Solid Self Nano-Emulsifying Drug Delivery System of Dasatinib: Optimization, In-vitro, Ex-vivo and In-vivo assessment.

IF 3 Q2 PHARMACOLOGY & PHARMACY Therapeutic delivery Pub Date : 2024-01-01 Epub Date: 2024-09-17 DOI:10.1080/20415990.2024.2397330

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

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Abstract

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 AUC_0-t for the DST-S-SNEDDS group than free DST.Conclusion: S-SNEDDS could be promising approach for improving bioavailability and efficacy of DST.

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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。

目的：达沙替尼（DST）是一种口服酪氨酸激酶抑制剂，水溶性较差。为了解决这一问题，我们配制了一种 DST 固体自纳米乳化给药系统（S-SNEDDS）：方法：使用芳樟醇、Cremophor RH40 和 Transcutol P 对负载 DST 的 SNEDDS 进行了 I-optimal 混合物设计，并对 S-SNEDDS 进行了理化表征、体外释放和体内渗透、细胞检测和药代动力学研究：结果：DST-S-SNEDDS 的球形尺寸和 PDI 分别为 141.53 ± 5.371 nm 和 0.282 ± 0.020。在 MDA-MB-231 中，DST-S-SNEDDS 的 IC50（1.825 μg/mL）明显低于游离 DST（7.298 μg/mL）。体内药代动力学研究显示，DST-S-SNEDDS 组的 AUC0-t 比游离 DST 组增加了 1.94 倍：结论：S-SNEDDS 是提高 DST 生物利用度和疗效的有效方法。

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来源期刊

Therapeutic delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.50

自引率

0.00%

发文量

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.