ArticleAAPS PharmSciTech2025
Unveiling the Potential of Nanosuspension Formulation Strategy for Improved Oral Bioavailability of Gefitinib.
Article in AAPS PharmSciTech, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed.
- Development and In Vitro Evaluation of Gefitinib-Salicylic Acid Nanocrystals for Improved Bioavailability.Pharmaceutics · 2026Article
- Self-Assembled Gefitinib Nanosuspension Prepared via Hummer Acoustic Resonance Technology: Enhanced Dissolution, In Vitro Anticancer Activity and Long-Term Stability.Pharmaceutics · 2026Article
- Design and Optimization of Indomethacin Nanocrystals using Machine Learning and Molecular Dynamics Simulations.AAPS PharmSciTech · 2026Article
- Mucoadhesive Carbohydrate-Based Polymeric Nanocapsule Loaded with Palbociclib for Enhanced GIT Retention and In Vitro Anticancer Efficacy in MDA-MB-231 Cells.AAPS PharmSciTech · 2025Article
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Gefitinib (GB), an oral tyrosine kinase inhibitor suffers major setbacks in clinical application due to limited aqueous solubility leading to poor oral bioavailability. Nanosuspension serves as a promising formulation strategy to overcome the above-mentioned drawbacks. Hence, the present study involves the development of gefitinib nanosuspension (GB-NS) using High-pressure homogenization (HPH) to increase its aqueous solubility and maximize oral bioavailability. GB-NS was optimized by utilizing the quality-by-design strategy to optimize independent variables such as homogenization pressure, drug-to-stabilizer ratio, and number of cycles. Lecithin was found to stabilize the nanosuspension with optimal particle size, PDI, and zeta potential of 157 ± 18.77 nm, 0.296 ± 0.040, and -33.25 respectively. Intriguingly, a drug-to-stabilizer ratio significantly influenced (p < 0.005) particle size and PDI, establishing its crucial role in optimization. The morphological characterization by SEM of GB-NS revealed a rod-shaped structure. Thereafter, the thermal and powder X-ray analysis depicted the crystalline nature of gefitinib in GB-NS. Additionally, GB-NS exhibited enhanced saturation solubility (~ 2.4- and ~ 3.4-fold) and dissolution rate (~ 2.5- and ~ 3.5-fold) compared to pure GB in 0.1 N HCl and PBS 6.8 respectively. GB-NS remained stable under both storage conditions ( 25°C and 4°C). Finally, the pharmacokinetic study depicted a considerable increase in C
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