Abstract
Most biopharmaceutics classification system (BCS) class IV drugs have limited oral bioavailability due to poor solubility and poorer permeability. This work aims to investigate the possibility of utilizing disulfide bridged nanoparticles to improve BCS IV drug solubility and oral absorption. Disulfide bridged nanoparticles were made using thiolated sodium alginate (TSA) and thiolated eudragit RS100 (TERS100). This study used paclitaxel (PTL) as a model drug to create PTL-loaded nanoparticles using the air oxidation approach. PTL-loaded nanoparticles boosted the solubility of PTL by over 11 times (∼59 μg/mL). The nanoparticles had particle sizes of 103 nm, polydispersity indices of 0.034, and zeta potentials of -21 mV, respectively. Nanoparticles demonstrated 75.34% and 89.18% entrapment and loading efficiency of PTL, respectively. The PTL release data from nanoparticles had good sustained release properties. The effective permeability of PTL from nanoparticles was 2.19-fold higher than that of pure PTL suspension. The relative bioavailability of PTL with disulfide bridged nanoparticles was 237.11%, which was much higher than that of PTL suspension, according to the pharmacokinetic data. These results show that disulfide bridged nanoparticles have a wide range of clinical applications.
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