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1.
Sci Rep ; 14(1): 6991, 2024 03 24.
Artigo em Inglês | MEDLINE | ID: mdl-38523180

RESUMO

Gout and hyperuricemia are characterized by high uric acid levels, and their treatment involves medications that have adverse effects. In this study, we evaluated oral liposomal formulations with eremantholide C and goyazensolide as a novel approach to reduce the toxicity associated with these substances while maintaining their anti-hyperuricemic activity. We characterized the formulations and evaluated them based on encapsulation efficiency and stability over 12 months and under simulated physiological environments. We determined the toxicity of the liposomal formulations in Caco-2 cells and the anti-hyperuricemic activity in rats. The formulations exhibited nanometric size, a narrow size distribution, and a negative zeta potential, indicating their stability and uniformity. The efficient encapsulation of the sesquiterpene lactones within the liposomes emphasizes their potential for sustained release and therapeutic efficacy. Stability evaluation revealed a small decrease in the eremantholide C concentration and a remarkable stability in the goyazensolide concentration. In Caco-2 cells, the liposomes did not exert toxicity, but did exhibit an antiproliferative effect. In vivo assays demonstrated that the liposomes reduced serum uric acid levels. Our study represents an advancement in gout and hyperuricemia treatment. The liposomal formulations effectively reduced the toxicity associated with the sesquiterpene lactones while maintaining their therapeutic effects.


Assuntos
Artrite Gotosa , Hidrocarbonetos Aromáticos com Pontes , Furanos , Gota , Hiperuricemia , Sesquiterpenos , Sesterterpenos , Humanos , Ratos , Animais , Lipossomos/uso terapêutico , Ácido Úrico/uso terapêutico , Hiperuricemia/tratamento farmacológico , Células CACO-2 , Gota/tratamento farmacológico , Lactonas/farmacologia , Lactonas/uso terapêutico
2.
Ann Ist Super Sanita ; 47(4): 429-44, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-22194079

RESUMO

Reproductive toxicity, with its many targets and mechanisms, is a complex area of toxicology; thus, the screening and identification of reproductive toxicants is a main scientific challenge for the safety assessment of chemicals, including the European Regulation on Chemicals (REACH). Regulatory agencies recommend the implementation of the 3Rs principle (refinement, reduction, replacement) as well as of intelligent testing strategies, through the development of in vitro methods and the use of mechanistic information in the hazard identification and characterization steps of the risk assessment process. The EU Integrated Project ReProTect (6th Framework Programme) implemented an array of in vitro tests to study different building blocks of the mammalian reproductive cycle: methodological developments and results on male and female germ cells, prostate and placenta are presented.


Assuntos
Alternativas aos Testes com Animais/tendências , Reprodução/efeitos dos fármacos , Toxicologia/tendências , Adulto , Animais , Bovinos , Avaliação Pré-Clínica de Medicamentos , União Europeia , Feminino , Fertilização/efeitos dos fármacos , Células Germinativas/efeitos dos fármacos , Humanos , Itália , Masculino , Testes de Mutagenicidade , Mutagênicos/toxicidade , Oócitos/efeitos dos fármacos , Placenta/efeitos dos fármacos , Gravidez , Próstata/efeitos dos fármacos , Projetos de Pesquisa , Espermatozoides/efeitos dos fármacos
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