Desenvolvimento de nanogel de Copaifera reticulata sobre a lesão muscular em ratos usando fonoforese / Development of nanogel from Copaifera reticulata on muscle lesions in rates with phonophoresis

A copaíba (Copaifera reticulata Ducke), planta medicinal bastante usada nas regiões Norte e Nordeste do Brasil, tem difícil permeação cutânea na forma in natura, e esta permeabilidade é aumentada através do uso de nanoformulações e ainda a fonoforese, ultrassom de baixa frequência que aumenta a permeabilidade cutânea de substâncias. Sendo assim, foi analisado e comparado o efeito do óleo-resina de copaíba, in natura e de sua nanoemulsão em gel (nanogel) associado à fonoforese, na reparação muscular em ratos Wistar. Pelo método inversão de fases, formulou-se a nanoemulsão de copaíba. Esta foi incorporada ao hidrogel Carbopol® (20% nanoemulsão, 80% Carbopol®). Os animais (n = 24, machos) foram divididos em seis grupos e posteriormente foram submetidos à lesão traumática do músculo gastrocnêmio. A reparação muscular foi analisada por meio de dosagem plasmática de Aspartato Aminotransferase (AST) e Creatina Quinase (CK). Os resultados apontaram que os tratamentos de aplicação tópica do óleo-resina, de sua associação à fonoforese e desta ao nanogel foram eficazes no experimento quanto à reparação da musculatura esquelética.

Copaifera reticulata Ducke is a medicinal plants greatly employed in northern and northeastern Brazil. However, skin penetration is difficult when it is applied in natura. However, permeability increases through nanoformulations and phonophoresis and low frequency ultrasound that increases skin permeability of compounds. The effect of oil-resin of copaiba, in natura and in gel (nano-emulsion), associated to phonophoresis, was analyzed and compared for muscle repair in Wistar rats. Copaiba nano-emulsion was formulated by phase inversion. It was incorporated to hydrogel Carbopol® (20% nano-emulsion, 80% Carbopol®). Male animals (n=24) were divided into six groups and later underwent traumatic lesion of the gastrocnemius muscle. Muscle repair was analyzed by plasmatic dosage of aspartate aminotransferase (AST) and kinase creatine (CK). Results show that topic treatments with oil-resin, associated with phonophoresis and nanogel were efficient in the assay for the repair of skeleton muscles.

Development and Evaluation of Antimicrobial and Modulatory Activity of Inclusion Complex of Euterpe oleracea Mart Oil and ß-Cyclodextrin or HP-ß-Cyclodextrin.

The development of inclusion complexes is used to encapsulate nonpolar compounds and improve their physicochemical characteristics. This study aims to develop complexes made up of Euterpe oleracea Mart oil (EOO) and ß-cyclodextrin (ß-CD) or hydroxypropyl-ß-cyclodextrin (HP-ß-CD) by either kneading (KND) or slurry (SL). Complexes were analyzed by molecular modeling, Fourier-transform infrared spectroscopy, scanning electron microscopy, powder X-ray diffraction, thermogravimetry analysis and differential scanning calorimetry. The antibacterial activity was expressed as Minimum Inhibitory Concentration (MIC), and the antibiotic resistance modulatory activity as subinhibitory concentration (MIC/8) against Escherichia coli, Streptomyces aureus, Pseudomonas aeruginosa and Enterococcus faecalis. Inclusion complexes with ß-CD and HP-ß-CD were confirmed, and efficiency was proven by an interaction energy between oleic acid and ß-CD of -41.28 ± 0.57 kJ/mol. MIC values revealed higher antibacterial activity of complexes compared to the isolated oil. The modulatory response of EOO and EOO-ß-CD prepared by KND as well as of EOO-ß-CD and EOO-HP-ß-CD prepared by SL showed a synergistic effect with ampicillin against E. coli, whereas it was not significant with the other drugs tested, maintaining the biological response of antibiotics. The antimicrobial response exhibited by the complexes is of great significance because it subsidizes studies for the development of new pharmaceutical forms.

Adsorption of Vi Capsular Antigen of Salmonella Typhi in Chitosan-Poly (Methacrylic Acid) Nanoparticles.

The development of a nanoparticulate system for the carrier antigen is now an important tool in the vaccination process, since a smaller number of doses is necessary for effective immunization. Thus, in this work a nanoparticulate system using polymers of chitosan and poly (methacrylic acid) (CS-PMAA) to adsorb the Vi antigen of Salmonella Typhi was developed. CS-PMAA nanoparticles with different proportions of chitosan and poly (methacrylic acid) were obtained and reached sizes from 123.9 ± 2.48 to 234.9 ± 2.66 nm, and spherical shapes were seen in transmission microscopy. At pH 7.2, the nanoparticles had a cationic surface charge that contributed to the adsorption of the Vi antigen. Qualitative analyses of the isolated Vi antigen were performed using Fourier-transform infrared spectroscopy, which indicated the presence of all the characteristic bands of the capsular polysaccharide, and nuclear magnetic resonance, which showed signals for the five hydrogens and the N-acetyl and O-acetyl groups which are characteristic of the Vi antigen structure. In the adsorption kinetics study, the Vi capsular antigen, contained in a phosphate buffer solution of pH 7.2, experienced 55% adsorption on the 1-1% (CS-PMAA) nanoparticles. The adsorption kinetics results showed the ability of the nanoparticulate system to adsorb the Vi antigen.

Biosynthesis, characterization and leishmanicidal activity of a biocomposite containing AgNPs-PVP-glucantime.

AIM: Development of functionalized nanocomposites containing AgNPs-PVP-Glucantime® to evaluate their leishmanicidal activity as a novel method for improving the pharmacological properties of the drug Glucantime® against extracellular promastigotes and intracellular amastigotes of Leishmania amazonensis in vitro to treat cutaneous leishmaniasis. MATERIALS & METHODS: The silver nanoparticles and nanocomposites prepared containing silver nanoparticles, polyvinylpyrrolidone and different amounts of Glucantime were characterized using transmission electron microscopy, x-ray diffraction, energy-dispersive x-ray spectroscopy and ζ potential analysis; in addition, the in vitro cytotoxicity was evaluated. RESULTS: The nanocomposites showed an inhibitory effect on the cellular viability of promastigote forms, with values of 47.06, 51.71 and 65.67% for nanocomposite1, nanocomposite2 and nanocomposite3, respectively, as well as a dose-dependent decrease in the infectivity index, with values of 33.33 and 23% for nanocomposite2 and nanocomposite3, respectively. CONCLUSION: The proposed nanocomposite reveals leishmanial activity and the absence of cytotoxicity in macrophages. Further investigations will be conducted in vivo.

The effects of extraction method on recovery rutin from Calendula officinalis L. (Asteraceae).

BACKGROUND: Calendula officinalis L. (Asteraceae) is a Mediterranean specie, but in Europe and America it is cultivated for ornamental or medicinal purposes. This species is widely used for presenting activities, antiinflammatory antibacterial and antioxidant. However the therapeutic action is linked to the amount of assets of the extracted raw material. The extraction method of bioactive compounds is an important step in the manufacturing of herbal medicines, because secondary metabolites with therapeutic potential are usually found in small quantities in plant materials. OBJECTIVE: Due the medical and commercial importance of C. officinalis, this study aimed to evaluate the impact of the extraction method on the quality of herbal extract and optimize the extraction of rutin from C. officinalis. MATERIALS AND METHODS: The extraction of rutin was performed by ultrasound and shaker and the optimized conditions were determined by response surface methodology. RESULTS: The results of ultrasound extraction assisted (UEA) and maceration dynamic (MD) showed that rutin yield ranged from 0.218 to 2.28% (w/w) when extract by ultrasound and 0.1-1.44% by MD. The optimal extraction condition for rutin (2.48% to UEA or 1.46% to MD) from C. officinalis by UEA or MD were a 19-22 min extraction, ethanol: water ratio of 35-40% and 0.05-0.056 mg/mL to raw material: solvent ratio. CONCLUSION: The UEA is more efficient to extraction rutin.