Cilnidipine nanocrystals; Formulation, characterization and bioavailability study

Abstract

Cilnidipine a fourth generation calcium channel blockers, it was utilized to reduce cardiovascular events. Since cilnidipine is a material classified as Biopharmaceutics Classification System (BCS) Class-II, which is extremely poorly soluble and has a high permeability in turn low bioavailability. Thus, by employing solvent anti-solvent technology, cilnidipine (CLD) can be produced as nanocrystals (NCs). Getting beyond those obstacles could boost the material's solubility and bioavailability. A pair of distinct stabilizers (Soluplus® and Tween20) in a ratio of CLD: Soluplus : Tween20 (1:0.25:0.5) were used to prepare cilnidipine nanocrystals (CLD NCs). Rats were used to evaluate and assess the pharmacokinetics in vivo parameters of CLD and CLD NCs. The optimal formula that was created revealed 62.1 nm with 0.18, which represent particle size and polydispersity index (PDI), respectively. At 6 minutes, 99% of CLD NCs were released in phosphate buffer 6.8. It is evident that CLD NCs had a higher relative bioavailability by around 3.17 times and that their area under the concentration time curve (AUC) and CPmax were greater than those of bulk CLD. Additionally, the CLD NCs' Tmax was lower than that of the CLD pure medication. Accordingly, it was evident from the observed pharmacokinetic parameters (AUC, CPmax, and Tmax) that the CLD NCs enhanced the the oral bioavailability of CLD in rats.