Lipid-Polymer Hybrid Nanocarriers for Oral Delivery of Felodipine: Formulation, Characterization and Ex-Vivo Evaluation

Abstract

Purpose: Felodipine, is a calcium-channel antagonist used for hypertension and angina pectoris. It is practically insoluble in aqueous media and shows low oral bioavailability (15%-20%). This investigation aims to prepare and characterize oral felodipine lipid-polymer hybrid nanocarriers (LPHNs) to increase solubility and control delivery for increasing bioavailability and enhance patient compliance. Methods: The newly microwave-based method was prepared with felodipine LPHNs (H1-H35) successfully. The (H1-H35) were subjected to thermodynamic stability experiments. After that, select nine felodipine LPHNs (F1-F9) that have smart physical stability for further optimization of different characterization processes. Results: The felodipine LPHNs (F4) are considered the most optimized formula. It was characterized by lower particle size (33.3 nm), lower PDI (0.314), high zeta potential (13.6 mV), entrapment efficiency is (81.645 %w/w), drug loading is (16.329 % w/w), the pH value is 4, excellent percent of light transmittance (95.5%), pseudoplastic rheogram, significantly high (p< 0.05) dissolution rate with sustained drug delivery and success ex-vivo intestinal permeation attributes. The (F4) subject for further investigations of fourier transformed infrared spectroscopy (FTIR), atomic force microscopy (AFM), and transmission electron microscopy (TEM). The results of FTIR, AFM, and TEM indicate there is no interaction between the felodipine and excipients and that the particulate system in the nanoscale dispersion system confirms the high stability. Conclusion: The optimized felodipine LPHNs (F1-F9) formulations were smart formulations for sustained oral delivery of felodipine and that F4 was the most optimized formula according to its characterization processes.