Mohd Aman Mohd Ateeq, Srushti Mahajan, Brojendra Nath Saren, Mayur Aalhate, Hoshiyar Singh, Essha Chatterjee, Indrani Maji, Ujala Gupta, Anitha Sriram, Santosh Kumar Guru, Pankaj Kumar Singh
{"title":"达沙替尼固体自纳米乳化给药系统：优化、体外、体内和体外评估。","authors":"Mohd Aman Mohd Ateeq, Srushti Mahajan, Brojendra Nath Saren, Mayur Aalhate, Hoshiyar Singh, Essha Chatterjee, Indrani Maji, Ujala Gupta, Anitha Sriram, Santosh Kumar Guru, Pankaj Kumar Singh","doi":"10.1080/20415990.2024.2397330","DOIUrl":null,"url":null,"abstract":"<p><p><b>Aim:</b> Dasatinib (DST) is an oral tyrosine kinase inhibitor with poor aqueous solubility. To outwit this issue, a solid self-nano emulsifying drug delivery system (S-SNEDDS) of DST was formulated.<b>Methods:</b> I-optimal mixture design was used for optimization of DST-loaded SNEDDS using Linalool, Cremophor RH40 and Transcutol P. S-SNEDDS underwent physicochemical characterization, <i>in-vitro</i> release and <i>ex-vivo</i> permeation, cell-based assays and pharmacokinetic study.<b>Results:</b> DST-S-SNEDDS showed globule size and PDI of 141.53 ± 5.371 nm and 0.282 ± 0.020, respectively. DST-S-SNEDDS revealed significantly lower IC<sub>50</sub> (1.825 μg/mL) than free DST (7.298 μg/mL) in MDA-MB-231. <i>In-vivo</i> pharmacokinetic study revealed 1.94-fold increment in AUC<sub>0-t</sub> for the DST-S-SNEDDS group than free DST.<b>Conclusion:</b> S-SNEDDS could be promising approach for improving bioavailability and efficacy of DST.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"749-768"},"PeriodicalIF":3.0000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11457667/pdf/","citationCount":"0","resultStr":"{\"title\":\"Solid Self Nano-Emulsifying Drug Delivery System of Dasatinib: Optimization, <i>In-vitro</i>, <i>Ex-vivo</i> and <i>In-vivo</i> assessment.\",\"authors\":\"Mohd Aman Mohd Ateeq, Srushti Mahajan, Brojendra Nath Saren, Mayur Aalhate, Hoshiyar Singh, Essha Chatterjee, Indrani Maji, Ujala Gupta, Anitha Sriram, Santosh Kumar Guru, Pankaj Kumar Singh\",\"doi\":\"10.1080/20415990.2024.2397330\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p><b>Aim:</b> Dasatinib (DST) is an oral tyrosine kinase inhibitor with poor aqueous solubility. To outwit this issue, a solid self-nano emulsifying drug delivery system (S-SNEDDS) of DST was formulated.<b>Methods:</b> I-optimal mixture design was used for optimization of DST-loaded SNEDDS using Linalool, Cremophor RH40 and Transcutol P. S-SNEDDS underwent physicochemical characterization, <i>in-vitro</i> release and <i>ex-vivo</i> permeation, cell-based assays and pharmacokinetic study.<b>Results:</b> DST-S-SNEDDS showed globule size and PDI of 141.53 ± 5.371 nm and 0.282 ± 0.020, respectively. DST-S-SNEDDS revealed significantly lower IC<sub>50</sub> (1.825 μg/mL) than free DST (7.298 μg/mL) in MDA-MB-231. <i>In-vivo</i> pharmacokinetic study revealed 1.94-fold increment in AUC<sub>0-t</sub> for the DST-S-SNEDDS group than free DST.<b>Conclusion:</b> S-SNEDDS could be promising approach for improving bioavailability and efficacy of DST.</p>\",\"PeriodicalId\":22959,\"journal\":{\"name\":\"Therapeutic delivery\",\"volume\":\" \",\"pages\":\"749-768\"},\"PeriodicalIF\":3.0000,\"publicationDate\":\"2024-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11457667/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Therapeutic delivery\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1080/20415990.2024.2397330\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/9/17 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Therapeutic delivery","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1080/20415990.2024.2397330","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/9/17 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Solid Self Nano-Emulsifying Drug Delivery System of Dasatinib: Optimization, In-vitro, Ex-vivo and In-vivo assessment.
Aim: Dasatinib (DST) is an oral tyrosine kinase inhibitor with poor aqueous solubility. To outwit this issue, a solid self-nano emulsifying drug delivery system (S-SNEDDS) of DST was formulated.Methods: I-optimal mixture design was used for optimization of DST-loaded SNEDDS using Linalool, Cremophor RH40 and Transcutol P. S-SNEDDS underwent physicochemical characterization, in-vitro release and ex-vivo permeation, cell-based assays and pharmacokinetic study.Results: DST-S-SNEDDS showed globule size and PDI of 141.53 ± 5.371 nm and 0.282 ± 0.020, respectively. DST-S-SNEDDS revealed significantly lower IC50 (1.825 μg/mL) than free DST (7.298 μg/mL) in MDA-MB-231. In-vivo pharmacokinetic study revealed 1.94-fold increment in AUC0-t for the DST-S-SNEDDS group than free DST.Conclusion: S-SNEDDS could be promising approach for improving bioavailability and efficacy of DST.
期刊介绍：
Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.
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