Browsing by Author "Ineu, Rafael Porto"
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- Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activityPublication . Leimann, Fernanda Vitória; Souza, Luma Borges de; Oliveira, Byanca Pereira Moreira de; Rossi, Bruna Franzon; Silva, Patricia Sabino da; Shiraishi, Carlos Seiti Hurtado; Kaplum, Vanessa; Abreu, Rui M.V.; Pereira, Carla; Barros, Lillian; Peron, Ana Paula; Ineu, Rafael Porto; Oechsler, Bruno Francisco; Sayer, Claudia; Araujo, Pedro Henrique Hermes de; Gonçalves, Odinei Hess; Shiraishi, Carlos S.H.Researchers have concentrated efforts in the search for natural-based reversible inhibitors for cholinesterase enzymes as they may play a key role in the treatment of degenerative diseases. Diverse plant alkaloids can inhibit the action of acetylcholinesterase and, among them, berberine is a promising bioactive. However, berberine has poor water solubility and low bioavailability, which makes it difficult to use in treatment. The solid dispersion technique can improve the water affinity of hydrophobic substances, but berberine solid dispersions have not been extensively studied. Safety testing is also essential to ensure that the berberine-loaded solid dispersions are safe for use. This study investigated the effectiveness of berberine-loaded solid dispersions (SD) as inhibitors of acetylcholinesterase enzyme (AChE). Docking simulation was used to investigate the influence of berberine on AChE, and in vitro assays were conducted to confirm the enzymatic kinetics of AChE in the presence of berberine. Berberine SD also showed improved cytotoxic effects on tumoral cells when dispersed in aqueous media. In vivo assays using Allium cepa were implemented, and no cytotoxicity/genotoxicity was found for the berberine solid dispersion. These results suggest that berberine SD could be a significant step towards safe nanostructures for use in the treatment of neurodegenerative diseases.
- Progesterone-loaded solid lipid nanoparticles for use in the regulation of the estrous cycle in female ratsPublication . Fogolari, Odinei; Leimann, Fernanda Vitória; Ineu, Rafael Porto; Rudy, Marcia; Ludwig, André Franco; Salles, Fernando Marques; Amorim, João Paulo de Arruda; Franci, Celso Rodrigues; Sagae, Sara Cristina; Sayer, Claudia; Araújo, Pedro Henrique Hermes de; Gonçalves, Odinei HessProtocols used for artificial insemination involve the effective synchronization of the estrous cycle by the administration of exogenous hormones including progesterone analogs. Although widespread in the world, the current techniques present many disadvantages that need to be overcome such as the time dependency of progesterone levels in the blood and the need to remove the release dispositive. Nanotechnology may offer the tools for it, and solid lipid nanoparticles (SLN) are a promising candidate to be used as nanocarriers for progesterone. In this work, progesterone-loaded SLNs were investigated in the regulation of the estrous cycle in female rats. First, the obtention of the SLN was investigated to determine how experimental parameters may affect the encapsulation efficiency of progesterone and the morphology of the nanoparticles. Also, in vitro release profiles of progesterone were also evaluated. Sexual receptivity, mutagenicity, hepatic inflammation and steatosis, hormone measurement, and biometric parameters of pups were also determined. Progesterone-loaded SLN induced estrous cycle synchronization and were able to maintain the estrous phase of the estrous cycle while inducing a greater latency release for its onset. Progesterone induced an increase in the sexual receptivity of the females and did not alter the biometric parameters like the body weight of the mothers and puppies, until weaning. Results gathered here demonstrated that encapsulation of progesterone may be a promising alternative to the conventional methods for synchronization of the estrous cycle of female animals in artificial insemination procedures.