Effect of isopropyl myristic acid ester on the physical characteristics and in vitro release of etoposide from PLGA microspheres |
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Authors: | Matthew J Schaefer Jagdish Singh |
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Institution: | (1) Department of Pharmaceutical Sciences, College of Pharmacy, North Dakota State University, 58105 Fargo, ND |
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Abstract: | The purpose of this paper was to study the effect of the isopropyl myristic acid ester (IPM) on the physicochemical characteristics
of etoposide-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres-specifically, the effects on the size and drug loading
of the microspheres, the polymer matrix and surface morphology, and the release of etoposide from the microspheres. The experiment
was structured to examine 2 IPM concentrations (25% and 50%) and 1 control (no IPM) at 2 different etoposide-loading percentages
(10% and 5%). The microspheres were prepared using a single-emulsion solvent-extraction procedure. Samples from each batch
of microspheres were then analyzed for size distribution. drug-loading efficiency, surface characteristics, in vitro release,
and in vitro microsphere degradation. The incorporation of 50% IPM significantly increased (P<05) the size of the microspheres when compared with the control and 25% IPM microspheres. However, incorporation of 25% or
50% IPM did not change (P>.05) the drug-loading efficiency in comparison with the microspheres prepared without IPM. The microspheres containing 50%
IPM were shown to significantly increase (P<.05) the release of etoposide from the microspheres at both etoposide concentrations. The microspheres prepared incorporating
25% IPM and 5% etoposide increased the in vitro release (P<.05) in comparison with the microspheres prepared without IPM. The 5% etoposide-PLGA microspheres showed a smooth, nonporous
surface that changed to a dimpled. nonporous surface after addition of 25% IPM. During the in vitro degradation study, the
IPM-containing microspheres slowly became porous but retained their structural integrity throughout the experiment. |
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Keywords: | Etoposide PLGA microspheres Isopropyl myristic acid ester In vitro release Scanning electron microscopy |
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