In vitro percutaneous penetration of acyclovir from solvent systems and Carbopol 971-P hydrogels: influence of propylene glycol.
The mechanism underlying propylene glycol (PG) effects on acyclovir (ACV) penetration through human epidermis were studied. Solvent systems and Carbopol gels containing increasing percentage of PG (from 0% to 70%, w/w) were used. Viscosity studies of both vehicles were carried out to characterise the influence of rheological behaviour. In solvent systems skin permeation values of ACV increase as the concentration of PG increase yielding a maximum enhancement ratio (ER = 10) for 70% PG. The release rate of ACV from gels was determined. Higuchi's model was used to estimate the apparent diffusion coefficient of the drug. These values show a decrease as the content of PG in the vehicle increases; this effect could be attributed to the increase of the viscosity in the diffusional pathway. When gels are used skin permeation values of ACV were smaller than those of the solvent systems. This could be attributed to the network structure created by the polymer that increases the length of the diffusional pathway. The maximum ER (= 6.8) was for Carbopol gel containing 50% PG. Therefore, these gels can be considered candidates for further research to confirm their usefulness as delivery systems for ACV topical formulations.
Díez-Sales
O
O
Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Valencia, Spain. octavio.diez@uv.es
Garrigues
T M
TM
Herráez
J V
JV
Belda
R
R
Martín-Villodre
A
A
Herráez
M
M
D000180:Acrylic Resins; D000212:Acyclovir / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000328:Adult; D000465:Algorithms; D000998:Antiviral Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005079:Excipients; D005260:Female; D006801:Humans; D020100:Hydrogels; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D008875:Middle Aged; D011145:Polyvinyls; D011409:Propylene Glycols / Q000737:chemistry*; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility; D012997:Solvents; D013816:Thermodynamics; D014783:Viscosity
D000180:Acrylic Resins; D000998:Antiviral Agents; D005079:Excipients; D020100:Hydrogels; D011145:Polyvinyls; D011409:Propylene Glycols; D012997:Solvents; C006912:carboxypolymethylene; D000212:Acyclovir