Abstract This study showcases the clinical efficacy of mucoadhesive patches designed for the buccal delivery of lidocaine and prilocaine hydrochlorides (1:1, 30 mg/patch). Such patches were developed for needle-free pre-operative local anesthesia in dentistry, aiming at mitigating the use of infiltrative anesthesia for medium-complexity clinical procedures. The patches were manufactured encompassing drug-release, mucoadhesive and backing layers, all prepared through film casting using biocompatible materials. Fifty-eight (n = 58) adult patients (65% women and 35% men) were randomly selected and included in a one-arm open clinical prospective cohort study. The average age of the subjects was of 50 years. The majority (59%) of the subjects, mostly women (82%), reported needle-phobia or anxiety due to dental procedures, which was assessed through a questionnaire approved by the ethical council for human use in research. The patches were positioned in the gingival region of the teeth involved in the procedure (86% on the maxillary and 14% on the mandibular bone). Two anesthetic patches were applied on each patient: one in the vestibular region and another in the palate/lingual portion, and these patches remained attached to the placement sites throughout the procedures. Concerning the dental procedures performed, 40% were cavity preparations and dental restorations of medium cavities; 29% staple facilities; 10% gingival retractions; 9% subgingival scrapings; 3% gingivalplasties; 3% supragingival preparations; 3% occlusal adjustments; and 2% subgingival preparations. In 90% of the cases, it was not necessary to complement with conventional infiltrative local anesthesia during the procedures. Patients did not report any discomfort or side effect during or after the administration of the patches. Among the cases in which there was the need for complementation, 50% were cavity preparations and dental restorations; 33% supragingival preparations; and 17% gingivoplasties. The complementary anesthesia volume was of 0.63 ± 0.23 mL and women corresponded to 83% of the participants who needed such intervention. Furthermore, in most cases, the patch was capable of initiating the anesthesia within a short time frame (5 minutes) and reaching the maximum anesthetic effect within 15 and 25 min, lasting at least 50 min. Undesirable side effects were not reported either 2 h after the administration or within the 6-month follow-up. Therefore, the anesthetic patches developed provide needle-free, painless, safe, and patient/dentist-friendly advances in performing routine medium-complexity dental procedures.

Resumo Apresentamos o conteúdo fenólico, o comportamento redox e o potencial antioxidante de vários chás medicinais selecionados do mercado brasileiro. As amostras foram classificadas como simples (uma única erva) ou compostas (mistura de duas ou mais ervas). Abordagens estatísticas multivariadas complementares foram utilizadas para esclarecer as correlações e interdependências entre as características físico-químicas e antioxidantes dos produtos. No geral, as concentrações de polifenóis e flavonoides totais se correlacionaram com a viabilidade termodinâmica da redução de espécies reativas de oxigênio. A modelagem estatística diferenciou os conjuntos de dados em componentes principais, de modo que o teor de flavonoides se apresentou como o principal parâmetro para segregar dados entre produtos simples e compostos. Por sua vez, o conteúdo de polifenóis totais nos chás foi mais relevante em sua capacidade antioxidante do que o conteúdo de flavonoides. Uma vez que os fabricantes não exibem a quantidade real de cada erva nos rótulos dos chás compostos, não foi possível confirmar se as misturas de várias espécies levam a um incremento substancial em sua capacidade antioxidante. Considerando o perfil redox e o teor de polifenóis totais, o consumo racional dos chás verde e preto e da erva-mate tradicional pode contribuir na prevenção de doenças associadas ao estresse oxidativo na população brasileira. Porém, estudos clínicos são necessários para validar essa hipótese.

Abstract In this work, it was evaluated the phenolic content, redox behavior and antioxidant capacity of several selected teas and tisanes from Brazilian market. The samples were classified as simple (single herb) or composed (blend of two or more herbs). In addition, complementary multivariate statistical approaches were used to identify the correlation and interdependence between the amount of major phytocomponents, such as phenols and flavonoids, as well as the antioxidant activity of the products. Results showed that the total polyphenol and total flavonoid concentrations are correlated to thermodynamic feasibility of reactive oxygen species reduction. The statistical modeling differentiated the results datasets in principal components, whose flavonoid content presented itself as the main parameter to segregate data between simple and composed products. On the other hand, the whole polyphenol content, in both teas and tisanes, was more relevant regarding their antioxidant capacity than the flavonoids content. Considering that the manufactures do not display the real amount of each herb in the labels of the composed products, it was not possible to confirm whether the blends of several species lead to a substantial enhancement on their antioxidant capacity. Furthermore, the redox profile and overall polyphenol content suggest that the consumption of green and black teas as well as traditional yerba mate may be worthwhile in preventing ailments associated with oxidative stress in Brazilian population. Notwithstanding, further clinical studies are required to validate this hypothesis.

This paper reports on the development of nanoparticles aiming at the in vitro controlled release of simvastatin (SVT). The nanoparticles were prepared by the nanoprecipitation method with polymers Eudragit® FS30D (EDGFS) or Eudragit® NE30D (EDGNE). EDGFS+SVT nanoparticles showed mean size of 148.8 nm and entrapment efficiency of 76.4%, whereas EDGNE+SVT nanoparticles showed mean size of 105.0 nm and entrapment efficiency of 103.2%. Infrared absorption spectra demonstrated that SVT incorporated into the polymer matrix, especially EDGNE. Similarly, the differential scanning calorimeter (DSC) curve presented no endothermic peak of fusion, indicating that the system is amorphous and the drug is not in the crystalline state. The maintenance of SVT in the amorphous state may favors its solubilization in the target release sites. In the in vitro dissolution assay, the SVT incorporated into the EDGFS+SVT nanoparticles showed a rapid initial release, which may be related to the pH of the dissolution medium used. Regarding the EDGNE+SVT nanoparticles, the in vitro release occurred in a bimodal behavior, i.e., an initial “burst” followed by a sustained delivery, with the kinetics of drug release following Baker-Lonsdale’s mathematical model. All these features suggest the nanoparticulate system’s potential to modulate SVT delivery and enhance its bioavailability.

Pterodon emarginatus Vogel, Fabaceae, is a tree species commonly known as "sucupira-branca". It is a popular medicinal plant in the Brazilian cerrado (Savanna). This study investigates the chemical variability of the essential oils from fruits of P. emarginatus. The fruits were collected from five sites in the Brazilian Cerrado and their essential oils were analyzed by GC/MS. The results obtained by Principal Component and Cluster Analysis identified two groups: cluster I containing β-caryophyllene and δ-elemene and cluster II containing α-copaene, β-cubebene, allo-aromadendrene, α-cubebene and γ-muurulene. The Canonical Discriminant Analysis was used to differentiate between clusters on the basis of essential oil composition. The results showed high variability in the composition of the essential oils from fruits of P. emarginatus, contributing to studies of domestication of this species.

Prior to obtain a standardized dried extract from V. ferruginea, lupeol was first time isolated from leaves and used as chemical maker. An analytical method using HPLC-PDA for lupeol determination in V. ferruginea intermediate products was developed using a C8 reverse-phase column, acetonitrile-acetic acid (99.99:0.01, v/v) as mobile phase at 0.8 mL min-1, oven temperature at 23-25 ºC, sample injection volume at 30 µL and detection at 210 nm. The method presented linearity from 10 to 160 µg mL-1, accuracy, precision, robustness and suitable sensitivity proving to be a useful tool to the obtainment process of lupeol standardized dried extracts of V. ferruginea.