Evaluation of Budesonide–Hydroxypropyl-β-Cyclodextrin Inclusion Complex in Thermoreversible Gels for Ulcerative Colitis

Lázaro, Carolina Martins; Oliveira, Carolina Camargo de; Gambero, Alessandra; Rocha, Thalita; Cereda, Cíntia Maria Saia; Araújo, Daniele Ribeiro de; Tófoli, Giovana Radomille

doi:10.1007/s10620-020-06075-y

Cited by 15 publications

(7 citation statements)

References 19 publications

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“…The improvement in permeability is also an important effect that allows a major distribution of active ingredients [ 32 ]. The ASE-CD effect observed here is in accordance with other studies in various models of inflammation, also at intestinal level [ 33 , 34 , 35 ].…”

Section: Resultssupporting

confidence: 93%

Recycling of Almond By-Products for Intestinal Inflammation: Improvement of Physical-Chemical, Technological and Biological Characteristics of a Dried Almond Skins Extract

et al. 2020

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Background: Almond skins are rich in bioactive compounds that undergo oxidation/degradation phenomena and are poorly soluble in water, reducing in vivo absorption and bioavailability, factors that influence the pharmacological activity of an active product. We developed a dried acetonic almond skins extract/cyclodextrin complex to improve extract solubility, dissolution rate and biological activity. Methods: A lyophilized acetonic almond skin extract was produced. To optimize complex formulation, phase solubility studies and complex characterization (absorption studies, differential scanning calorimetry (DSC), morphology, solubility studies) were performed. To evaluate a possible use in healthy products, tumor necrosis factor-α levels and reactive oxygen species release, as well as cicloxygenase-2 and inducible nitric oxide synthase expression in intestinal epithelial cells, were also evaluated. Results: Phase solubility studies showed a Bs-type profile. A 1:1 dried acetonic almond skins extract/cyclodextrin ratio was able to improve extract water solubility and dissolution rate (100% in 45 min). The UV-Vis spectra of complex revealed a hypsochromic and hyperchromic effect, probably due to a partial inclusion of extract in cyclodextrin cavity through weak bonds, confirmed by DSC and morphology studies. The technological improvement in the extract characteristics also led to better biological activity. In fact, the complex effectively reduces tumor necrosis factor-α levels with respect to the pure extract and significantly inhibits the reactive oxygen species release, even if only at the lower concentration of 5 μg/mL. Conclusion: The complex was able to overcome solubility problems and could be used in inflammatory disease.

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Section: Resultssupporting

confidence: 93%

Recycling of Almond By-Products for Intestinal Inflammation: Improvement of Physical-Chemical, Technological and Biological Characteristics of a Dried Almond Skins Extract

et al. 2020

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“…Fortunately, after that, compelling research has been done. For example, the study of HPβCD/budesonide ICs in the form of thermoreversible gels for ulcerative colitis [ 147 ]; or HPβCD/5-fluorouracil IC encapsulated in a thermoreversible gelling film for colorectal cancer [ 148 ]. Despite its low popularity, this administration route may still be hiding its potential to deliver drugs locally or systemically, and the use of mucoadhesive and thermoresponsive materials whose development could be supported by CDs may provide interesting progress to the field.…”

Section: Resultsmentioning

confidence: 99%

Technological evolution of cyclodextrins in the pharmaceutical field

Rincón-López

Almanza-Arjona

Riascos

et al. 2021

Journal of Drug Delivery Science and Technology

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We herein disclose how global cyclodextrin-based pharmaceutical technologies have evolved since the early 80s through a 1998 patents dataset retrieved from Derwent Innovation Index. We used text-mining techniques based on the patents semantic content to extract the knowledge contained therein, to analyze technologies related to the principal attributes of CDs: solubility, stability, and taste-masking enhancement. The majority of CDs pharmaceutical technologies are directed toward parenteral aqueous solutions. The development of oral and ocular formulations is rapidly growing, while technologies for nasal and pulmonary routes are emerging and seem to be promising. Formulations for topical, transdermal, vaginal, and rectal routes do not account for a high number of patents, but they may be hiding a great potential, representing opportunity research areas. Certainly, the progress in materials sciences, supramolecular chemistry, and nanotechnology, will influence the trend of that, apparently neglected, research. The bottom line, CDs pharmaceutical technologies are still increasing, and this trend is expected to continue in the coming years. Patent monitoring allows the identification of relevant technologies and trends to prioritize research, development, and investment in both, academia and industry. We expect the scope of this approach to be applied in the pharmaceutical field beyond CDs technological applications.

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“…LASSBio-1524 and Its Analogs Reduce Macroscopic and Microscopic Damage and Phosphorylated p38 MAPK in Colon of Mice. Studies have shown that tissue damage in the colon during experimental colitis is associated with increased inflammatory cells and mediators (Lazaro et al, 2020). To further verify and relate the reduction of mediator production with tissue improvement, histologic sections and subsequent analysis of colon damage were performed.…”

Section: Resultsmentioning

confidence: 99%

Therapeutic Effects of Anti-Inflammatory N-Acylhydrazones in the Resolution of Experimental Colitis

Cordeiro

Freitas

Fraga

et al. 2020

J Pharmacol Exp Ther

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Inflammatory bowel diseases are caused by inflammation of the gastrointestinal tract, which may or may not have a specific cause or pathogen. They affect millions of people around the world and there are still few effective treatments. The aim of this work is to investigate the anti-inflammatory effect of the IKK-b inhibitor LASSBio-1524 and its three analogs, LASSBio-1760, LASSBio-1763, and LASSBio-1764, on mediator production and expression of inflammatory enzymes using experimental animal models of intestinal inflammatory diseases. Colitis was performed using two different models, which mimic Crohn disease (induced by dinitrobenzene acid) and ulcerative colitis (induced by sodium dextran sulfate) in mice. In both models, a therapeutic protocol with a daily dose of 1, 3, or 30 mmol/kg was performed. LASSBio-1524 and its three analogs reduced the secretion of tumor necrosis factor-a, IL-1b, IL-6, IL-12, and IFN-g and increased secretion of IL-10, protecting gastrointestinal homeostasis. All compounds reduced macro-and microscopic colonic damage caused by experimental colitis and p38 mitogenactivated protein kinase expression in the colon, as well as leukocytosis and anemia resulting from the disease. Our data may suggest LASSBio-1524 and its analogs (LASSBio-1760, LASSBio-1763, and LASSBio-1764 as promising candidates for new prototypes designed to treat inflammatory bowel diseases. SIGNIFICANCE STATEMENTThree new N-acylhydrazones were synthetized as analogs of LASSBio-1524. All new substances were evaluated in dextran sulfate-and dinitrobenzene acid-induced colitis, with LASSBio-1760, LASSBio-1762, and LASSBio-1763 presenting a significant effect in both models of colitis without toxic effects. The new substances could be considered as a new prototype for the development of new anti-inflammatory treatments of colitis.

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Evaluation of Budesonide–Hydroxypropyl-β-Cyclodextrin Inclusion Complex in Thermoreversible Gels for Ulcerative Colitis

Cited by 15 publications

References 19 publications

Recycling of Almond By-Products for Intestinal Inflammation: Improvement of Physical-Chemical, Technological and Biological Characteristics of a Dried Almond Skins Extract

Recycling of Almond By-Products for Intestinal Inflammation: Improvement of Physical-Chemical, Technological and Biological Characteristics of a Dried Almond Skins Extract

Technological evolution of cyclodextrins in the pharmaceutical field

Therapeutic Effects of Anti-Inflammatory N-Acylhydrazones in the Resolution of Experimental Colitis

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