Comparative evaluation of pharmacokinetic parameters between a pure nisoldipine suspension and a nisoldipine-loaded bilosome suspension

Abstract

Bilosomes are nanocarriers that contain bile salts in their vesicular bilayer, thereby enhancing their flexibility and durability in the gastrointestinal tract. Unlike conventional vesicular systems they provide distinct advantages such as streamlined manufacturing procedures, cost efficiency, and improved stability. The main objective of this study was to attain a comparison of the pharmacokinetic parameters of nisoldipine (NSD) after administering an ordinary NSD suspension and an NSD-loaded bilosome suspension. The study used 60 Swiss albino rats weighing 200±15 g and divided into two groups (n=30 each). A dose of 2.2 mg/kg of NSD was administered from the ordinary NSD suspension to the rats of the first group and the same dose of NSD-loaded bilosome suspension was administered to the rats of the second group. NSD levels were determined in the rat plasma by using high-performance liquid chromatography. Our results showed that the Cmax, the Tmax, and the AUC0-36 were 51.47±0.94 ng/mL, 2±0.3 h, and 323.33±21 ng×h/mL for the pure suspension, and 116.41±1.22 ng/mL, 4±0.7 h, and 916±64.09 ng×h/mL for the bilosome suspension, respectively. The maximum concentration was significantly different between the pure and the bilosomal preparation (P<0.05), while the relative bioavailability of the pure suspension was 2.9 times that of the bilosomal suspension, 36 h after a single-dose NSD administration. In conclusion, the prepared bilosomal suspension enhanced the bioavaila¬bility of NSD, and could be considered as a vital delivery system.