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Formulating and Characterizing Lipid Nanoparticles for Gene Delivery using a Microfluidic Mixing Platform
Published on: February 25, 2021
Characterization, in vitro release, and pharmacokinetics of rupestonic acid derivative nanostructured lipid carriers
Xin Fan1, Xin Wang1, Shuyan Han1
1State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, 830011, China; University of Chinese Academy of Sciences, No 19(A) Yuquan Road, Shijingshan District, Beijing, 100049, China.
Abstract:
This study aimed to enhance the oral bioavailability of the rupestonic acid derivative CAM106 by developing nanostructured lipid carriers (NLCs) as its delivery system. CAM106-NLCs were prepared via the organic solvent evaporation method, with formulation optimization using the Box-Behnken response surface design. The optimized CAM106-NLCs showed an encapsulation efficiency of 98.36 ± 0.05 %, drug loading of 6.05 ± 0.04 %, and mean particle size of 165.4 ± 9.87 nm, with a spherical morphology as confirmed by transmission electron microscopy (TEM). The optimized CAM106-NLCs exhibited excellent short-term stability when stored at 4 °C. In vitro release studies demonstrated that CAM106-NLCs exhibited improved release profiles compared to free CAM106. Furthermore, in vivo pharmacokinetic studies in rats demonstrated that CAM106-NLCs enhanced the relative oral bioavailability of CAM106 by approximately 2.11-fold, underscoring their potential to improve oral delivery.
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