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Research Article
Preparation,
Characterisation and In Vivo Evaluation of
Silybin Nanoparticles for the Treatment of Liver
Fibrosis
Chandrasekhar R Bonepally1,
Sai Jyothsna Gandey1, Krishnaveni Bommineni1,
Krishna Mohan Gottumukkala2 and Jithan
Aukunuru3*
1Vaagdevi College of Pharmacy,
Warangal, AP, 2Department of Pharmaceutical
Sciences, JNTU, Hyderabad, AP, 3Mother Teresa
College of Pharmacy, Hyderabad, AP, India
*For
correspondence :
E-mail:
aukunjv@gmail.com
Received:
17 November
2011 Revised accepted:
25 November 2012
Tropical
Journal of Pharmaceutical Research, February 2013;
12(1): 1-6
http://dx.doi.org/10.4314/tjpr.v12i1.1
Abstract
Purpose: To
formulate and characterize nanoparticles containing
silybin, and evaluate their activity against carbon
tetrachloride (CCl4)-induced liver toxicity.
Methods:
Silybin nanoparticles were formulated by o/w emulsion
solvent evaporation technique using poly-ε-caprolactone
as polymer. Four different nanoparticle formulations (NP1,
NP2, NP3 and NP4) were
prepared by varying the drug/polymer ratio. The
particles were characterized for particle size, drug
content and in vitro drug release. The pharmacokinetics
and pharmacodynamics of the silybin formulations in male
Wistar rats were evaluated following i.v.
administration, using silybin solution as reference. The
hepatoprotective activity of the formulations was also
determined in a CCl4-treated rat model.
Results:
Silybin nanoparticles were successfully prepared using
o/w emulsion solvent evaporation technique. The
nanoparticles sustained the release of the drug both in
vitro and in vivo for up to 10 days and offered better
pharmacokinetic properties than the free drug itself.
Intravenous nanoparticulate administration reversed
serum liver enzyme levels by 95 % compared to only 50 %
for the drug solution.
Conclusion: The
developed silybin nanoparticles showed superior
pharmacokinetic properties and hepatoprotective activity
to silybin solution.
Keywords : Silybin, Nanoparticles, Pharmacokinetics, Pharmacodynamics,
Hepatoprotective activity. |