Solid Self Nano-Emulsifying Drug Delivery System of Dasatinib: Optimization, <i>In-vitro</i> , <i>Ex-vivo</i> and <i>In-vivo</i> assessment

<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.

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Publication Details

Journal
Therapeutic Delivery
Published
2024-09-17
DOI
https://doi.org/10.1080/20415990.2024.2397330
Citations
7
Primary Topic
Drug Solubulity and Delivery Systems
Type
article
Field-Weighted Citation Impact
1.46
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article

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

Pankaj Kumar Singh, Anitha Sriram, Mohd Aman Mohd Ateeq, Ujala Gupta et al.
7 citations
Therapeutic Delivery
Drug Solubulity and Delivery Systems
1.46
article

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

Pankaj Kumar Singh, Anitha Sriram, Mohd Aman Mohd Ateeq, Ujala Gupta, Santosh Kumar Guru, Essha Chatterjee, Brojendra Nath Saren, Indrani Maji, Mayur Aalhate, Srushti Mahajan, Hoshiyar Singh
article en
7 citations

Abstract

<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.

Therapeutic DeliveryVol. 15(10)
National Institute of Pharmaceutical Education and Research - Ahmedabad (IN)
Good health and well-being
Openalex Percentile: Top 20%
Drug Solubulity and Delivery Systems
1.46
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Solid Self Nano-Emulsifying Drug Delivery System of Dasatinib: Optimization, <i>In-vitro</i> , <i>Ex-vivo</i> and <i>In-vivo</i> assessment — Pankaj Kumar Singh, Anitha Sriram, et al. · Therapeutic Delivery (2024) | TGRS Research Map | TGRS