Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation. (12th October 2016)

• Record Type: Journal Article
• Authors: Yuan, Huiling; Li, Xin; Zhang, Caiyun; Pan, Wenli; Liang, Yumeng; Chen, Yang; Chen, Weidong; Liu, Lulu; Wang, Xiaomin
• Is Part Of: Drug delivery. Volume 23:Number 8(2016:Nov.)
• Page Start: 2772
• Page End: 2779
• Publication Date: 2016-10-12
• Subjects: Cytotoxicity -- gambogenic acid -- in vivo pharmacokinetics -- in vitro release -- nanosuspensions; Drug delivery systems -- Periodicals; Drug targeting -- Periodicals; 615.05
• DOI: 10.3109/10717544.2015.1077294
• Languages: English
• ISSNs: 1071-7544

Abstract

Abstract: Nanosuspensions (NS) can enhance the saturation solubility and dissolution velocity of poorly soluble drugs. PEG as a non-ionic surfactant plays an important role in surface modification of nanoparticles for prolonging in vivo circulation. In this study, anti-solvent precipitation method was introduced to prepare gambogenic acid nanosuspensions (GNA-NS) with PVPK30 and PEG2000 as stabilizers to settle the disadvantages of GNA. The obtained nanoparticles were spherical with a mean particle size of 183.7 nm and a zeta potential of −22.8 mV. The entrapment efficiency and drug loading of the resultant formulation were 97.3 and 29.73%. X-ray diffraction analysis confirmed the amorphous phase of GNA in NS. Fourier transform infrared indicated there may be hydrogen bond interaction between the drug and excipients. After lyophilization of GNA-NS, the freeze-dried powder displayed sufficient long-term physical stability at 4 and 25 °C. In comparison to GNA solution, in vitro studies of GNA-NS showed much slower release and higher cytotoxicity in HepG2 cells. What's more, the pharmacokinetic study in rats revealed that the AUC 0–∞ and t 1/2 of GNA-NS were increased 2.63- and 1.77-fold than that of the reference formulation. Taken together, in vitro/in vivo evaluations showed NS would be an effectively strategy to change the poor aqueous solubility and prolong the half-life for GNA. The GNA-NS with enhanced bioavailability and drug efficacy provided a promising delivery system for the application of GNA.