ArticlePharmaceuticals (Basel, Switzerland)2024
Evaluation of Solubility, Dissolution Rate, and Oral Bioavailability of β-Cyclodextrin and Hydroxypropyl β-Cyclodextrin as Inclusion Complexes of the Tyrosine Kinase Inhibitor, Alectinib.
Article in Pharmaceuticals (Basel, Switzerland), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Positively Charged Polymers Based on Cyclodextrins for Trametinib and Selumetinib Delivery in Glioblastoma Cancer.ChemMedChem · 2026Article
- In Vitro and In Vivo Evaluation of Alectinib-Loaded Dendrimer Nanoparticles as a Drug Delivery System for Non-Small Cell Lung Carcinoma.Pharmaceutics · 2025Article
- Article
- Smart Drug Delivery Systems Based on Cyclodextrins and Chitosan for Cancer Therapy.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Alectinib-Loaded Chitosan-Alginate Nanoparticles: A Novel Synthesis Method with In Vitro and In Vivo Evaluations.Pharmaceutics · 2025Article
- Prioritizing oral bioavailability in drug development strategies.Future medicinal chemistry · 2025Article
- Development and Evaluation of a Cost-Effective, Carbon-Based, Extended-Release Febuxostat Tablet.Molecules (Basel, Switzerland) · 2024Article
Corrections and comments
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Authors and funding
7 authors.
Funding
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Abstract
This study aims to improve the solubility and dissolution rate of alectinib (ALB), a tyrosine kinase inhibitor commonly used for treating non-small-cell carcinoma (NSCLC). Given ALB's low solubility and bioavailability, complexation with β-cyclodextrin (βCD) and hydroxy propyl β-cyclodextrin (HPβCD) was evaluated. Some of the different preparation methods used with varying ALB-to-CD ratios led to the formation of complexes that were characterized using Fourier-Transform Infrared (FTIR) techniques and Differential Scanning Calorimetry (DSC) to prove complex formation. The encapsulation efficiency was also determined. The simulations were carried out for ALB's interactions with βCD and HPβCD. This study identified the most soluble complex (ALB-HPβCD; 1:2 ratio) and evaluated its dissolution. The bioavailability of the ALB-HPβCD complex was evaluated in Wistar rats relative to free ALB. Pharmacokinetic profiles revealed increased Cmax (240 ± 26.95 ng/mL to 474 ± 50.07 ng/mL) and AUC0-48 (5946.75 ± 265 ng.h/mL to 10520 ± 310 ng.h/mL) with no change in the elimination rate constant. In conclusion, the complexation of ALB-HPβCD manages to increase in vitro solubility, the dissolution rate, and oral bioavailability, providing a favorable approach to improving ALB administration.
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Registered trials
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