A sustained release dosage form of acyclovir for buccal application: An experimental study in dogs

Abstract

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.

Canine Reproductive, Respiratory, and Ocular Diseases due to Canine Herpesvirus

“…59 Acyclovir is bioavailable when administered orally to dogs and is widely distributed within tissues; however, target plasma concentrations and effective dosages for CHV infection are currently unknown. [57][58][59] Acyclovir toxicosis resultant from accidental ingestion is reported in dogs with dosages as low as 40 mg/kg and the routine clinical use of this, and other systemic antiviral medications, in dogs for CHV infection requires further investigation of safety and efficacy. 60 The canine pharmacokinetics of newer-generation antiherpesviral drugs, including famciclovir, are reported.…”

Mucoadhesive Polymeric Films of Acyclovir Proniosomes for Buccal Administration

“…Several studies have been reported wherein acyclovir has been formulated as buccal tablets or films [8,9]. However, the mucoadhesive buccal tablets of acyclovir currently in the market have been approved for the topical or local delivery of the drug in the oral cavity for the treatment of herpes labialis and is expected to be minimally absorbed through the oral mucosa.…”