Author(s):
Moinuddin, Pavan Kumar
Email(s):
pawan.kumar@muit.in
DOI:
10.52711/0974-360X.2026.00192 
Address:
Moinuddin1, Pavan Kumar2
1Maharishi School of Pharmaceutical Sciences, Maharishi University of Information Technology, MUIT, Lucknow – 226013, Uttar Pradesh, India.
2Maharishi School of Pharmaceutical Sciences, Maharishi University of Information Technology, MUIT, Lucknow - 226013, Uttar Pradesh, India.
*Corresponding Author
Published In:
Volume - 19,
Issue - 3,
Year - 2026
ABSTRACT:
Due to its oral administration and antiproliferative properties against chronic myeloid leukaemia (CML), dasatinib has been identified as a second-generation tyrosine kinase inhibitor (TKI). Central-composite designs (CCD) was followed to optimise dasatinib and hesperidin loaded solid lipid nanoparticles (SLNs), which were made in-house using a high-shear homogenisation approach. After leukaemia cells were injected intravenously into a mouse model, the produced SLNs' oral administring in vivo anti-leukemic activity and bioavailability (PK) were evaluated. In the leukemic mice, dasatinib was given as an SLN formulation in addition to a pure drug suspension. liquid chromatography (HPLC) system was used to analyse and compare the pharmacokinetic parameters to those of the drug suspension. For the pure drug and SLN formulations, the mean half-lives were calculated to be 4.62hours and 8.76hours, respectively; the mean maximum plasma concentrations (Cmax) were found to be 184.12µg/L and 390.53µg/L; and the mean Tmax values were recorded at 2 and 4hours. The suspension's mean area under the curve (AUClast) was 1080.95 hr•ng/mL, while the SLN formulation's was 3669.50hr•ng/mL. The group treated with the SLN formulation showed a statistically drastinc increase in survival. When compared to the free medication, the SLN showed increased cytotoxic efficacy. Thus, it was discovered that dasatinib's double drug-targeted SLN formulation improved cellular sensitivity to the encapsulated medication more successfully than the non-encapsulated formulation.
Cite this article:
Moinuddin, Pavan Kumar. Assessment of Oral Bioavailability and In-vivo Anti-leukemic Efficacy of Dasatinib-Loaded Solid Lipid Nanoparticles. Research Journal Pharmacy and Technology. 2026;19(3):1341-5. doi: 10.52711/0974-360X.2026.00192
Cite(Electronic):
Moinuddin, Pavan Kumar. Assessment of Oral Bioavailability and In-vivo Anti-leukemic Efficacy of Dasatinib-Loaded Solid Lipid Nanoparticles. Research Journal Pharmacy and Technology. 2026;19(3):1341-5. doi: 10.52711/0974-360X.2026.00192 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2026-19-3-53
REFERENCES:
1. Haouala A, Widmer N, Duchosal MA, Montemurro M, Buclin T, Decosterd LA. Drug interactions with the tyrosine kinase inhibitors imatinib, dasatinib, and nilotinib. Blood, The Journal of the American Society of Hematology. 2011; 117(8): e75-87. Available from: DOI: https://doi.org/10.1182/blood-2010-07-294330
2. Hartmann JT, Haap M, Kopp HG, Lipp HP. Tyrosine kinase inhibitors-a review on pharmacology, metabolism and side effects. Current drug metabolism. 2009; 10(5): 470-81. Available from: DOI: https://doi.org/10.2174/138920009788897975
3. Russo E, Spallarossa A, Tasso B, Villa C, Brullo C. Nanotechnology of tyrosine kinase inhibitors in cancer therapy: A perspective. International journal of molecular sciences. 2021; 22(12): 6538. Available from: DOI: https://doi.org/10.3390/ijms22126538
4. Eustace AJ, Crown J, Clynes M, O’Donovan N. Preclinical evaluation of dasatinib, a potent Src kinase inhibitor, in melanoma cell lines. Journal of Translational Medicine. 2008; 6(1): 1-1. Available from: DOI: https://doi.org/10.1186/1479-5876-6-53
5. Broniscer A, Baker SD, Wetmore C, Pai Panandiker AS, Huang J, Davidoff AM, Onar-Thomas A, Panetta JC, Chin TK, Merchant TE, Baker JN. Phase I Trial, Pharmacokinetics, and Pharmacodynamics of Vandetanib and Dasatinib in Children with Newly Diagnosed Diffuse Intrinsic Pontine GliomaPhase I Study of Vandetanib and Dasatinib in Children. Clinical Cancer Research. 2013; 19(11): 3050-8. Available from: DOI: https://doi. org/ 10.1158/1078-0432.CCR-13-0306
6. Kamath AV, Wang J, Lee FY, Marathe PH. Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS- 354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL. Cancer chemotherapy and pharmacology. 2008; 61: 365-76. Available from: DOI: https://doi.org/10.1007/ s00280-007-0478-8
7. Tomii T, Imamura T, Tanaka K, Kato I, Mayumi A, Soma E, Yano M, Sakamoto K, Mikami T, Morita M, Kiyokawa N. Leukemic.cells expressing NCOR1-LYN are sensitive to dasatinib in vivo in a patient-derived xenograft mouse model. Leukemia. 2021; 35(7): 2092-6. Available from: DOI: https://doi.org/ 10.1038/ s41375-020-01091-3
8. Manda H, Rao BK, Yashwant, Kutty NG, Swarnkar A, Swarnkar SK, et al. Antioxidant, Anti-Inflammatory and Antipyretic Activities of Ethyl Acetate Fraction of Ethanolic Extract of Schrebera swietenioides roxb. Root. Int J Toxicol Pharmacol Res. 2009; 1(1): 7–11. Available from: http://impactfactor.org/PDF/ IJTPR/1/IJTPR,Vol1,Issue1,Article2.pdf
9. Manda H, Swarnkar SK, Swarnkar A, Rasal AS, Shanbhag R, Gopalan Kutty N, et al. Wound Healing Potential of Pyrazole Derivative.Pharmacolgyonline. 2009;2:53–60. Available from: https://pharmacologyonline.silae.it/files/newsletter/2009/vol2/7.
10. Dheer R, Swarnkar SK, Syed F, Syeed F. Chromatographic Analysis of Barleria prionitis Linn. Res J Pharm Tech. 2019; 12(8): 3679–86. Available from: DOI: https://doi. org/10.5958/0974-360X.2019.00628.0
11. Gupta MK, Gupta R, Khunteta A, Swarnkar S. An Overview of Novel Techniques employed in Mouth Dissolving Drug Delivery System. Int J Eng generic Res. 2018; 4(3): 09–27.
12. Khunteta A, Swarnkar SK, Gupta Manish Kumar, Swarnkar Aruna, Jain Pankaj, Paliwal Sarvesh, Assessment of in-vitro antioxidant potential of ethyl acetate fraction of hydroalcoholic extract of Aerva javanica Linn. flowering tops. Asian Journal of Pharmaceutical Research and Development. 2019; 7(5): 133-137. Available from: DOI: https://doi.org/10.22270/ajprd.v7i5.520
13. Jain PK, Jain S, Chak P, Swarnkar SK et al. High-performance thin-layer chromatographic investigation of rutin in the leaves of Phoenix sylvestris in sequence with pharmacognostical and phytochemical evaluation. JPC-J Planar Chromat. 2020; 33: 191–201. Available from: DOI: https://doi.org/10.1007/s00764-020-00016-1
14. Laxane SN, Swarnkar SK, Zanwar SB, Setty MM. Anti-inflammatory Studies of the Alcoholic Extract of Zornia Gibbosa. Pharmacolgyonline. 2011; 1: 67–76. Available from: https:// pharmacologyonline.silae.it/files/archives/2011/vol1/005.sumit.pdf
15. Swarnkar S, Khunteta A, Gupta M, Jain P, Paliwal S. Pharmacognostic, Phytochemical and Pharmacological Review of “Phog”-Calligonum polygonoides L . J D rug D eliv T her. 2019; 9(2): 469–73. Available from: DOI: https://doi.org/10.22270/ jddt.v9i2.2384
16. Dheer R, Swarnkar S, Pesticidal residue analysis and phytochemical screening in leaves and roots of Barleria prionitis Linn., Journal of Drug Delivery and Therapeutics. 2018; 8(5): 455- 459. Available from: DOI: https://doi.org/10.22270/jddt.v8i5.1908
17. Swarnkar SK, Jain Y, Kumawat ML, Khunteta A, Paliwal S. Exploration of autonomic involvement in mechanism of antinociceptive activity of flowering top extract of Aerva javanica Linn. Asian Journal of Biochemical and Pharmaceutical Research. 2019; SI: 33-66.
18. Wang H, Wang H, Yang W, Yu M, Sun S, Xie B. Improved oral bioavailability and liver targeting of sorafenib solid lipid nanoparticles in rats. AAPS PharmSciTech. 2018; 19: 761-8. Available from: DOI: https://doi.org/10.1208/s12249-017-0901-3
19. Hoshino-Yoshino A, Kato M, Nakano K, Ishigai M, Kudo T, Ito K. Bridging from preclinical to clinical studies for tyrosine kinase inhibitors based on pharmacokinetics/pharmacodynamics and toxicokinetics/toxicodynamics. Drug metabolism and pharmacokinetics. 2011; 26(6): 612-20. Available from: DOI: https://doi.org/10.2133/dmpk.DMPK-11-RG-043