Preparations from Pimenta pseudocaryophyllus (Gomes) L.R. Landrum (Myrtaceae) have been widely used in Brazilian folk medicine. This study aims to evaluate the antimicrobial activity of the crude ethanol extracts, fractions, semipurified substances, and essential oils obtained from leaves of two chemotypes of P. pseudocaryophyllus and to perform the antinociceptive and anti-inflammatory screening. The ethanol extracts were purified by column chromatography and main compounds were spectrally characterised (1D and 2D 1H and 13C NMR). The essential oils constituents were identified by GC/MS. The broth microdilution method was used for testing the antimicrobial activity. The abdominal contortions induced by acetic acid and the ear oedema induced by croton oil were used for screening of antinociceptive and anti-inflammatory activities, respectively. The phytochemical analysis resulted in the isolation of pentacyclic triterpenes, flavonoids, and phenol acids. The oleanolic acid showed the best profile of antibacterial activity for Gram-positive bacteria (31.2–125 μg mL−1), followed by the essential oil of the citral chemotype (62.5–250 μg mL−1). Among the semipurified substances, Ppm5, which contained gallic acid, was the most active for Candida spp. (31.2 μg mL−1) and Cryptococcus spp. (3.9–15.6 μg mL−1). The crude ethanol extract and fractions from citral chemotype showed antinociceptive and anti-inflammatory effects.

A isotretinoína, quimicamente conhecida como ácido-13-cisretinóico, faz parte do amplo grupo de compostos relacionados à vitamina A. É empregada particularmente no tratamento da acne cística e nodular e como inibidor da proliferação de células neoplásicas, por exercer efeito regulador sobre a diferenciação celular. Os efeitos adversos envolvendo o uso de isotretinoína estão relacionados à pele e membranas mucosas, sistemas nervoso, músculo esquelético, linfático, gastrintestinal, cardiorespiratório e geniturinário. A isotretinoína é um composto termo e fotossensível e, por assim se apresentar, desperta o interesse pelo estudo de sua estabilidade, empregando-se para isso várias metodologias analíticas como a CLAE, CG, análise térmica, espectroscopia de massa, microcalorimetria, difratometria de raios-X e muitas outras que devem ser selecionadas de acordo com o interesse do pesquisador.

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This article reports the development of a pharmaceutical product containing vegetable actives from a Brazilian medicinal plant. The possibility of forming a microemulsion using Pterodon emarginatus ("sucupira") oil was evaluated and the anti-inflammatory potential of this microemulsion was also examined. A formulation was developed using P. emarginatus oil, a mixture of ethoxylated Castor Oil (Ultramone ® R-540/propylene glycol 2:1) (surfactant/cosurfactant) and distilled water at a ratio of 10:15:75, respectively. The microemulsion which was selected was then subjected to the preliminary stability test and analyzed in terms of average diameter of droplets, pH, zeta potential, and polydispersity index, on the 1 st , 7 th , 15 th , and 30 th days after preparation and stored at different temperatures (5 ± 2 °C, 25 ± 2 °C, and 40 ± 2 °C). The anti-inflammatory in vivo activity of both oil and formulation were evaluated, using the experimental model of croton oil-induced ear edema. The preliminary stability test showed that the microemulsion stored at 5 and 25 °C retained its original features throughout the 30-day period. The anti-inflammatory potential of both oil and formulation was shown to be statistically significant (p < 0.001), when compared to the control group, however, the microemulsion proved to be more effective (p < 0.05) than the oil when applied directly to the ear. Descrevemos o desenvolvimento de um produto farmacêutico contendo ativo vegetal baseado em uma planta medicinal brasileira. Foi avaliada a habilidade de formação de uma microemulsão à base do óleo de Pterodon emarginatus (sucupira) e seu potential anti-inflamatório. Uma formulação foi desenvolvida utilizando o óleo de P. emarginatus, mistura de óleo de mamona etoxilado (Ultramona ® R-540)/propilenoglicol (2:1) (tensoativo/cotensoativo) e água destilada, na proporção de 10:15:75, respectivamente. A microemulsão selecionada foi submetida ao teste preliminar de estabilidade e foi analisada quanto ao diâmetro médio das gotículas, pH, potential zeta e índice de polidispersão, no 1º, 7º, 15º e 30º dias após o preparo e foram estocadas em diferentes temperaturas (5±2 °C, 25±2 °C e 40±2 °C). Avaliaram-se a atividade anti-inflamatória in vivo do óleo de sucupira e da formulação, usando o modelo experimental do edema de orelha induzido pelo óleo de cróton. No teste preliminar de estabilidade observou-se que a formulação estocada a 5 °C e a 25 °C mantiveram suas características originais durante 30 dias. O potencial anti-inflamatório de ambos, óleo de sucupira e formulação foi estatisticamente significativo (p <0.001), quando comparado ao controle, porém a microemulsão foi mais eficiente (p <0.05) que o óleo aplicado diretamente nas orelhas dos animais. Unitermos:Pterodon emarginatus/pharmacognosy. Pterodon emarginatus/óleo/atividade antiinflamatória. Plantas medicinais. Microemulsão. Fitoterápico. Tecnologia farmacêutica.

The isoflavone genistein (GEN) is a natural product with potential applications for skin cancer treatment and chemoprevention; however its high lipophilicity and chemical instability limits its clinical use. Therefore, attempts towards protecting GEN against degradation and increasing its penetration in the skin might be a valid approach. In this work, GEN loaded-PLA nanocapsules (GEN-NC) were prepared by interfacial deposition of preformed polymer (nanoprecipitation); physicochemical characterization and stability studies for 90 days were conducted. GEN-NC were incorporated into semi-solid formulations and permeation experiments were carried out using porcine ear skin. GEN-NC optimized formulation presented a mean diameter of 139 +/- 7.31 nm, polydispersity index of 0.128 +/- 0.08, encapsulation efficiency of 89.63 +/- 2.27% and drug loading from 0.6 to 1.4 w/w%. Stability studies demonstrated that nanocapsules did not exhibit aggregation during the 90 days of the assay, however, a drop in encapsulation efficiency was observed in the first 10 days. Permeation experiments demonstrated that a higher amount of GEN reaches deeper layers of the skin and increased penetration was achieved when GEN-NC were incorporated in a semi-solid gel formulation, indicating that GEN-NC might be a promising nanocarrier system for skin delivery of GEN.

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"Guaraná" (Paullinia cupana) is used as a physical activity enhancer and stimulator due to its methylxanthines and condensed tannins. The aim of this work was to evaluate the dissolution behavior of five herbal medicines in the form of capsules and tablets containing guaraná. Assay and dissolution methods were validated and results obtained allowed simultaneous marker quantification with precision, accuracy, selectivity and robustness. Findings showed that 100% of the herbal medicinal products analyzed did not provide satisfactory results concerning the presence of four markers, 60% had three markers (caffeine, catechin and epicatechin), while 40% had only caffeine at tested dosage forms. In addition, after 30 minutes, only capsule A showed at least 80% of the dissolved markers. In other capsules, marker dissolution did not exceed 60% whereas 60% of the samples had some characteristic pharmacotechnical problems. These results evidence the need for rigorous quality control to help ensure the therapeutic action of these drugs. To this end, dissolution studies are an essential tool for quality assurance of herbal medicines. Uniterms:Herbal medicines/quality control. Herbal medicines/dissolution behavior. Medicinal plants. Guaraná/pharmacognosy. Paullinia cupana/pharmacognosy. Guaraná (Paullinia cupana) é utilizado como revigorante e estimulante devido à presença de metilxantinas e taninos condensados. Este trabalho visou avaliar o comportamento de dissolução de cinco fitoterápicos, na forma de cápsulas e comprimidos, contendo guaraná. O método de quantificação e de dissolução foram validados e os resultados obtidos permitiram a quantificação dos marcadores simultaneamente, com precisão, exatidão, seletividade e robustez. Foi verificado que 100% dos fitoterápicos analisados encontravam em desacordo quanto à presença dos quatro marcadores, sendo que 60% apresentaram três marcadores (cafeína, catequina e epicatequina) e 40% apresentaram somente a cafeína. Além disso, após o tempo de 30 minutos de ensaio foi possível observar que somente a cápsula A apresentou pelo menos 80% dos marcadores dissolvidos. Nas demais cápsulas o comportamento de dissolução apresentado pelos marcadores não ultrapassou 60% e, além disso, 60% das amostras apresentaram alguns problemas farmacotécnicos característicos. Frente aos resultados obtidos torna-se evidente a necessidade de um rigoroso controle de qualidade que contribua para assegurar a ação terapêutica desses medicamentos e, nesse sentido, o estudo de dissolução constitui uma ferramenta essencial para a garantia de qualidade dos fitoterápicos.Unitermos: Fitoterápicos/controle de qualidade. Fitoterápicos/comportamento de dissolução. Plantas medicinais. Guaraná/farmacognosia. Paullinia cupana/farmacognosia.

Enalapril maleate (EM) is a widely used anti-hypertensive drug which is unstable when mixed with excipients. Enalaprilate and diketopiperazine (DPK) are the main degradation products of enalapril. The in situ preparation of enalapril sodium salt (NaE) has been used to improve drug stability in dosage forms; however, gas release and product rejection ensue when the chemical reaction for obtaining the sodium salt is not completely finished before packaging. This study evaluated the effect of stearic acid (SA) on enalapril stability in microcrystalline cellulose (MCC) pellets containing EM or NaE. MCC pellets containing SA were prepared by the extrusion-spheronization technique and characterized. Enalapril stability and dissolution were then evaluated. DPK and enalaprilate formation were reduced by the addition of SA in pellets containing EM. The overall enalapril degradation in these formulations was lower when compared with pellets containing EM or even NaE prepared without SA. The immediate-release characteristic was maintained by the addition of 5% crospovidone to all the formulations tested. The incorporation of SA into NaE pellets resulted in unexpected enalapril degradation, caused by the interaction of these compounds, as suggested by a thermal analysis of the SA-NaE binary mixture. The findings presented here showed that formulations containing SA could substitute the formation of NaE, since they provide better enalapril stability in solid dosage forms. In addition, it is suggested that the stabilization effects would be observed for other N-carboxyalkyl dipeptide analogs with angiotensin converting enzyme inhibition activity, since these new entities share the same degradation pathway of enalapril.