Hybrid polylactic acid/Eudragit L100 nanoparticles: A promising system for enhancement of bioavailability and pharmacodynamic efficacy of luteolin

Luteolin is a valuable natural drug for the treatment of oxidative stress associated diseases, but its use is hindered by gastric instability and poor bioavailability. Given that hybrid polymeric nanoparticles may have potential applications in the design of oral drug delivery systems, this study aims to develop luteolin loaded hybrid polylactic acid/Eudragit L100 nanoparticles. By nanoprecipitation, different formulations were prepared, optimized and characterized in terms of physicochemical properties, stability and in vivo performance.

The optimum formulation presented particle size of 452.23 ± 22.4 nm, zeta potential of 0.92 mV ± 0.04, entrapment efficiency of 71.02 ± 14.6% and loading efficiency of 11.21 ± 3.1%, in accordance with the values predicted created by Box-Behnken design. In vitro, the system was capable of protection of luteolin in simulated gastric fluid, while a release study confirmed the controlled luteolin release pattern. Interaction between system components was verified through infrared and thermal analysis. The maximum plasma concentration of luteolin in the optimized formulation was significantly improved (212.2 %, p < 0.05) when compared to conventional luteolin suspension whereas the relative bioavailability accounted 2.61-fold.

In vivo pharmacodynamic studies in CCL₄ toxicity induced model revealed faint liver, kidney and testicular changes in terms of biochemical and histological evaluation. The findings of this study revealed that hybrid polylactic acid/Eudragit L100 nanoparticles are responsible for improved pharmacological efficacy of orally administered luteolin, thereby indicating the benefits of using such system to overcome the problems facing luteolin oral delivery.

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Article information: Mohammed Elmowafy, Nabil A. Alhakamy, Khaled Shalaby, Sultan Alshehri, Hazim M. Ali, Elshaer F. Mohammed, Nabil K. Alruwaili, Ameeduzzafar Zafar, Hybrid polylactic acid/Eudragit L100 nanoparticles: A promising system for enhancement of bioavailability and pharmacodynamic efficacy of luteolin, Journal of Drug Delivery Science and Technology, Volume 65, 2021. https://doi.org/10.1016/j.jddst.2021.102727.