Design and characterization of solid lipid nanoparticles of Ibrutinib

Ibrutinib, a Bruton's tyrosine kinase (BTK) inhibitor used in the treatment of B-cell malignancies, faces significant limitations due to its poor aqueous solubility and low oral bioavailability. To address these challenges, the present study aimed to develop and characterize solid lipid nanoparticles (SLNs) of Ibrutinib using the homogenization–bath sonication method. Preformulation studies, including FTIR and PXRD, confirmed no chemical interaction between Ibrutinib and excipients and revealed conversion of the drug from crystalline to amorphous form, thereby enhancing solubility. Gelucire 44/14 was selected as the optimal lipid, with Labrasol and Tween 80 chosen as lipophilic and hydrophilic surfactants, respectively, based on their emulsification efficiency and stability enhancement properties. Among the formulations developed (S1–S6), formulation S6 showed the most favorable characteristics: a particle size of 132.6 nm, PDI of 0.219, zeta potential of –31.2 mV, and entrapment efficiency of 96%. In vitro drug release of S6 demonstrated a biphasic pattern with an initial burst followed by sustained release, achieving 99.5% release over 24 hours. Drug release kinetics followed the Korsmeyer- Peppas model, suggesting a combined diffusion and erosion mechanism. Stability studies conducted at 40 ± 2 °C and 75 ± 5% RH for one month indicated no significant deviation in physical parameters or drug content, confirming the robustness of the formulation. In conclusion, the optimized SLN formulation of Ibrutinib successfully improved solubility, sustained drug release, and exhibited excellent stability, making it a promising approach for enhancing therapeutic efficacy.