Optimization of Andrographolide Nanocrystal-loaded Liposomes by Box-Behnken Design and its In vitro and In vivo Evaluation
Liangxing Tu, Siying Wang, Hansong Wu, Zijian Zou, Banghuai Xing, Lingyu Yang, Zhiyang Lu, Meng ChengIntroduction:
The optimum process for andrographolide nanocrystal-loaded liposomes was optimized using Box-Behnken design, and its in vitro and in vivo evaluation was subsequently studied.
Methods:
Scanning electron microscopy, transmission electron microscopy, X-ray powder diffraction, and differential scanning calorimetry were used to study the physical and chemical properties. Short-term stability was assessed by measuring changes in particle size and PDI. The in vitro release behavior of andrographolide nanocrystals, andrographolide liposomes, and andrographolide nanocrystal- loaded liposomes in pure water and PBS buffer was studied by the dialysis bag method. The pharmacokinetic properties of andrographolide formulations in vivo were explored when using male Sprague-Dawley rats.
Results:
Encapsulation within liposomes, regardless of the initial drug form, effectively sustained the drug, with Slow release of 80 % in PBS (p<0.05). Andrographolide nanocrystal-loaded liposomes had good short-term stability. Additionally, the pharmacokinetic behavior showed that, excluding the higher Cmax of andrographolide liposomes and andrographolide nanocrystal-loaded liposomes, the pharmacokinetic parameters were similar (p<0.05). These hardly improve the pharmacokinetic behaviors by the intravenous route, and the potential mechanisms for the widely reported higher therapeutic efficacy of these technologies may be enhanced target efficacy or cellular uptake.
Discussion:
This study conducted in vitro and in vivo performance tests on liposomes loaded with nanocrystals, and explored the performance of this preparation from various perspectives.
Conclusion:
This nanocrystal-loaded liposomes display great potential for the therapeutic mechanisms of nanoformulations, and helps researchers to better design and understand the therapeutic mechanisms of nanoformulations.