The study aimed to include the isolated vitexin of Jatropha mutabilis in the β-cyclodextrin cavity to improve the solubility of this flavone. Its characterization was performed by techniques such as 1H NMR/ROESY (Nuclear Magnetic Resonance Spectroscopy), FT-IR (Infrared Spectroscopy with Fourier Transform), SEM (Morphological analysis of IC by Scanning Electron Microscopy) and dissolution study in vitro. In addition, the following activities were evaluated in the animal models: expectorant, phenol red dosage in bronchoalveolar lavage and antitussive, cough induced by citric acid. In the characterization of the complex, interaction between hydrogens of ring B of vitexin and (H3) of β-CD was observed, in addition to changes in morphology. In the dissolution test, an increase in the rate of dissolution of vitexin was observed in the first 30 min for the CI vitexin/β-CD when compared with vitexin. Regarding the pharmacological activity, it was observed that the inclusion complex (IC) vitexin/β-CD in the equivalent doses of 0.2, 1 and 5 mg/kg of flavone presented higher expectorant activity when compared to vitexin (p < 0.05), suggesting increased bioavailability. As for the antitussive activity, both vitexin and the complex had similar effects and were dose independent. In the toxicity test using Artemia salina, vitexin and IC vitexin/β-CD were considered non-toxic. At last, the study efficacy of vitexin/β-CD IC as an expectorant and of vitexin as antitussive. All of these data are being described for the first time.
Hyptis pectinata is a herb popularly used in Brazil for the treatment of inflammations, pain, bacterial infections and cancer. In the present study, inflorescences (MPIn), leaves (MPL), branches (MPB), root (MPR) extracts and three compounds isolated from MPIn were assayed against breast tumor cell lines. The structures of the three compounds (pectinolide J, hyptolide and pectinolide E) were determined by means of spectroscopic analysis. Pectinolide J was isolated for the first time. The MPIn, MPL and MPR exhibited specific antiproliferative activity on tumor cell lines when compared to normal cell lines with IC50 of 52.01 ± 0.64, 45.91 ± 0.02 μg/mL and 82.84 ± 0.03 μg/mL, respectively. Although the isolated substances did not present good antiproliferative activity, when the three were associated, a greater biological effect was observed, suggesting a synergistic effect. Hyptolide (5.6 ± 0.4 μg/mL) showed IC50 sufficiently low to be considered as a drug prototype.
1 February 2021 in Journal of Drug Delivery Science and Technology
Metal–organic frameworks (MOFs) are promising materials for drug delivery due to their structural tunability and high surface area. This work reports on the synthesis of ZIF-8 for the in situ encapsulation of hesperidin, a flavonoid with poor water solubility used in the treatment of circulatory system disorders, as a gastric-targeted drug delivery system (DDS). A 23 full factorial design was used to optimize drug loading, investigating the effects of DMSO concentration, 2-MIm/Zn2+ molar ratio, and final solution volume (water content). The materials were characterized by ATR-FT-IR, TG, XRD, and SEM analyses, confirming successful ZIF-8 synthesis and partial hesperidin encapsulation. Drug release kinetics were evaluated at pH 1.0 and 6.86. The system showed a faster and more pronounced release at pH 1.0, driven by MOF degradation, demonstrating its potential as a gastric-targeted DDS. This study confirms the feasibility of ZIF-8 to improve hesperidin solubility and bioavailability, highlighting a novel strategy for its therapeutic application.