ArticleScientific reports2025
Physicochemical characterization and biological evaluation of amorphous solid dispersions of an anticancerous drug: Erlotinib HCl.
Article in Scientific reports, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed.
- Nonclinical and Clinical Assessments of an Optimized Tablet Formulation of the Novel HER2-Selective Tyrosine Kinase Inhibitor Zongertinib: Focus on Relative Bioavailability and Impact of Variation of Gastric pH.Molecular pharmaceutics · 2025Trial
- The Impact of Polymers in Amorphous Solid Dispersion on the Bioavailability of Sulfonylureas and Meglitinides.Drug design, development and therapy · 2026Review
- Exploring the anticancer potential ofIn silico pharmacology · 2025Article
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Authors and funding
5 authors.
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Abstract
Erlotinib hydrochloride (ERL), a tyrosine kinase inhibitor, is effective in treating various cancers. However, low aqueous solubility limits its bioavailability and therapeutic efficacy. We developed an amorphous solid dispersion (ASD) of ERL with biocompatible polymers, polyvinylpyrrolidone (PVP-K30), and polyethylene glycol (PEG-4000) for enhanced amorphization, miscibility, and molecular interactions. The present study focuses on the physicochemical characterization of formulated ASD of ERL using Fourier Transform Infrared Spectroscopy (FTIR), X-ray Powder Diffraction (PXRD), UV-Visible Spectroscopy, and High-Performance Liquid Chromatography (HPLC), along with biological evaluation including antioxidant, cytotoxicity, and antitumor studies in mouse tumor models. FTIR analysis confirmed the retention of ERL's characteristic peaks in ASDs with PVP, PEG, and PVP/PEG, with shifts to lower frequencies for C=O bending, CH₂ deformation and CH symmetric deformation, indicating reduced molecular vibration energy, increased molecular flexibility, and strong drug-polymer interactions. PXRD analysis confirmed the transformation of crystalline ERL into an amorphous state in ASDs, as evidenced by the diminished ERL peaks at 11.7°, 16.2°, 21.7°, 24.75°, 25.56°, and 29.37°. UV spectroscopy revealed shifts in absorption peaks (256 nm), suggesting favorable drug-polymer interactions. HPLC demonstrated enhanced release rates at 4.72 retention time. In dissolution studies, the ERL + PEG formulation attained the greatest dissolution rate (80%). ERL + PVP showed superior DPPH radical scavenging activity with an IC
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