SAILOR, G. U.
Design of Experiment Approach Based Formulation Optimization of Berberine Loaded Solid Lipid Nanoparticle for Antihyperlipidemic Activity - Vol.83(2), March-April - Mumbai Indian Journal of Pharmaceutical Science 2021 - 204-218p.
Berberine is an isoquinoline alkaloid possesses multitude of biological e ffects. However, quaternary
amine cation of berberine causes poor water solubility, resulting in low bioavailability which limits its
pharmacological purpose. The aim of this study was to prepare and optimize berberine loaded solid
lipid nanoparticle and to evaluate its pharmacokinetic and antihyperlipidemic activity. The solid lipid
nanoparticles were prepared by solvent injection method and 3 2 full factorial design was used to study
the e ffect of concentration of polyvinyl alcohol (X 1) and amount of lipid (X 2) on particle size (Y 1) and
entrapment e fficiency (Y2). The formulation was optimized using desirability function and evaluated
for physicochemical, morphological, in vitro drug release and in vivo pharmacokinetic study. In vivo
antihyperlipidemic activity of the formulation was also studied using high fat diet induced hyperlipidemia
model. The formulation optimized by validated experimental design comprise of 1 % w/v polyvinyl alcohol,
279 mg lipid (stearic acid) to achieve particle size of 395 nm with 82.44 % entrapment e fficiency. In vitro
release study of berberine loaded solid lipid nanoparticle showed an initial burst release followed by slow
and continuous release. Berberine loaded solid lipid nanoparticle also showed 4.13 folds improvement
in relative bioavailability compared to Berberine suspension. Furthermore, Berberine loaded solid lipid
nanoparticle ameliorate the levels of total cholesterol (-41 %), TG (-49 %), lipoprotein cholesterol-C
(-80 %) and high-density lipoprotein cholesterol(+119 %) compared to hyperlipidemic control and also
found to be better than pure drug. The prepared berberine loaded solid lipid nanoparticle are successful
drug delivery system demonstrating its e ffectiveness in controlling hyperlipidemia due to the improved
bioavailability of berberine.
PHARMACEUTICS
Design of Experiment Approach Based Formulation Optimization of Berberine Loaded Solid Lipid Nanoparticle for Antihyperlipidemic Activity - Vol.83(2), March-April - Mumbai Indian Journal of Pharmaceutical Science 2021 - 204-218p.
Berberine is an isoquinoline alkaloid possesses multitude of biological e ffects. However, quaternary
amine cation of berberine causes poor water solubility, resulting in low bioavailability which limits its
pharmacological purpose. The aim of this study was to prepare and optimize berberine loaded solid
lipid nanoparticle and to evaluate its pharmacokinetic and antihyperlipidemic activity. The solid lipid
nanoparticles were prepared by solvent injection method and 3 2 full factorial design was used to study
the e ffect of concentration of polyvinyl alcohol (X 1) and amount of lipid (X 2) on particle size (Y 1) and
entrapment e fficiency (Y2). The formulation was optimized using desirability function and evaluated
for physicochemical, morphological, in vitro drug release and in vivo pharmacokinetic study. In vivo
antihyperlipidemic activity of the formulation was also studied using high fat diet induced hyperlipidemia
model. The formulation optimized by validated experimental design comprise of 1 % w/v polyvinyl alcohol,
279 mg lipid (stearic acid) to achieve particle size of 395 nm with 82.44 % entrapment e fficiency. In vitro
release study of berberine loaded solid lipid nanoparticle showed an initial burst release followed by slow
and continuous release. Berberine loaded solid lipid nanoparticle also showed 4.13 folds improvement
in relative bioavailability compared to Berberine suspension. Furthermore, Berberine loaded solid lipid
nanoparticle ameliorate the levels of total cholesterol (-41 %), TG (-49 %), lipoprotein cholesterol-C
(-80 %) and high-density lipoprotein cholesterol(+119 %) compared to hyperlipidemic control and also
found to be better than pure drug. The prepared berberine loaded solid lipid nanoparticle are successful
drug delivery system demonstrating its e ffectiveness in controlling hyperlipidemia due to the improved
bioavailability of berberine.
PHARMACEUTICS