Preparation, Characterisation and In vivo Evaluation of Bis-demethoxy Curcumin Analogue (BDMCA) Nanoparticles

Purpose: To fabricate biodegradable nanoparticle formulation of bis-demethoxy curcumin analogue (BDMCA), a novel curcumin analogue, and evaluate its in vitro and in vivo characteristics.
Methods: Nanoparticle formulations were fabricated by a double emulsion solvent evaporation technique using polycaprolactone as the polymer. The nanoparticles were characterised for drug content, particles size, in vitro drug release and the drug-polymer interaction. The in vivo properties of the formulations in male Wistar rats were evaluated from the pharmacokinetics and pharmacodynamics of BDMCA following i.v. administration of the nanoparticles. BDMCA solution was administered i.v. as a reference. Hepatoprotectivity of the formulation was determined in a CCl4-treated rat model.
Results: The BDMCA nanoparticles were successfully prepared using double emulsion solvent evaporation technique. The nanoparticle formulations effectively sustained the release of the drug for more than 10 days both in vitro and in vivo. They also offered better pharmacokinetic properties to the drug than that afforded by the free drug itself. Intravenous nanoparticular administration reversed serum liver enzyme levels by 90%, compared to 52 % for repeated i.v. administration of the solution form.
Conclusion: BDMCA particle demonstrated good pharmacokinetic and pharmacodynamic properties following i.v. administration.

Keywords
Curcumin analogue; Nanoparticles; pharmacokinetics; Pharmacodynamics; Hepatoprotective activity