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. 2019;7(1):72-85.
doi: 10.2174/2211738507666190319124513.

Preparation, Optimization and In vitro Evaluation of Glipizide Nanoparticles Integrated with Eudragit RS-100

P Saharan  1 , K Bahmani  2 , S P Saharan  1
Affiliations

Preparation, Optimization and In vitro Evaluation of Glipizide Nanoparticles Integrated with Eudragit RS-100

P Saharan et al. Pharm Nanotechnol. 2019.

Abstract

Background: Solubility is an important criterion for drug efficacy, independent of the route of administration. It also poses a major challenge for pharmaceutical industries, which are developing new pharmaceutical products, since 40% of the active substances being identified are either insoluble or poorly soluble in aqueous media.

Objective: The objective of this study was to develop nanoformulation of glipizide drugloaded nanoparticles providing controlled release formulation.

Method: Nanoparticles were prepared by the solvent evaporation method. Eudragit RS100, a nonbiodegradable polymer with varying ratios was used for making the formulation. The effect of key formulation variables on the particle size and entrapment efficiency and drug loading of nanoparticles were studied by using factorial design.

Results: DSC thermograms indicate that glipizide was dispersed in an amorphous state in the polymer. TEM study indicates that the nanoparticles were in spherical shape. The mean diameter was dependent on the presence of the amount of Eudragit RS100 and viscosity of the organic phase. The in vitro study showed that the cumulative drug release was from 69.52-81.44 % in 10 hrs at pH 6.8 in phosphate buffer respectively.

Conclusion: The developed NPs could reduce dose frequency, decrease side effects, and improve patient compliance. Using factorial design, maximum entrapment efficiency with minimum particle size could be achieved with a few experiments.

Keywords: Characterization; Eudragit RS-100; glipizide; nanoparticles; optimization; solvent evaporation..

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Figures

Fig. (1)
Fig. (1)
Response surface plot showing combined effects of Eudragit rs-100 and pva on particle size of nanoparticles.
Fig. (2)
Fig. (2)
Response surface plot showing combined effect of Eudragit rs-100 and pva on % entrapment efficiency of nanoparticles.
Fig. (3)
Fig. (3)
Response surface plot showing combined effect of Eudragit rs-100 and pva on percent drug loading of nanoparticles.
Fig. (4)
Fig. (4)
Particle size of glipizide loaded Eudragit rs100 nanoparticles of different formulations.
Fig. (5)
Fig. (5)
Entrapment efficiency of glipizide loaded Eudragit rs100 nanoparticles of different formulations.
Fig. (6)
Fig. (6)
Drug loading of glipizide loaded Eudragit rs100 nanoparticles different formulations.
Fig. (7)
Fig. (7)
FTIR spectra of glipizide.
Fig. (8)
Fig. (8)
DSC thermogram of glipizide loaded rs 100 optimized batch.
Fig. (9)
Fig. (9)
Drug release profile of F1-F16.
Fig. (10)
Fig. (10)
Drug release profile of formulations (F7-F13).
Fig. (11)
Fig. (11)
TEM image of glipizide loaded rs 100 optimized batch.
See this image and copyright information in PMC

References

    1. Dora C.P., Singh S.K., Kumar S., Datusalia A.K., Deep A. Development and characterization of nanoparticles of glibenclamide by solvent displacement method. Acta Pol Pharm Drug Res. 2010;67(3):283–290. - PubMed
    1. Baily C.J. Potential new treatments for type two diabetes. Trends Pharmacol. Sci. 2000;21:259–265. - PubMed
    1. Harlay C.R. Glipizide GRTS has advantages over other second generation sulfonylurea. Clin. Drug Investig. 2002;22:575–584.
    1. Hesieh S.H., Lin J.D., Chang H.Y., Ho Ch., Liou M.J. Sustained release versus immediate release glipizide for the treatment of diabetes mellitus in Chinese patients: a randomized, double blind, double dummy, parallel group, 12 week clinical study. Clin. Ther. 2006;28:1318–1326. - PubMed
    1. Venkateswarlu K., Shanthi A. Formulation and evaluation of sustained release glipizide matrix. IOSR J Pharm Biol Sci. 2012;2(5):17–23.