Comparative permeability of some acyclovir derivatives through native mucus and crude mucin dispersions.
The permeability of some guanine derivatives (acyclovir [ACV], deoxyacyclovir [DCV], and their N-acetyl congeners) through native porcine mucus and crude porcine mucin dispersions (30% and 50% w/v) was investigated in two-compartment dialysis cells. High correlation between apparent permeability coefficients Papp of tested substances determined in these two models was observed, although the examined compounds permeated faster through the native mucus. It was also established that Papp values decrease with increasing hydrophilicity and molecular mass of the tested substances. Furthermore, the influence of some substances that affect mucus structure (cysteine, N-acetylcysteine [NCY], sodium taurocholate [ST], and sodium chloride) on the permeation rate of the examined compounds through mucus and mucin dispersions was examined. It was shown that the Papp values of guanine derivatives were generally lower after the addition of these substances to the native mucus and mucin dispersions, although the lowering effect was more pronounced in the case of native mucus.
Legen
University of Ljubljana, Faculty of Pharmacy, Slovenia.
Kristl
A
A
D000212:Acyclovir / Q000031:analogs & derivatives* / Q000737:chemistry*; D000465:Algorithms; D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry*; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D004058:Diffusion; D019793:Fluorescein / Q000737:chemistry; D006147:Guanine / Q000737:chemistry; D066298:In Vitro Techniques; D008954:Models, Biological; D009077:Mucins / Q000737:chemistry*; D009093:Mucus / Q000737:chemistry*; D010539:Permeability; D051381:Rats; D013552:Swine
D000998:Antiviral Agents; D009077:Mucins; D006147:Guanine; C041468:desciclovir; D019793:Fluorescein; D000212:Acyclovir