Views:0 Author:Site Editor Publish Time: 2021-02-04 Origin:Site
Nasal administration is suitable for drugs with high efficacy and low bioavailability. There are two absorption pathways in nasal mucosa: lipid channel through cells and water-based pore between cells. Therefore, generally speaking, drugs need to have certain lipophilicity to pass through the nasal mucosa; macromolecular drugs such as proteins and peptides are not fully absorbed in the nasal mucosa; the presence of enzymes in the nasal cavity will catalyze the degradation of some drugs with unstable enzymes.
The inclusion of cyclodextrin into the nasal cavity can increase the solubility of the drug, improve the enzyme stability of the drug, increase the permeability of nasal mucosa and promote the nasal absorption of protein and peptide drugs.
Among all the cyclodextrin derivatives, methylated cyclodextrin, such as DM-β-CD, is the most studied cyclodextrin in nasal drug delivery preparations, because it can greatly increase the permeability of nasal mucosa, followed by HP-β-CD, SBE-β-CD and so on.
The following research examples can well illustrate the effect of cyclodextrin on drug nasal mucosa absorption.
There are some shortcomings in the clinical application of buserelin acetate, such as biological instability, poor absorption through biofilm, rapid plasma clearance and so on. The absorption of buserelin acetate through rat nasal mucosa can be improved by the simultaneous administration of cyclodextrin derivatives. DM-β-CD is the most effective derivative, followed by Carboxy DM-β-CD with sustained-release absorption. This is mainly due to the fact that they affect the integrity of nasal mucosa and inhibit the proteolytic enzymes in nasal cavity.
The bioavailability of lutein was increased from 18% of the suspension to 58% of the inclusion compound. Compared with other absorption enhancers used in the nasal delivery system, the effect of DM-β-CD on the ciliary oscillation frequency was very mild.