<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml">A 32 factorial design was employed to produce glipizide lipospheres by the emulsification phase separation technique using paraffin wax and stearic acid as retardants. The effect of critical formulation variables, namely levels of paraffin wax (X1) and proportion of stearic acid in the wax (X2) on geometric mean diameter (<italic>dg</italic>), percent encapsulation efficiency (% <italic>EE</italic>), release at the end of 12 h (<italic>rel</italic>12) and time taken for 50% of drug release (<italic>t</italic>50), were evaluated using the <italic>F</italic>-test. Mathematical models containing only the significant terms were generated for each response parameter using the multiple linear regression analysis (MLRA) and analysis of variance (ANOVA). Both formulation variables studied exerted a significant influence (<italic>p</italic> &lt; 0.05) on the response parameters. Numerical optimization using the desirability approach was employed to develop an optimized formulation by setting constraints on the dependent and independent variables. The experimental values of <italic>dg</italic>, % <italic>EE</italic>, <italic>rel</italic>12 and <italic>t</italic>50 values for the optimized formulation were found to be 57.54 ± 1.38 μm, 86.28 ± 1.32%, 77.23 ± 2.78% and 5.60 ± 0.32 h, respectively, which were in close agreement with those predicted by the mathematical models. The drug release from lipospheres followed first-order kinetics and was characterized by the Higuchi diffusion model. The optimized liposphere formulation developed was found to produce sustained anti-diabetic activity following oral administration in rats.</abstract>

A 32 factorial design was employed to produce glipizide lipospheres by the emulsification phase separation technique using paraffin wax and stearic acid as retardants. The effect of critical formulation variables, namely levels of paraffin wax (X1) and proportion of stearic acid in the wax (X2) on geometric mean diameter (dg), percent encapsulation efficiency (% EE), release at the end of 12 h (rel12) and time taken for 50% of drug release (t50), were evaluated using the F-test. Mathematical models containing only the significant terms were generated for each response parameter using the multiple linear regression analysis (MLRA) and analysis of variance (ANOVA). Both formulation variables studied exerted a significant influence (p < 0.05) on the response parameters. Numerical optimization using the desirability approach was employed to develop an optimized formulation by setting constraints on the dependent and independent variables. The experimental values of dg, % EE, rel12 and t50 values for the optimized formulation were found to be 57.54 ± 1.38 μm, 86.28 ± 1.32%, 77.23 ± 2.78% and 5.60 ± 0.32 h, respectively, which were in close agreement with those predicted by the mathematical models. The drug release from lipospheres followed first-order kinetics and was characterized by the Higuchi diffusion model. The optimized liposphere formulation developed was found to produce sustained anti-diabetic activity following oral administration in rats.

Design and statistical optimization of glipizide loaded lipospheres using response surface methodology

Department of Pharmaceutical, K.L.E.S's College of Pharmacy, Bangalore-560010, India

Department of Pharmacology, K.L.E.S's College of Pharmacy, Bangalore-560010, India

Acta Pharmaceutica

A 32 factorial design was employed to produce glipizide lipospheres by the emulsification phase separation technique using paraffin wax and stearic acid as...

Design and statistical optimization of glipizide loaded lipospheres using response surface methodology

Published Online: Sep 18, 2007

Page range: 269 - 285

DOI: https://doi.org/10.2478/v10007-007-0022-8

Keywords
liposfere, glipizid, faktorijalni dizajn, metodologija odgovora površine, optimizacija

This content is open access.

Design and statistical optimization of glipizide loaded lipospheres using response surface methodology

Published Online: Sep 18, 2007

Page range: 269 - 285

DOI: https://doi.org/10.2478/v10007-007-0022-8

Keywordsliposfere, glipizid, faktorijalni dizajn, metodologija odgovora površine, optimizacija

This content is open access.

Keywords
liposfere, glipizid, faktorijalni dizajn, metodologija odgovora površine, optimizacija