In order to develop nasal powder preparations with higher bioavailability f
or peptide delivery, the effect of a combination of hydroxypropyl cellulose
(HPC) and microcrystalline cellulose (MCC) used as base materials and micr
oenvironment for the drugs in the preparations was examined. Significant en
hanced absorption of leuprolide, calcitonin and FITC-dextran was attained b
y the addition of a small amount of HPC to MCC. It is suggested that MCC wo
rks as an absorption enhancer by causing a locally high concentration of dr
ugs in the vicinity of the mucosa surface. On the other hand, HPC works to
increase retention of drugs on the nasal mucosa due to its gel-forming prop
erty. In comparison to the powder mixtures of MCC and HPC in which drugs we
re distributed to the MCC or HPC, selective distribution of drugs to MCC is
shown to be a critical factor for enhancing nasal absorption. These result
s showed that the microenvironment of drugs in the functional base material
could critically affect the nasal absorption of drugs. (C) 1999 Published
by Elsevier Science B.V. All rights reserved.