine skin and nasal mucosa intended to be applied in permeation/retention studies and for development of topical nanoemulsions. Chromatographic separation was carried out using a C18 column packed with 2.6 μm particle size in isocratic conditions using as mobile phase water:acetonitrile (83:17, v/v), acidified with 0.1% trifluoracetic acid (v/v), with a total time of analysis of 3.5 min and detection at 330 nm. RA analysis was specific in the presence of both non-biological (blank nanoemulsion and receptor fluid) and biological matrices (porcine ear skin and porcine nasal mucosa). No interference of degradation products of RA was verified after different stress conditions such as acidic, alkaline, oxidative, light exposure (UV-A and UV-C) and thermal demonstrating the method stability-indicating property. The analytical (0.1–10.0 μg·mL−1) and bioanalytical (0.5–10.0 μg·mL−1) linearity was proved by analysis of the calibration curves of RA and no matrix effect was observed. The method was sensitive, precise and accurate, and showed recovery higher than 85%. The method was considered robust as evaluated by a Plackett-Burman experimental design. In the validated conditions, the RA was determined in the nanoemulsions obtained by spontaneous emulsification procedure (1.007 ± 0.040 mg·mL−1), porcine ear skin (1.13 ± 0.19 μg·cm−2) and nasal mucosa (22.46 ± 3.99 μg·cm−2) after retention/permeation studies. Thus, a highly sensitive, simple, fast and stability-indicating method was developed for RA analysis during the development of topical nanoemulsions and bioanalytical assays in complex matrices.
•A simple and fast analytical and bioanalytical UFLC method for RA was validated.•The method proved to be stability-indicating using different stress conditions.•The method was selective, linear, precise, accurate and robust with low matrix effect.•The method was able to estimate RA incorporated in pharmaceutical nanoemulsions.•The method was applied to assay RA in skin and nasal mucosa samples.
There is a growing interest in the pharmaceutical field concerning isoflavones topical delivery systems, especially with regard to their skin care properties and antiherpetic activity. In this ...context, the present work describes an ultra-fast liquid chromatography method (UFLC) for determining daidzein, glycitein, and genistein in different matrices during the development of topical systems containing isoflavone aglycones (IA) obtained from soybeans. The method showed to be specific, precise, accurate, and linear (0.1 to 5µgmL−1) for IA determination in soybean acid extract, IA-rich fraction obtained after the purification process, IA loaded-nanoemulsions, and topical hydrogel, as well as for permeation/retention assays in porcine skin and porcine esophageal mucosa. The matrix effect was determined for all complex matrices, demonstrating low effect during the analysis. The stability indicating UFLC method was verified by submitting IA to acidic, alkaline, oxidative, and thermal stress conditions, and no interference of degradation products was detected during analysis. Mass spectrometry was performed to show the main compounds produced after acid hydrolysis of soybeans, as well as suggest the main degradation products formed after stress conditions. Besides the IA, hydroxymethylfurfural and ethoxymethylfurfural were produced and identified after acid hydrolysis of the soybean extract and well separated by the UFLC method. The method’s robustness was confirmed using the Plackett-Burman experimental design. Therefore, the new method affords fast IA analysis during routine processes, extract purification, products development, and bioanalytical assays.
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•An analytical and bioanalytical UFLC method for isoflavone aglycones was validated.•Acid hydrolysis of soybeans was performed to obtain the isoflavone aglycones.•Extract impurities as hydroxymethylfurfural and ethoxymethylfurfural were detected.•A pure rich-fraction was produced and incorporated in nanoemulsions and hydrogels.•Permeation assays in porcine skin or porcine esophageal mucosa were performed.
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•Acid hydrolyzed soybean extracts (AHSE) are isoflavone-rich products.•Acid hydrolysis of soybeans produced furanic compounds (HMF and EMF) as impurities.•The amount of HMF and EMF ...was determined by a validated chromatography method.•The mutagenic effect of EMF was evaluated by the Salmonella/microssome assay.•The genotoxic effect of EMF was evaluated by the comet assay with HepG2 cells.
Soybean acid hydrolyzed extracts are raw-materials widely used for manufacturing of pharmaceuticals and cosmetics products due to their high content of isoflavone aglycones. In the present study, the main sugar degradation products 5-hydroxymethyl-2-furfural (HMF) and 5-ethoxymethyl-2-furfural (EMF) were quantitatively determined after acid hydrolysis of extracts from different soybean cultivars by a validated liquid chromatography method. The furanic compounds determined in samples cover the range of 0.16–0.21mg/mL and 0.22–0.33mg/mL for HMF and EMF, respectively. Complementarily, due to the scarce literature regarding the EMF toxicology, this study also assessed the EMF mutagenicity by the Salmonella/microsome test and genotoxicity by the comet assay. The results revealed that EMF did not show mutagenicity at the range of 50–5000μg/plate in S. typhimurium strains TA98, TA97a, TA100, TA102 and TA1535, but induced DNA damage in HepG2 cells at non-cytotoxic doses of 0.1–1.3mg/mL, mainly by oxidative stress mechanisms. Based on literature of HMF genotoxicity, and considering the EMF genotoxicity results herein shown, purification procedures to remove these impurities from extracts are recommended during healthcare products development to ensure the security of the products.
Nanotechnology-based delivery systems have been considered a promising approach for topical application, considering their characteristics of penetration into/across the skin. The present review ...aimed to evaluate the recent international scenario of patents concerning the use of nanotechnology- based delivery systems as skin penetration enhancers. A survey of recent patent documents was conducted by using the Espacenet patent database including the terms "skin" in the title and "promot* or enhanc* and penetrat* or absorp* or permeat*" and "nano*" with the truncation symbol (*) in the abstract of documents. A total of 110 patents were published from 2008 to 2018, with 94 technologies being considered. The results demonstrated an increase in innovations concerning nanotechnologybased delivery systems as skin penetration enhancers in recent years. Most patent applicants are from China (60.6%) and Korea (21.3%), and companies (68%) were the most prominent owners. The majority of patent applications (76%) were intended for cosmetic purposes; the types of products and nanostructures were also investigated. Overall results demonstrated the increased interest around the world in patenting products involving skin permeation promotion and nanotechnology for pharmaceutical and, mainly, for cosmetics purposes.
Os acidentes com animais peçonhentos têm importância na saúde pública, sendo fundamental ações educativas para prevenção, diagnóstico e tratamentos. No Brasil, os soros hiperimunes são preconizados ...para o tratamento dos acidentados. Esses produtos são produzidos por laboratórios oficiais seguindo requisitos das Boas Práticas de Fabricação (BPF) e distribuídos gratuitamente pelo Sistema Único de Saúde. Buscando atender uma demanda da sociedade, o projeto de extensão “Kaizen: Formação de recursos humanos e o aperfeiçoamento contínuo profissional, institucional e social sobre animais peçonhentos e a produção de soros na saúde pública” estabeleceu uma parceria entre o Instituto Vital Brazil (IVB) e o Curso de Farmácia da Universidade Federal do Rio de Janeiro (UFRJ-Macaé) para o desenvolvimento de ciclos de ações educativas para diferentes públicos. O primeiro ciclo foi realizado pela universidade e direcionado aos colaboradores do IVB envolvendo conteúdos das BPF. O segundo ciclo foi realizado pelo IVB para o público de Macaé e municípios limítrofes com a participação de estudantes de ensino fundamental, médio e superior, além de agentes de combate de endemias, exército brasileiro, defesa civil, centro de zoonoses e guarda ambiental. Após a realização das ações, formulários de avaliação foram fornecidos aos participantes, observando-se alto grau de satisfação. Dessa forma, as ações contribuíram para o aprimoramento do conhecimento das BPF, além de ampliar os espaços de construção do conhecimento e aprendizagem para evitar os acidentes com animais peçonhentos, assim como nos tratamentos e produção dos soros hiperimunes e distribuição na saúde pública.
Os medicamentos podem constituir risco à saúde pública e ao meio ambiente se descartados incorretamente. Neste cenário vem sendo desenvolvido o projeto “Descarte de medicamentos: diagnóstico, ...educação e gerenciamento em domicílios e estabelecimentos farmacêuticos do município de Macaé-RJ” cujo objetivo envolve a realização de ações educativas e o estabelecimento de procedimentos para o correto manejo desses resíduos em conformidade com as Boas Práticas de Gerenciamento dos Resíduos de Serviços de Saúde (RSS). Um sistema de logística reversa foi desenvolvido através da disponibilização de um dispositivo contentor com espaços destinados à segregação de formas farmacêuticas sólidas, semissólidas e líquidas na cidade Universitária de Macaé-RJ. Em dias pré-determinados realizou-se o recebimento dos resíduos de medicamentos, seguidos da identificação, análise e armazenamento temporário. A coleta, transporte externo, tratamento e destinação ambientalmente adequada do resíduo foi conduzida pela empresa Transforma Gerenciamento de Resíduos, parceira do projeto e licenciada para a atividade. A caracterização dos materiais foi realizada com formulário validado observando-se 21,2 kg de resíduos durante o ano de 2019. Durante este mesmo ano a ação educativa “Posso jogar remédio no lixo?” foi realizada para diferentes públicos escolares do ensino médio de Macaé e região, sendo observado ótimos indicadores de satisfação junto ao público participante. Assim, além do diálogo e troca de saberes envolvendo os resíduos de medicamentos, o presente estudo estabeleceu procedimentos para o seu adequado gerenciamento, contribuindo para a saúde pública e ambiental e podendo servir como fonte de consulta para estimular e orientar novas iniciativas relacionadas ao tema.
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