Brimonidine Tartrate–Eudragit Long-Acting Nanoparticles: Formulation, Optimization, In Vitro and In Vivo Evaluation
In the present study, an effort was made to design prolonged release Eudragit nanoparticles of brimonidine tartrate by double emulsion–solvent evaporation technique for the treatment of open-angle glaucoma. The effect of various formulation variables like initial drug amount, lecithin proportion, ph...
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Published in | AAPS PharmSciTech Vol. 12; no. 4; pp. 1087 - 1101 |
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Main Authors | , , |
Format | Journal Article |
Language | English |
Published |
Boston
Springer US
01.12.2011
|
Subjects | |
Online Access | Get full text |
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Summary: | In the present study, an effort was made to design prolonged release Eudragit nanoparticles of brimonidine tartrate by double emulsion–solvent evaporation technique for the treatment of open-angle glaucoma. The effect of various formulation variables like initial drug amount, lecithin proportion, phase volume and pH, secondary emulsifier and polymer proportion were studied. Various process variables like energy and duration of emulsification, lyophilization on the characteristics of nanoparticles and
in vitro
drug release profile were studied. The selected formulations were subjected to
in vivo
intraocular pressure-lowering efficacy studies by administering aqueous dispersion of nanoparticles into the lower cul de sac of glaucomatous rabbits. The prepared Eudragit-based nanoparticles were found to have narrow particle size range and improved drug loading. The investigated process and formulation variables found to have significant effect on the particle size, drug loading and entrapment efficiency, and
in vitro
drug release profile of nanoparticles. The selected formulations upon
in vivo
ocular irritability and tolerability tests were found to be well tolerated with no signs of irritation.
In vivo
pharmacodynamic efficacy studies revealed that the selected nanoparticle formulations significantly improved the therapy as area under the ∆IOP
vs
. time curve [AUC
(∆IOP
vs
.
t
)
] showed several fold increase in intensity and duration of intraocular pressure (IOP) decrease. All the selected nanoparticle formulations were found to prolong the drug release
in vitro
and prolong IOP reduction efficacy
in vivo
, thus rendering them as a potential carrier in developing improved drug delivery systems for the treatment of glaucoma. |
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Bibliography: | ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-1 content type line 23 |
ISSN: | 1530-9932 1530-9932 |
DOI: | 10.1208/s12249-011-9675-1 |