Yngrid Batista da Silva, Giselle Bedogni, Guaraciara de Andrade Picanço, Jéssica Yonara de Souza, Waylla Silva Nunes, Tatiane Luiza da Costa, Geovana Batista de Campos, Lina Vargas Michelena, Claudio Javier Salomon, Marina Clare Vinaud
{"title":"纳米配方芬苯达唑作为治疗神经囊虫病的一种有吸引力的方法:体外和体内研究。","authors":"Yngrid Batista da Silva, Giselle Bedogni, Guaraciara de Andrade Picanço, Jéssica Yonara de Souza, Waylla Silva Nunes, Tatiane Luiza da Costa, Geovana Batista de Campos, Lina Vargas Michelena, Claudio Javier Salomon, Marina Clare Vinaud","doi":"10.1080/10837450.2024.2422936","DOIUrl":null,"url":null,"abstract":"<p><strong>Purpose: </strong>This work aimed to develop fenbendazole nanocrystals to evaluate their effects on the energetic metabolism of <i>Taenia crassiceps</i> cysticerci, following an intracranial inoculation in mice.</p><p><strong>Methods: </strong>Fenbendazole was nanoformulated by the antisolvent method using poloxamers 188 and 407 as stabilizers. The nanosuspensions were lyophilized without cryoprotectants and the nanocrystals were characterized in terms of particle size, zeta potential, and dissolution performance. The <i>in vivo</i> study was performed in infected animals treated with nanoformulated fenbendazole and raw drug and their metabolic impact was quantified by analyzing specific metabolites.</p><p><strong>Results: </strong>Fenbendazole samples were obtained by nanoprecipitation in > 80% yield. The average particle size of the freeze-dried samples was between 372 nm and 1600 nm. The nanosystems released a greater amount of the drug into the solution, compared to the raw drug. The <i>in vivo</i> studies showed that the fenbendazole-treated groups induced gluconeogenesis, partial blockage of the TCA cycle, and increased protein catabolism. As seen, the nanoformulation presented a greater effect on these parameters than the raw drug leading to remarkable modifications in the metabolism of the parasite, which in turn can influence the overall course of the infection and treatment outcomes.</p><p><strong>Conclusion: </strong>These findings suggest that nanoformulated fenbendazole may be considered a valuable approach for an effective treatment of neurocysticercosis.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1093-1100"},"PeriodicalIF":2.6000,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Nanoformulated fenbendazole as an attractive approach for treating neurocysticercosis: <i>in vitro</i> and <i>in vivo</i> studies.\",\"authors\":\"Yngrid Batista da Silva, Giselle Bedogni, Guaraciara de Andrade Picanço, Jéssica Yonara de Souza, Waylla Silva Nunes, Tatiane Luiza da Costa, Geovana Batista de Campos, Lina Vargas Michelena, Claudio Javier Salomon, Marina Clare Vinaud\",\"doi\":\"10.1080/10837450.2024.2422936\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Purpose: </strong>This work aimed to develop fenbendazole nanocrystals to evaluate their effects on the energetic metabolism of <i>Taenia crassiceps</i> cysticerci, following an intracranial inoculation in mice.</p><p><strong>Methods: </strong>Fenbendazole was nanoformulated by the antisolvent method using poloxamers 188 and 407 as stabilizers. The nanosuspensions were lyophilized without cryoprotectants and the nanocrystals were characterized in terms of particle size, zeta potential, and dissolution performance. The <i>in vivo</i> study was performed in infected animals treated with nanoformulated fenbendazole and raw drug and their metabolic impact was quantified by analyzing specific metabolites.</p><p><strong>Results: </strong>Fenbendazole samples were obtained by nanoprecipitation in > 80% yield. The average particle size of the freeze-dried samples was between 372 nm and 1600 nm. The nanosystems released a greater amount of the drug into the solution, compared to the raw drug. The <i>in vivo</i> studies showed that the fenbendazole-treated groups induced gluconeogenesis, partial blockage of the TCA cycle, and increased protein catabolism. As seen, the nanoformulation presented a greater effect on these parameters than the raw drug leading to remarkable modifications in the metabolism of the parasite, which in turn can influence the overall course of the infection and treatment outcomes.</p><p><strong>Conclusion: </strong>These findings suggest that nanoformulated fenbendazole may be considered a valuable approach for an effective treatment of neurocysticercosis.</p>\",\"PeriodicalId\":20004,\"journal\":{\"name\":\"Pharmaceutical Development and Technology\",\"volume\":\" \",\"pages\":\"1093-1100\"},\"PeriodicalIF\":2.6000,\"publicationDate\":\"2024-12-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceutical Development and Technology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/10837450.2024.2422936\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/11/9 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutical Development and Technology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/10837450.2024.2422936","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/11/9 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Nanoformulated fenbendazole as an attractive approach for treating neurocysticercosis: in vitro and in vivo studies.
Purpose: This work aimed to develop fenbendazole nanocrystals to evaluate their effects on the energetic metabolism of Taenia crassiceps cysticerci, following an intracranial inoculation in mice.
Methods: Fenbendazole was nanoformulated by the antisolvent method using poloxamers 188 and 407 as stabilizers. The nanosuspensions were lyophilized without cryoprotectants and the nanocrystals were characterized in terms of particle size, zeta potential, and dissolution performance. The in vivo study was performed in infected animals treated with nanoformulated fenbendazole and raw drug and their metabolic impact was quantified by analyzing specific metabolites.
Results: Fenbendazole samples were obtained by nanoprecipitation in > 80% yield. The average particle size of the freeze-dried samples was between 372 nm and 1600 nm. The nanosystems released a greater amount of the drug into the solution, compared to the raw drug. The in vivo studies showed that the fenbendazole-treated groups induced gluconeogenesis, partial blockage of the TCA cycle, and increased protein catabolism. As seen, the nanoformulation presented a greater effect on these parameters than the raw drug leading to remarkable modifications in the metabolism of the parasite, which in turn can influence the overall course of the infection and treatment outcomes.
Conclusion: These findings suggest that nanoformulated fenbendazole may be considered a valuable approach for an effective treatment of neurocysticercosis.
期刊介绍:
Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology.
Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as:
-Preformulation and pharmaceutical formulation studies
-Pharmaceutical materials selection and characterization
-Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation
-QbD in the form a risk assessment and DoE driven approaches
-Design of dosage forms and drug delivery systems
-Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies
-Drug delivery systems research and quality improvement
-Pharmaceutical regulatory affairs
This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.