ArticleHeliyon2024
Development, optimization, and characterization of polymeric micelles to improve dasatinib oral bioavailability: Hep G2 cell cytotoxicity and in vivo pharmacokinetics for targeted liver cancer therapy.
Article in Heliyon, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed.
- Fast-Dissolving and Highly Soluble Dasatinib Multicomponent Crystals Efficiently Inhibit Leukemia Cell Viability.ACS omega · 2026Article
- Antitumor Efficacy of Apatinib and Etoposide-Loaded D-α-Tocopheryl Polyethylene Glycol Succinate Mixed Micelles Against Multidrug-Resistant Ovarian Cancer Cells.Pharmaceutics · 2026Article
- Dasatinib Cube-O-Needle hybrid system for effective and safe site-specific treatment for triple-negative breast cancer.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Breaking barriers: nanosystems to overcome solubility and permeability challenges of second-generation tyrosine kinase inhibitors.Beilstein journal of nanotechnology · 2026Review
- Recent Advances and Future Prospects in Biological-Membrane-Targeted Polymers.Polymer science & technology (Washington, D.C.) · 2025Review
- Difenoconazole-Loaded Nanostructured Lipid Carriers: Preparation, Characterization, and Evaluation.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Harnessing the Power of Nanocarriers to Exploit the Tumor Microenvironment for Enhanced Cancer Therapy.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Hyaluronic acid-coated capecitabine nanostructures for CD44 receptor-mediated targeting in breast cancer therapy.RSC advances · 2025Article
- Pluronic P123/L64 Mixed Micelles as Immediate Release Systems to Enhance the Bioavailability of Praziquantel in Rats.International journal of nanomedicine · 2025Article
- Nanomaterials targeting cancer stem cells to overcome drug resistance and tumor recurrence.Frontiers in oncology · 2025Review
Corrections and comments
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The efficacy of dasatinib (DAS) in treating hepatocellular carcinoma (HCC) is hindered by its poor bioavailability, limiting its clinical potential. In this study, we explored the use of TPGS-Soluplus micelles as an innovative drug delivery platform to enhance DAS solubility, stability, and therapeutic impact. A series of TPGS-Soluplus copolymers were synthesized, varying the D-α-tocopheryl polyethylene glycol succinate (TPGS) forms (1000, 2000, and 3500) and adjusting the TPGS to Soluplus weight ratios (1:1, 1:2, and 1:3). Our goal was to identify the optimal formulation with the highest entrapment efficiency, smallest particle size, and enhanced drug loading. The TPGS1000-Soluplus copolymer, with a DAS-to-polymer ratio of 1:30 and a TPGS ratio of 1:2, demonstrated superior performance, achieving an entrapment efficiency of 64.479 ± 1.45 % and drug loading of 5.05 ± 1.01 %. The DAS-loaded micelles (DAS-PMs) exhibited a notably small particle size of 64.479 ± 1.45 nm and demonstrated controlled release kinetics, with 85.60 ± 5.4 % of the drug released over 72 h. Cellular uptake studies using Hep G2 cells revealed significantly enhanced absorption of DAS-PMs compared to free DAS, reflected in lower IC50 values in MTT assays at 24 and 48 h. Pharmacokinetic analysis further highlighted the benefits of the DAS-PMs, with an AUC0-∞ 2.16 times higher and mean residual time (MRT) 1.3 times longer than free DAS, a statistically significant improvement (p < 0.01). These findings suggest that TPGS-Soluplus micelles offer a promising strategy for improving the bioavailability and efficacy of DAS in HCC treatment, presenting a potential new therapeutic avenue for patients with limited options. This innovative formulation could significantly enhance DAS delivery, potentially leading to improved clinical outcomes in liver cancer therapy.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.