Design and development of orally disintegrating films: A platform based on hydroxypropyl methylcellulose and guar gum.

From a design of experiments (DOE) performed under four independent variables, with the filmogenicity conditions and shortest disintegration time as the answers, a new oral disintegrating film (ODF) based on hydroxypropyl methylcellulose (HPMC) and guar gum (GG) with the essential oil of Plectranthus amboinicus L. (EOPA) was developed. Sixteen formulations were tested for filmogenicity, homogeneity, and viability. The better selected ODF required 230.1 s for complete disintegration. The retention rate of the EOPA was quantified using the nuclear magnetic resonance hydrogen technique (H1 NMR), which identified the presence of 0.14 % carvacrol. The scanning electron microscopy showed a smooth and homogeneous surface with the presence of small white dots. Through the disk diffusion test, the EOPA was able to inhibit the growth of clinical strains of the Candida genus and gram-positive and gram-negative bacterial strains. This work opens new perspectives for the development of antimicrobial ODFS used in clinical practice.

Jatropha mutabilis, a new source of vitexin: HPLC quantification and pharmacological evaluation.

Jatropha mutabilis (Pohl) Baill is an endemic species of the Caatinga biome, little studied in terms of chemical composition. The objective of this work was to develop an analytical methodology to quantify vitexin in the ethanolic extract of J. mutabilis and to evaluate the expectorant and antitussive activities in mice. The expectorant activity was performed by measuring the phenol red obtained from the bronchoalveolar fluid in animals and the antitussive activity was evaluated by the cough method induced by citric acid (0.4 M). The method developed by HPLC-DAD proved to be simple, linear, precise, accurate, robust and specific. Besides, both vitexin (0.2, 1 and 5 mg/kg) and the extract of J. mutabilis (20, 102, 510 mg/kg) showed efficacy in decrease cough and increase aqueous mucus in mice, but vitexin was more potent. Lastly, the identification of vitexin opens the possibility of new studies for J. mutabilis.

Toxicological, chemopreventive, and cytotoxic potentialities of rare vegetal species and supporting findings for the Brazilian Unified Health System (SUS).

Caatinga flora which are found in a poor Brazilian region contain a substantial number of endemic taxa with biomedical and social importance for regional communities. This study examined the antioxidant and cytotoxic potential of 35 samples (extracts/fractions) from 12 Caatinga species and determined the antiproliferative and genotoxic action of dichloromethane fraction from Mimosa caesalpiniifolia stem bark (DC-Mca) on human and vegetal cells. Samples were assessed for chemopreventive ability, toxic effects on Artemia salina shrimp as well as cytotoxicity on tumor cell lines and erythrocytes. DC-Mca was also tested with respect to antiproliferative and genotoxic effects upon normal leukocytes and meristematic cells from A. cepa roots. Some extracts reduced free radical levels >95% and 7 samples exhibited a lethal concentration (LC) 50 < 100 µg/ml upon Artemia salina larvae. Eight samples displayed in vitro antitumor effects and three produced hemolysis. Data also demonstrated the pharmacological significance of bioactive extracts from Brazilian semi-arid region. There was no significant relationship between antioxidant, toxic, and antiproliferative activities, and that these properties were dependent upon the extractant. DC-Mca contained betulinic acid as main compound (approximately 70%), which showed higher (1) cytotoxic activity on cancer cell lines and dividing leukocytes, (2) reduced mitotic index of Allium cepa roots, and (3) induced cell cycle arrest and chromosomal bridges, thereby providing native promising sources for phytotherapy development. ABBREVIATIONS: ABTS: 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid); AcOH: ethyl acetate; ANOVA: analysis of variance; SUS: Brazilian Unified Health System; DC-Mca: dichloromethane fraction from Mimosa caesalpiniifolia stem bark; DMSO: dimethylsulfoxide; DPPH: 1,1-diphenyl-2-picrylhydrazyl; EC50: effective concentration 50%; EtOAc: ethyl acetate; FDA: Food and Drug Administration; GC-Qms: gas chromatograph quadrupole mass spectrometer; GI: genotoxic index; HCT-116: colon carcinoma line; HL-60: promyelocytic leukemia line; HPLC: high-performance liquid chromatography; HRAPCIMS: high resolution atmospheric pressure chemical ionization mass spectrum; IC50: inhibitory concentration 50%; LC50: lethal concentration 50%; MeOH = methyl alcohol; MI: mitotic index; MTT: 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide; MutI: mutagenic index; OVCAR-8 = ovarian carcinoma line; PBMC: peripheral blood mononuclear cells; RPMI-1640: Roswell Park Memorial Institute medium; SF-295: glioblastoma line; TEAC: trolox equivalent antioxidant capacity; TLC: thin-layer chromatography; Trolox: 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid.

Antinociceptive activity of ethanol extract from Duguetia chrysocarpa Maas (Annonaceae).

The ethanol extract from the fruits of Duguetia chrysocarpa was evaluated for its antinociceptive activity in chemical and thermal models of nociception in mice. The intraperitoneal administration of the ethanol extract (100, 200, and 400 mg/kg body weight) showed a dose-dependent inhibition of acetic-acid-induced abdominal writhes. The extract also produced a significant inhibition of both phases of the formalin test in all doses tested and increased the reaction time in hot-plate test at dose of 200 mg/kg. The data obtained suggest that the antinociceptive effect of the extract may be mediated via both peripheral and central mechanisms. The phytochemical investigation yielded the isolation of the benzenoid derivative 3-methoxy-4-ethoxy benzoic acid which is being reported for the first time in this genus.