Optimisation of cilnidipine nanoparticles using box-behnken design: in-vitro, toxicity and bioavailability assessment

ABSTRACT

Cilnidipine is an antihypertensive drug with low solubility and poor bioavailability. This study aimed to formulate and optimise nanoparticles to improve the solubility, drug release and bioavailability of cilnidipine. The cilnidipine nanoparticles were prepared by the anti-solvent precipitation-ultrasound technology and optimised by a 3-factor, 3-level Box- Behnken design. Particle size and zeta potential of the cilnidipine nanoparticles were 60 ± 7.18 nm and -14.5 ± 4.12 mV, respectively. A greater value of pharmacokinetic parameters–maximum plasma concentration and area under curve has indicated better drug absorption in the form of nanoparticles. The value of half-life of cilnidipine nanoparticles (1.2 h) decreased compared to the drug (2.4 h),which concluded that, the increased absorption of cilnidipine nanoparticles. These findings reinforce that the formulation of nanoparticles is a new approach for solubility and bioavailability enhancement of cilnidipine.

GRAPHICAL ABSTRACT

KEYWORDS:

• Cilnidipine
• nanoparticles
• surface response
• Box Behnken design
• pharmacokinetic study

Acknowledgments

The authors are very thankful to Savitribai Phule Pune University, Pune and Diya Laboratory, Mumbai, for providing DSC, PXRD and FTIR analysis facilities.

Disclosure statement

No potential conflict of interest was reported by the author(s).