Association of Rhizophora mangle and ascorbic acid in hydrogels: Evaluation of cytotoxic and immunomodulatory effects

Abstract Polyphenolics from Rhizophora mangle (R. mangle) have shown wound healing and anti- inflammatory effects that may be potentiated by being associated with ascorbic acid, an important substance for collagen and elastin synthesis that plays a role in tissue repair. In our study, we aimed to formulate an association of R. mangle and ascorbic acid in hydrogels and evaluate the association's cytotoxic and immunomodulatory effects. In a pre-formulation study, three gelling polymers (i.e.xanthan gum, poloxamer and hydroxyethyl cellulose) were tested. The selected polymer (i.e. xanthan gum) was used to evaluate cytotoxic and immunomodulatory effects using flow cytometry. Xanthan gum (1.5%) had a homogeneous appearance, an orange colour, a smooth surface, intense brightness and the typical odour, as well as non-Newtonian pseudoplastic behaviour. With a pH of 5.0-5.3 and a non-cytotoxic profile, xanthan gum induced the proliferation and activation of CD4 +, CD8+ and NK T lymphocytes and the production of IL- 2, IL-4, IL-10, IL-17 and TNF-α cytokines in stimulated splenocytes. The results suggest that the association of R. mangle and ascorbic acid in 1.5% xanthan gum hydrogel may be promising in preparations for wound-healing processes.

Mupirocin ointments: In vitro x In vivo bioequivalence evaluation

Abstract Bioequivalence (BE) assessment of topical drug products is a long-standing challenge. Agencies such as the Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have published several drafts in recent years suggesting different approaches as alternative to evaluate the BE. A proposed Topical Classification System (TCS) has even been discussed. Given the above, the objective of this research was to use in vitro and in vivo BE approaches to evaluate Brazilian marketed mupirocin (MPC) ointments, previously classified as TCS class The in vitro permeation test (IVPT) was performed by applying formulations to pig skin by Franz cells. The in vivo methodology was dermatopharmacokinetic (DPK). These approaches (in vivo tape stripping and IVPT) demonstrated capability of distinguishing among different formulations, thus making them useful methodologies for BE evaluation.

Critical analysis on the use of cholecalciferol as a COVID-19 intervention: a narrative review

ABSTRACT BACKGROUND: The World Health Organization has declared that a pandemic situation exists in relation to the disease caused by the new coronavirus, COVID-19. So far, the absence of a vaccine against the new coronavirus has led people worldwide to seek various therapeutic alternatives, including use of cholecalciferol. DESIGN AND SETTING: Narrative review developed by a research group at a public university in Recife (PE), Brazil. METHODS: We searched the literature on the use of cholecalciferol for prevention or treatment of COVID-19, using the MEDLINE and LILACS databases, with the keywords "vitamin D", "cholecalciferol", "SARS-CoV-2", "COVID-19" and "coronavirus", from January 1, 2020, to June 10, 2020. Narrative reviews, cohort studies and ecological studies were selected. RESULTS: We retrieved 32 references, of which 8 were considered eligible for intensive review and critical analysis. These comprised five narrative reviews, two observational studies and one protocol proposal. Most of the studies selected reported positive effects from use of vitamin D for prevention or treatment of COVID-19. However, there was little quantitative data to assess the real impact of using this vitamin as an intervention against this disease. CONCLUSIONS: Current studies on vitamin D used for purposes other than bone health promotion cannot be taken as support to justify its use in a disease as recent as COVID-19. Studies of greater robustness, with higher levels of clinical evidence, need to be conducted. Rational use of this vitamin needs to be ensured, thereby minimizing the impacts on the patient and the public healthcare system.

Percepção olfativa e gustativa na doença de Parkinson / Olfative and taste perception in Parkinson's disease

RESUMO Objetivo Analisar a percepção e discriminação olfativa e gustativa e a autopercepção do olfato e paladar em pessoas com Doença de Parkinson, comparando-as com indivíduos hígidos. Método Estudo observacional, analítico, transversal e quantitativo. Verificou-se a percepção e a discriminação olfativa e gustativa em indivíduos com Doença de Parkinson, comparados a um grupo controle, pareado por sexo e idade, por meio dos Testes de Percepção Olfativa e de Tiras Gustativas, respectivamente, após limpeza nasal e escovação oral. A autopercepção foi avaliada pela Escala Visual Analógica antes e após os testes específicos de percepção e discriminação. Resultados Foram incluídos indivíduos de ambos os sexos, sendo 35 com Doença de Parkinson e 20 designados ao grupo controle, pareados pela média de idade. A autopercepção olfativa do grupo com Doença de Parkinson melhorou após o teste olfativo. Não houve diferença na autopercepção gustativa no grupo Doença de Parkinson antes e após o teste gustativo. No teste de avaliação da percepção olfativa, o grupo Doença de Parkinson discriminou menos essências que o grupo controle. Ambos os grupos apresentaram semelhante percepção e discriminação gustativa. Conclusão A percepção olfativa das pessoas com Doença de Parkinson foi menor, comparativamente ao grupo de indivíduos hígidos e a autopercepção da eficácia olfativa melhorou após o teste, em ambos os grupos. Quanto ao paladar, não houve diferença na percepção e discriminação entre os grupos, o sabor azedo foi o mais identificado e houve melhora na autopercepção da eficácia gustativa somente no grupo sem a doença de Parkinson, após o teste.

ABSTRACT Purpose To analyze the olfactory and gustatory perception and discrimination and self-perception of smell and taste in people with Parkinson's disease, comparing them with healthy nodes. Methods Observational, analytical, cross-sectional, and quantitative study. Olfactory and gustatory perception and discrimination were verified following Parkinson's disease, compared to a control group, matched by sex and age, using the Olfactory Perception and Taste Strips Tests, respectively, after nasal cleaning and oral brushing. Self-perception was assessed by the Visual Analogue Scale before and after specific tests of perception and discrimination. Results We included individuals of both sexes, 35 with Parkinson's Disease and 20 assigned to the control group, matched for mean age. The olfactory self-perception of the group with Parkinson's disease improved after the olfactory test. There was no difference in taste self-perception in the Parkinson's disease group before and after the taste test. In the olfactory perception assessment test, the Parkinson's disease group discriminated fewer essences than the control group. Both groups have similar generation and taste discrimination. Conclusion The olfactory perception of people with Parkinson's disease was lower, compared to the group of healthy desires, and the self-perception of olfactory efficacy improved after the test, in both groups. As for taste, there was no difference in perception and discrimination between groups, the sour taste was the most identified and there was an improvement in self-perception of taste efficiency in the group without Parkinson's disease after the test.

Metronidazole thermogel improves retention and decreases permeation through the skin

ABSTRACT Metronidazole (MTZ) is widely used as the standard antibiotic for the treatment of rosacea and, more recently, is being used off label in Brazilian hospitals for the treatment of wounds. Following oral administration, minimal amounts of active agent reaches the skin and side effects are strongly induced. Consequently, MTZ is currently being applied topically in order to improve the therapeutic efficacy with reduced side effects, with Rozex(r) (RZ) (an MTZ gelled formulation) being the only marketed product. This study examined whether the use of MTZ 0.75% from thermogel formulations could improve drug retention and reduce dermal exposure compared to that by Rozex(r). Following a 21 h permeation study, the highest total amount of MTZ permeated through the rat healthy and disturbed skin was seen with Rozex(r), but similar to all formulations regardless of the skin condition. On the other hand, the amount retained in the epidermis/dermis was larger for thermogel formulations; at least 4 fold that of Rozex(r), when the stratum corneum was present as a barrier. In conclusion, thermogel formulations can be favorable alternatives to Rozex(r) for the topical application of MTZ with improved efficacy and reduced side effects.

Disfuncao gustatoria e olfatoria em laringectomizados / Gustatory and olfactory dysfunction in laryngectomized patients

Após a cirurgia de laringectomia total, o fluxo aéreo nasal é transferido definitivamente para o traqueostoma, comprometendo a chegada de moléculas odoríferas até a cavidade nasal, podendo repercutir em alterações na percepção olfatória e gustatória nesses indivíduos. OBJETIVO: Avaliar as funções do olfato e do paladar em laringectomizados totais. Desenho do estudo: Estudo de série. MÉTODO: A amostra envolveu um grupo com 25 pacientes submetidos à laringectomia total e outro grupo de comparação com 25 pacientes não laringectomizados. A função gustatória foi avaliada por tiras gustativas de papel de filtro. Para avaliação da função olfatória, foi aplicado o teste Brief Smell Identification Test. RESULTADOS: No grupo de laringectomizados, houve maior frequência de hipogeusia (80%; p < 0,05), assim como de hiposmia (88%; p < 0,001), isoladas e concomitantes (72%; p < 0,001). Na discriminação dos sabores, o sabor amargo não diferiu entre os grupos, diferentemente dos demais sabores. No aspecto olfatório, os laringectomizados tiveram pior desempenho na detecção de odores de alerta e os relacionados à alimentação. Identificou-se que história de tabagismo e de alcoolismo foi significantemente mais frequente dentre laringectomizados. CONCLUSÃO: A diminuição das funções olfatória e gustatória em laringectomizados totais foi evidenciada nesse estudo. .

After total laryngectomy surgery, nasal airflow is moved permanently to the tracheostomy opening, compromising the contact of odorant molecules with the nasal cavity, which may reflect changes in the olfactory and gustatory perception in these individuals. OBJECTIVE: To evaluate the functions of smell and taste in total laryngectomized patients. Study design: a study of series. METHOD: The sample included a group of 25 patients submitted to total laryngectomy and another group of 25 patients who did not underwent the procedure. The taste function was evaluated by gustatory strips of filter paper. To assess the olfactory function we employed the Brief Smell Identification Test. RESULTS: Among the laryngectomized patients there was more hypogeusia (80%, p < 0.05), as well as hyposmia (88%, p < 0.001), alone and concomitant (72%, p < 0.001). Concerning flavor discrimination, the bitter taste did not differ between the groups - which was different from the other flavors. In the olfactory aspect, laryngectomized patients performed worse in detecting warning and food-related odors. We found that a history of smoking and alcohol consumption were significantly more frequent among laryngectomized patients. CONCLUSION: We found a decrease of gustatory and olfactory functions in total laryngectomized patients in this study. .

Análise e estudo viscosimétrico de diferentes géis de cetoprofeno 2.5% / Analysis and viscosimetric study of various 2.5% ketoprofen gels

O cetoprofeno é um fármaco pertencente à classe dos anti-inflamatórios não-esteroidais, inibe a síntese de prostaglandinas promovendo um potente efeito analgésico e anti-inflamatório. Para uso tópico, está disponível como medicamento de referência e diversos genéricos sob a forma gel 2,5%, além das preparações manipuladas em farmácias magistrais, adquiridas mediante receita médica. Este estudo objetivou avaliar a qualidade do cetoprofeno gel 2,5% manipulado em duas farmácias do Recife (PE) e, posteriormente, compará-lo ao medicamento de referência e a um genérico correspondente. Os resultados das análises mostraram que medicamentos referência e o genérico apresentaram, de forma geral, características semelhantes. As formulações magistrais também mostraram características próximas entre si, mas diferentes dos industrializados, indicando a necessidade de reformulação destas preparações magistrais avaliadas, como obediência à legislação vigente RDC 67/2007 da Agência Nacional de Vigilância Sanitária.

Ketoprofen is a non-steroidal anti-inflammatory drug that inhibits prostaglandin synthesis and promotes a strong analgesic and anti-inflammatory effect. For topical use, it is available as a reference drug as well as several generic preparations in gel at 2.5%, apart from preparations compounded in pharmacies and sold under medical prescription. The aim of this study was to assess the quality of 2.5% ketoprofen gels compounded in two pharmacies in Recife and then compare them with a reference drug and a corresponding generic drug. The results of the analysis show that the generic and reference drugs display, in general, similar characteristics. The compounded formulations also had similar characteristics, when compared to each other, but were different from the manufactured gels. These results indicate that these compounded preparations must be reformulated to comply with RDC 67/2007, the current regulation issued by the National Agency of Sanitary Surveillance (ANVISA).

Determination of the critical hydrophile-lipophile balance of licuri oil from Syagrus coronata: application for topical emulsions and evaluation of its hydrating function

The aims of this study were to determine the critical hydrophile-lipophile balance (HLB) of licuri oil, and to perform a clinical assay to evaluate its hydrating effects. For the determination of the HLB, serial emulsions were prepared with the oil. Regarding the clinical study, 13 human subjects were recruited to evaluate the hydrating power of the emulsified preparation containing licuri oil, and comparing it with the same preparation containing sweet almond oil (SAO). The critical HLB of licuri oil was represented by the zones within the concentrations of 10% for the oil and 15% for the pair of tensoactive agents, with a value of 11.8. Both preparations showed similar hydrating power. We propose that licuri oil can be considered a new lipophilic adjuvant with hydrating characteristics, which can be used in cosmetic preparations, replacing consecrated oils, such as SAO.

O objetivo deste estudo foi determinar o EHL crítico do óleo licuri e realizar um ensaio clínico para avaliar os seus efeitos hidratantes. Para a determinação do EHL foram preparadas emulsões seriadas contendo esse óleo. Em relação ao estudo clínico, avaliamos o poder hidratante de preparação emulsionada com óleo de licuri, comparando-a com a mesma preparação contendo óleo de amêndoas doces (OAD), em 13 voluntários. O EHL crítico do óleo de licuri foi representado pelas zonas dentro das concentrações de 10% para o óleo e 15% para o par de tensoativos, com um valor de 11,8 e ambas as preparações mostraram poder hidratante similar. Desta forma, o óleo de licuri pode ser considerado um novo adjuvante lipofílico com função hidratante, o qual pode ser usado em preparações cosméticas, substituindo óleos de consagrado uso, tais como o OAD.

Consumption of medicines in high-risk pregnancy: evaluation of determinants related to the use of prescription drugs and self-medication

The use of drugs during pregnancy still represents a challenge for medicine, since the majority of drugs cross the placental barrier with a potential to cause several congenital problems to the fetus, and most of them have not been clinically tested in pregnant patients. At the same time, the medicalization phenomenon, self-medication, and lack of patient information about the misuse of medicines are additional problems. Thus, the aim of this study was to evaluate the pattern of medicine consumption in high-risk pregnancies and the determinants related to this consumption pattern. In order to do so, a cross-sectional descriptive study was performed with puerperal women who had a history of high-risk pregnancy. Statistically significant associations were found between self-medication and fewer prenatal visits, and cigarette use during pregnancy and a higher number of children. According to these data, the vulnerability of this population to the risks of drug use is evident, demonstrating a gap that requires urgent interventions in health-care education.

O uso de medicamentos na gestação representa, ainda hoje, um desafio para a medicina, visto que grande parte dos fármacos atravessa a barreira placentária e, na maioria, não foi testada clinicamente em gestantes, podendo vir a ocasionar diversos problemas congênitos ao feto. Ao mesmo tempo, a automedicação, o fenômeno da medicalização e a falta de informação sobre os riscos do mau uso de medicamentos são problemas adicionais. Diante disto, o objetivo deste estudo consistiu em avaliar o padrão de consumo de medicamentos na gestação de alto risco e os determinantes relacionados ao seu padrão de consumo. Para tanto, realizou-se um estudo descritivo de corte transversal com puérperas, que apresentaram gestação de alto risco. Verificaram-se associações estatisticamente significativas entre automedicação e mulheres com menor número de consultas de pré-natal, uso de cigarro na gestação e maior número de filhos. De posse destes dados, fica evidente a vulnerabilidade dessa população aos riscos decorrentes do uso de medicamentos, sendo esta lacuna um campo de prática com necessidade de intervenções urgentes no âmbito da educação em saúde.

Assay and physicochemical characterization of the antiparasitic albendazole

The aim of this study was to characterize three batches of albendazole by pharmacopeial and complementary analytical techniques in order to establish more detailed specifications for the development of pharmaceutical forms. The ABZ01, ABZ02, and ABZ03 batches had melting points of 208 ºC, 208 ºC, and 209 ºC, respectively. X-ray diffraction revealed that all three batches showed crystalline behavior and the absence of polymorphism. Scanning electron microscopy showed that all the samples were crystals of different sizes with a strong tendency to aggregate. The samples were insoluble in water (5.07, 4.27, and 4.52 mg mL-1, respectively) and very slightly soluble in 0.1 M HCl (55.10, 56.90, and 61.70 mg mL-1, respectively) and additionally showed purities within the range specified by the Brazilian Pharmacopoeia 5th edition (F. Bras. V; 98% to 102%). The pharmacopeial assay method was not reproducible and some changes were necessary. The method was validated and showed to be selective, specific, linear, robust, precise, and accurate. From this characterization, we concluded that pharmacopeial techniques alone are not able to detect subtle differences in active pharmaceutical ingredients; therefore, the use of other complementary techniques is required to ensure strict quality control in the pharmaceutical industry.

O objetivo do trabalho foi caracterizar três lotes de albendazol com técnicas analíticas farmacopéicas e complementares a fim de estabelecer especificações mais detalhadas para o desenvolvimento de formas farmacêuticas. Os lotes ABZ01, ABZ02 e ABZ03 apresentaram fusão em 208 ºC, 208 ºC e 209 ºC. Foi possível evidenciar, por difração de raios X, que os três lotes apresentaram comportamento cristalino e ausência de polimorfismo. Através da microscopia eletrônica de varredura verificou-se que todas as amostras apresentaram cristais com diferentes tamanhos e forte tendência de agregação. As amostras foram insolúveis em água (5,07; 4,27 e 4,52 µg mL-1) e muito pouco solúveis em HCl 0,1M (55,10; 56,90 e 61,70 µg mL-1) e, ainda, apresentaram pureza dentro da faixa especificada pela F.Bras.V (98% a 102%). O método farmacopéico de doseamento não foi reprodutível, e algumas mudanças foram necessárias. O método foi validado e demonstrou ser seletivo, específico, linear, robusto, preciso e exato. A partir dessa caracterização, pode-se concluir que apenas técnicas farmacopéicas não são capazes de detectar diferenças sutis entre os ingredientes farmacêuticos ativos, necessitando, portanto, de uso de outras técnicas complementares para garantir um rígido controle de qualidade na indústria farmacêutica.