In vitro approaches to antioxidant screening for the development of a sunscreen formulation

Abstract The incorporation of antioxidants into sunscreens may provide additional skin photoprotection against the harmful photobiological effects of ultraviolet radiation. The present study evaluated the applicability of a screening approach to the assessment of the antioxidant and photoprotective properties of vitamin C, vitamin E, and coenzyme Q10 and then determined the performance of the most effective antioxidant in a sunscreen formulation. Antioxidant activity was assessed by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, 2,2`-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay, and oxygen radical absorbance capacity (ORAC) assay, and the photoprotective potential was investigated by the yeast photoprotection assay. The antioxidant with the best effect was incorporated into sunscreen formulations which were evaluated for 120 days regarding their in vitro photoprotective parameters. Vitamin C showed high antioxidant capacity as well as a photoprotective potential against simulated solar irradiation applied for times longer than 1 h. Although the Sun Protection Factor, UVA/UVB ratio and critical wavelength did not differed significantly (p<0.05) between the formulation blank and the formulations containing 0.5% or 1% vitamin C, formulations with vitamin C kept their photostability for 6 months. Consequently, the proposed screening approach seems to be promising for the development of an antisolar photostable formulation containing vitamin C as an antioxidant.

Nuclear and mitochondrial genome instability induced by fractions of ethanolic extract from Hovenia dulcis Thunberg in Saccharomyces cerevisiae strains.

Hovenia dulcis is a plant commonly used as a pharmaceutical supplement, having displayed important pharmacological properties such antigiardic, antineoplastic and hepatoprotective. The purpose of this work was investigate the cytotoxic, genotoxic and mutagenic potential from fractions of Hovenia dulcis ethanolic extract on Saccharomyces cerevisiae strains FF18733 (wild type) and CD138 (ogg1). Ethanolic extract from Hovenia dulcis leaves was fractioned using organic solvents according to increasing polarity: Hexane (1:1), dichlorometane (1:1), ethyl acetate (1:1) and butanol (1:1). Three experimental assays were performed, such as (i) inactivation of cultures; (ii) mutagenesis (canavanine resistance system) and (iii) loss of mitochondrial function (petites colonies). The findings shown a decrease in cell viability in FF18733 and CD138 strains; all fractions of the extract were mutagenic in CD138 strain; only ethyl acetate and butanol fractions increased the rate of petites colonies for CD138 strains. Ethyl acetate and n-butanol fractions induces mutagenicity, at the evaluated concentrations, in mitochondrial and genomic DNA in CD138 strain, mediated by oxidative lesions. In conclusion, it is possible to infer that the lesions caused by the extract fractions could be mediated by reactive oxygen species and might reach multiple molecular targets to cause cellular damage.

Design, Synthesis and Evaluation of New Fluoroamodiaquine Analogues.

Malaria is one of the most important tropical diseases; the use of amodiaquine as a current chemotherapy in the treatment of malaria has shown some problems such as hepatotoxicity and agranulocytosis. In this work we present the rational design, synthesis, and biological evaluation (antimalarial activity, cytotoxicity and genotoxicity) of four new fluoroamodiaquine analogues. The results showed significant correlation between MolDock score and IC50 values. The molecules 7b and c were the most active of the planned compounds, with lower IC50 against Plasmodium falciparum W2 strain (0.9 and 0.8 µM, respectively) and an excellent cytotoxicity profile. The present study revealed no mutagenicity or genotoxicity for the analogues. Confirming our docking results, the molecular dynamics showed that compound 7b remains stably bound to the heme group by means of π-stacking interactions between quinoline and the porphyrin ring. Based on these findings, this study may prove to be an efficient approach for the rational design of hemozoin inhibiting compounds to treat malaria.

[Pharmaceutical care and attention suspended: compromise-formations between pharmacy and psychoanalysis [corrected]]. / Atenção Farmacêutica e Atenção Flutuante: formações de compromisso entre Farmácia e Psicanálise.

This paper presents an interdisciplinary overview of the rational use of medicine from a metapsychological standpoint. The need to reinstate the activity of the pharmaceutical professionals vis-à-vis their patients through pharmaceutical care demands the intervention of new know-how that can ensure a revitalization of this human relationship. In this sense, by means of a compilation of passages from the works of Freud, some of the most important metapsychological concepts were presented: psychic apparatus, evenly hovering attention and commitment formations. These concepts were then presented as an applicable theoretical tool for qualitative analysis in pharmaceutical care, though especially for participant observation. Thus, the main objective was to provide new tools for the pharmacists in terms of listening and receptivity, which can enhance their professional routine regarding the relationship with their patients, as well as in the gathering and interpretation of qualitative data concerning human issues involving pharmaceutical care.

Atencao Farmaceutica e Atencao Flutuante: formacoes de compromisso entre Farmacia e Psicanalise / Pharmaceutical care and suspended attention: compromise-formations between pharmacy and psychoanalysis

O presente trabalho apresenta uma visão interdisciplinar do uso racional do medicamento a partir de uma perspectiva metapsicológica. A necessidade de resgate da atuação do profissional farmacêutico junto ao paciente, através da Atenção Farmacêutica, demanda a intervenção de novos saberes que possam proporcionar uma revitalização desta relação humana. Neste sentido, através de uma compilação de passagens da obra freudiana, foram apresentados alguns dos principais conceitos metapsicológicos: aparelho psíquico, atenção flutuante e formações de compromisso. Tais conceitos foram então apresentados como ferramenta teórica articulável com análises qualitativas em Atenção Farmacêutica, mais particularmente com a observação participante. Assim, os objetivos principais foram de fornecer ao farmacêutico novas ferramentas de escuta e acolhimento que podem aprimorar a atuação profissional na relação com seu paciente, assim como na obtenção e interpretação de dados qualitativos relacionados às questões humanas envolvidas nas pesquisas em Atenção Farmacêutica.

This paper presents an interdisciplinary overview of the rational use of medicine from a metapsychological standpoint. The need to reinstate the activity of the pharmaceutical professionals vis-à-vis their patients through pharmaceutical care demands the intervention of new know-how that can ensure a revitalization of this human relationship. In this sense, by means of a compilation of passages from the works of Freud, some of the most important metapsychological concepts were presented: psychic apparatus, evenly hovering attention and commitment formations. These concepts were then presented as an applicable theoretical tool for qualitative analysis in pharmaceutical care, though especially for participant observation. Thus, the main objective was to provide new tools for the pharmacists in terms of listening and receptivity, which can enhance their professional routine regarding the relationship with their patients, as well as in the gathering and interpretation of qualitative data concerning human issues involving pharmaceutical care.

In vitro and in vivo influence of penetration enhancers in the topical application of celecoxib.

OBJECTIVE: We investigated the potential effects of oleic acid (OA) and glycerol monooleate (GMO) on the skin delivery of CXB. METHODS: The influence of both OA and GMO (5.0% or 10.0%) on the in vitro skin permeability of CXB (2.0%) was evaluated using propylene glycol (PG) as a vehicle. Also the in vitro potential cytotoxicity and genotoxicity and in vivo assays (skin irritation in rabbits and topical anti-inflammatory activity by in mice) were conducted. RESULTS: As expected, the amount of CXB that permeated through the skin was minimal, but drug retention on the viable skin (epidermis plus dermis) was higher in association with treatment with 5.0% OA or GMO compared to the control treatment, meaning that there was a localized effect of CXB in the skin. No formulation presented cytotoxic or genotoxic potential, suggesting safety for cutaneous application. In vivo skin irritation assays indicated that no formulation was irritating to the skin becomes its use possible for a prolonged time. In vivo anti-inflammatory experiments indicated that both edema and protein extravasation were inhibited with a maximum % inhibition of 53.5.0% and 61.0% for 5.0 % GMO, respectively, and 48.0% and 35.5% for 5.0% OA, respectively. Such formulations were able to inhibit around twofold the percentage of ear edema in mice compared to a commercial product reference diclofenac commercial formula. CONCLUSION: There is no topical formulation currently available that contains both CXB and 5.0% GMO or OA, suggesting them as potential adjuvants that improve the skin delivery of CXB.

Antiophidian sera sterility control: topics in perspective / Controle de esterilidade de soros antiofídicos: temas em perspectiva

The aim of this work is to review the most important topics about the antiophidic sera sterility, including obtaining methods, sterilization procedures and clean room control using Vital Brazil Institute (VBI) as an example. Bibliographical research was performed through Medline, Lilacs, PubMed, ISI and the Fundação Oswaldo Cruz - RJ and VBI Libraries, from 1960 to 2009. The antiophidic sera for human use are immunobiologic products produced in Brazil by three national laboratories, including VBI. Due to the parenteral use, these products should be sterile and pyrogen-free, which demands the microbiological control during the whole fabrication process. The sterility and pyrogen tests are important steps to ensure the quality and safety of these immunobiological products. Thus, these tests are target for continue evaluation and improvement. The most interfering aspects in the consistency and analytical patterns include the proper method selection, sampling, culture conditions and validation criteria. As the national and international legal requirements are cautious with the assays validation and approval of sterile parenteral products; the intrinsic limitations for established assays still require more investigation aiming the continue improvement of the microorganism and contaminants detection methods and optimization of the analysis extent.

O objetivo deste trabalho é revisar os tópicos mais relevantes para o controle da esterilidade de soros antiofídicos, abordando-se métodos de obtenção, procedimentos de esterilização e o controle de áreas limpas utilizando como exemplo os procedimentos adotados pelo Instituto Vital Brazil (IVB). Um levantamento bibliográfico foi realizado no Medline, ISI, Biblioteca da Fundação Oswaldo Cruz-RJ e IVB, no período de 1960 a 2009. Os soros antiofídicos para uso humano são produtos imunobiológicos fabricados no Brasil por três laboratórios nacionais, dentre eles o IVB. Por serem de administração parenteral, devem ser obrigatoriamente estéreis e apirogênicos, exigindo controle microbiológico durante todo o processo de fabricação. O teste de esterilidade e apirogenia são importantes instrumentos para garantir a qualidade e segurança microbiológica desses produtos, sendo alvo de avaliações constantes para seus aprimoramentos. Os aspectos que mais interferem na sua consistência e valor analítico incluem a escolha adequada do método, amostragem, condições de cultivo e critérios de validação. À medida que os requisitos legais nacionais e internacionais se mostram rigorosos na validação de ensaios e aprovação de produtos estéreis parenterais, limitações intrínsecas ao ensaio padronizado requisitam mais investigações, objetivando o aprimoramento contínuo nos métodos de detecção de microorganisms, contaminantes e otimização do tempo total de análise.