Amorphous solid dispersions of erlotinib HCl for enhancing solubility and bio-availability

The bioavailability and therapeutic effectiveness of BCS Class II anticancer drugs, such as erlotinib (ERL), are limited by poor solubility.Amorphous solid dispersion (ASD) is an innovative formulation technique to enhance dissolution, solubility, and pharmacokinetic profiles.Erlotinib, a tyrosine kinase inhibitor with limited solubility, was transformed into an amorphous state using solvent evaporation with polymers like polyvinylpyrrolidone (PVP) and polyethylene glycol (PEG).Analytical techniques including FTIR, UV-vis spectroscopy, XRD, DSC, and dielectric spectroscopy confirmed the transition and highlighted polymer effects on drug properties.Dielectric studies revealed a single -relaxation in ERL+PVP, but dual relaxations in ERL+PEG+PVP ASDs.-relaxation appeared in the glassy states of ERL+PEG and ERL+PEG+PVP.Molecular dynamics simulations showed ERL+PEG is a fragile glass former, while ERL+PVP and ERL+PEG+PVP are strong glass formers, influenced by hydrogen bonding and molecular mobility.ASDs improved solubility, stability, and biological performance, enhancing antioxidant and antiproliferative properties.ERL+PEG ASD significantly inhibited DLA-induced tumor growth in mice, achieving a 98.78 0.3% reduction.These findings demonstrate the potential of polymer-based amorphization strategies to optimize drug delivery and therapeutic efficacy.