ABSTRACT Leishmaniasis is a disease that affects millions of people and it is an important public health problem. The drugs currently used for the treatment of leishmaniasis present undesirable side effects and low efficacy. In this study, we evaluated the in vitro activity of Melampodium divaricatum (MD-EO) and Casearia sylvestris (CS-EO) essential oils (EO) against promastigote and amastigote forms of Leishmania amazonensis. Sesquiterpenes E-caryophyllene (56.0%), germacrene D (12.7%) and bicyclogermacrene (9.2%) were identified as the main components of MD-EO, whereas E-caryophyllene (22.2%), germacrene D (19.6%) and bicyclogermacrene (12.2%) were the main constituents of CS-EO. CS-EO and E-caryophyllene were active against promastigote forms of L. amazonensis (IC50 24.2, 29.8 and 49.9 µg/mL, respectively). However, MD-EO, CS-EO and E-caryophyllene were more active against amastigote forms, with IC50 values of 10.7, 14.0, and 10.7 µg/mL, respectively. E-caryophyllene presented lower cytotoxicity against macrophages J774-A1 (CC50 of 62.1 µg/mL) than the EO. The EOs and E-caryophyllene should be further studied for the development of new antileishmanial drugs.

Uma fração oleaginosa obtida do extrato etanólico de frutos de Pterodon pubescensBenth (FHPp) foi microencapsulada em um sistema polimérico. Estes sistemas foram desenvolvidos utilizando o método de coacervação complexa, constituído de alginato/quitosana massa molecular média (F1-MC), alginato/quitosana com desacetilação superior a 75% (F2-MC) e alginato/quitosana de massa molecular baixa (F3-MC). Estes sistemas desenvolvidos têm o potencial tanto de mascarar o sabor do extrato, quanto de protegê-lo de possível degradação química. A influência dos parâmetros de formulação e processo foram determinadas por caracterização química, determinação da eficiência de microencapsulação da fração oleaginosa e por avaliação morfológica da microcápsula. As formulações mostraram-se ligeiramente amareladas, inodoras e com sabor agradável. Os diâmetros médios das microcápsulas foram de 0,4679 µm (F2-MC), 0,5885 µm (F3-MC) e 0,9033 µm (F1-MC). A melhor formulação foi F3-MC, considerando-se que apresentou eficiência de encapsulação de 61,01 ± 2,00%, e perfil de liberação in vitro de 75,88 ± 0,45%; o conteúdo dos vouacapanos 3-4 foi 99,49 ± 2,80%. O melhor modelo para descrever a cinética de liberação foi o modelo proposto por Higuchi para F1-MC e F3-MC, entretanto, para F2-MC foi o modelo de primeira ordem, e o mecanismo de liberação foi do tipo super caso II para todas as formulações.

An oleaginous fraction obtained from an alcohol extract of the fruit of Pterodon pubescensBenth. (FHPp) was microencapsulated in polymeric systems. These systems were developed using a complex coacervation method and consisted of alginate/medium-molecular-weight chitosan (F1-MC), alginate/chitosan with greater than 75% deacetylation (F2-MC), and alginate/low-molecular-weight chitosan (F3-MC). These developed systems have the potential to both mask the taste of the extract, and to protect its constituents against possible chemical degradation. The influence of the formulation parameters and process were determined by chemical profiling and measurement of the microencapsulation efficiency of the oleaginous fraction, and by assessment of microcapsule morphology. The obtained formulations were slightly yellow, odorless, and had a pleasant taste. The average diameters of the microcapsules were 0.4679 µm (F2-MC), 0.5885 µm (F3-MC), and 0.9033 µm (F1-MC). The best formulation was F3-MC, with FHPp microencapsulation efficiency of 61.01 ± 2.00% and an in vitro release profile of 75.88 ± 0.45%; the content of vouacapans 3-4 was 99.49 ± 2.80%. The best model to describe the release kinetics for F1-MC and F3-MC was that proposed by Higuchi; however, F2-MC release displayed first-order kinetics; the release mechanism was of the supercase II type for all formulations.

A sensitive RP-HPLC method with UV detection successfully measured phenol(s) in an ointment containing 3% Stryphnodendron adstringens extract. Chromatography used acetonitrile (0.05% trifluoroacetic acid):water (0.05% trifluoroacetic acid) (v/v), flow rate 0.8 mL min-1. Quantitation was accomplished by the external-standard method. Linearity for 2.00 to 16.00 μg mL-1 (gallic acid) and 1.14 to 18.24 μg mL-1 (gallocatechin) was established. Intra- and inter-day precision levels were under 5%. LOD and LOQ were 0.231 and 0.770 μg mL-1 (gallic acid) and 0.151 and 0.504 μg mL-1 (gallocatechin), respectively. Determination of phenols was unaffected by product excipients.

A qualidade de preparações fitofarmacêuticas deve ser avaliada de acordo com os requisitos estabelecidos pela Agência Nacional de Vigilancia Sanitária na RDC n. 48 (ANVISA-BRASIL). As análises para avaliar a integridade dos produtos da droga vegetal incluem a quantificação de substâncias marcadoras através de métodos validados. O trabalho objetivou quantificar cafeína e polifenóis totais em soluções extrativas e no granulado obtidos das sementes de P. cupana var. sorbilis através de método espectrofotométrico. O método apresentou linearidade para a cafeína e polifenóis no intervalo de 5-25 µg/ml e 2,4-5,6 µg/ml, respectivamente. Soluções da fração semipurificada (EPA) e do granulado (GRA) mostraram resposta linear no intervalo de 0,288-0,672 µg/ml e 0,4-1,2 µg/ml respectivamente. A precisão e exatidão foram determinadas para a solução de EPA na concentração de 100 µg/ml. O método espectrofotométrico obteve um bom desempenho na quantificação de cafeína e polifenóis totais, uma vez que a presença de interferentes foi previamente avaliada.

The present work was designed to quantify the caffeine and total polyphenols in the extractive solution and the granulated form from the seeds of Paullinia cupana var. sorbilis, by the spectrophotometric method. The method showed linearity for the caffeine and polyphenols in the range of 5-25 µg/ml and 2.4-5.6 µg/ml respectively. The solutions of the semipurified fraction (EPA) and granulated form (GRA) showed linear responses in the range of 0.288-0.672 and 0.4-1.2 µg/ml, respectively. The precision and accuracy were determined for the EPA solution at a concentration of 100 µg/ml. The spectrophotometric method performed well in quantifying the caffeine and total polyphenols.