Acyclovir is an
antiviral agent and it has been particularly used for the treatment of
herpes simplex infections. The treatment of
infection in the oral cavity is often difficult, because of insufficient
drug concentration in saliva when
acyclovir is administered via the oral route in conventional
tablet form for systemic uptake. Therefore, it was aimed to prepare a
tablet for
buccal administration and to investigate its effectiveness by performing in vitro and in vivo experiments.The solubility (1.559-4.584) and octanol/water partition coefficients ( - 2.176 to - 1.625) of the
acyclovir were investigated at different pH conditions. A series of
tablet formulations were prepared for buccal application and their dissolution properties were determined in
artificial saliva medium. The effect of
tablet ingredients on the release rate and mucoadhesion force was investigated. The dissolution properties of commercially available
acyclovir tablets were also determined in the artificial gastric juice. Franz type diffusion cells were used to determine
acyclovir penetration through buccal mucosa from prepared buccal
tablets. Selected buccal
tablets, commercial
tablets and intravenous
acyclovir solutions were administered to mongrel dogs and
drug levels in the blood determined by HPLC.A pharmacokinetic model for buccal application was also developed and blood concentrations were calculated theoretically and compared with the experimental results. Prepared buccal
tablets were found to be effective for the treatment of
viral infections locally within the oral cavity and also for systemic treatment.