Preparation, Characterisation
and In vivo Evaluation of
Bis-demethoxy
Curcumin Analogue (BDMCA) Nanoparticles
CA
Anuradha and Jithan Aukunuru*
Vaagdevi College of Pharmacy,
Ramnagar, Hanamkonda, AP, India-506001
*Corresponding author:
E-mail:
aukunjv@gmail.com
Tel: 0091-870-2455111
Received: 17 June 2009
Revised
accepted: 19 December 2009
Tropical
Journal of Pharmaceutical Research, February 2010;
9(1):
51-58
Abstract
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