Study of isopropyl myristate microemulsion systems containing cyclodextrins to improve the solubility of 2 model hydrophobic drugs |
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Authors: | Indranil Nandi Mohammad Bari Hemant Joshi |
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Institution: | (1) Geneva Pharmaceutical Technology Corp, 08810 Dayton, NJ;(2) Forest Laboratories Inc, 11096 Inwood, NY;(3) Barr Laboratories, 10970 Pomona, NY |
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Abstract: | The objectives of this project were to evaluate the effect of alkanols and cyclodextrins on the phase behavior of an isopropyl
myristate microemulsion system and to examine the solubility of model drugs. Triangular phase diagrams were developed for
the microemulsion systems using the water titration method, and the solubility values of progesterone and indomethacin were
determined using a conventional shake-flask method. The water assimilation capacities were determined to evaluate the effective
microemulsion formation in different systems. The alkanols showed higher microemulsion formation rates at higher concentrations.
A correlation between the carbon numbers of the alkanol and water assimilation capacity in the microemulsions studied was
observed; isobutanol and isopentanol produced the best results. The addition of cyclodextrins showed no effect or had a negative
effect on the microemulsion formation based on the type of cyclodextrin used. Isopropyl myristate-based microemulsion systems
alone could increase the solubility values of progesterone and indomethacin up to 3300-fold and 500-fold, respectively, compared
to those in water. However, the addition of cyclodextrins to the microemulsion systems did not show a synergistic effect in
increasing the solubility values of the model drugs. In conclusion, microemulsion systems improve the solubility of progesterone
and indomethacin. But the two types of cyclodextrins studied affected isopropyl myristatebased microemulsion systems negatively
and did not improve the solubilization of 2 model drugs. |
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Keywords: | phase diagram microemulsion solubilization cyclodextrin surfactant progesterone indomethacin |
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