Solid lipid nanoparticles of anticancer drug andrographolide: formulation, in vitro and in vivo studies

Abstract

Diterpenoidal anti-cancer drug andrographolide (AD) was encapsulated into solid lipid nanoparticle (SLN) because of poor aqueous solubility and high lipophilicity. AD-SLNs were prepared by solvent injection method and characterized for droplet size, surface morphology, zeta potential, etc. In vitro drug release was carried out by dialysis-membrane method. A pharmacokinetic study was performed by UPLC/Q-TOF-MS method to determine the maximum plasma concentration (C_max), area under the curve (AUC), etc. There was an improvement in C_max and AUC of AD-SLNs when compared with AD, thereby enhancing the bioavailability of AD. The t_max was increased than that of AD suspension, indicating the sustained release pattern of AD-SLNs. The antitumor activity was carried out on Balb/c mice showing better results with AD-SLNs as compared to AD. Thus, the AD-loaded SLNs would be useful for delivering poorly water-soluble AD with enhanced bioavailability and improved antitumor activity.

• Andrographolide
• antitumor activity
• pharmacokinetics
• solid lipid nanoparticles
• UPLC/Q-TOF-MS method

Acknowledgements

The authors are thankful to Department of Science and Technology, Government of India, for financial support and to Gattefosse (France) for providing gift sample of lipids. Authors are also thankful to Dr. Dwarka Nath, INMAS, New Delhi, India for providing EAC cells for in vivo anticancer activity.