Absorption Enhancing Effect of Cyclodextrins on Intranasally Administered Insulin in Rats |
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Authors: | Merkus Frans W. H. M. Verhoef J. Coos Romeijn Stefan G. Schipper Nicolaas G. M. |
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Affiliation: | (1) Center for Bio-Pharmaceutical Sciences, Subdivision of Pharmaceutical Technology and Biopharmaceutics, Leiden University, P.O. Box 9502, 2300 RA Leiden, The Netherlands |
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Abstract: | The absorption enhancing effect of -, -, and -cyclodextrin (CD), dimethyl- -cyclodextrin (DM CD), and hydroxypropyl- -cyclodextrin (HP CD) on intranasally administered insulin was investigated in rats. Coadministration of 5% (w/v) DM CD to the insulin solution resulted in a high bioavailability, 108.9 ± 36.4% (mean ± SD, n = 6), compared to i.v. administration, and a strong decrease in blood glucose levels, to 25% of their initial values. Coadministration of 5% -CD gave rise to an insulin bioavailability of 27.7 ± 11.5% (mean ± SD, n = 6) and a decrease in blood glucose to 50% of its initial value. The rate of insulin absorption and the concomitant hypoglycemic response were delayed for the -CD-containing solution as compared to the DM CD preparation. The other CDs, HP CD (5%), -CD (1.8%), and -CD (5%), did not have significant effects on nasal insulin absorption. DM CD at a concentration of 5% (w/v) induces ciliostasis as measured on chicken embryo tracheal tissue in vitro, but this effect is reversible. In conclusion, DM CD is a potent enhancer of nasal insulin absorption in rats. |
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Keywords: | cyclodextrins insulin nasal administration rats ciliary movement |
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