title: Formulation and evaluation of nano based drug delivery system for the buccal delivery of acyclovir.
abstract: Oral bioavailability of acyclovir is limited, primarily because of low permeability across the gastrointestinal membrane. The purpose of this study is the prospective evaluation of buccal films impregnated with acyclovir loaded nanospheres as a drug delivery system to improve systemic bioavailability. Acyclovir polymeric nanospheres were prepared by double emulsion solvent evaporation technique. Nanospheres were embedded into buccoadhesive films (A1-A4) comprising of different concentrations of polymers (Eudragit RL 100, HPMC K15 and carbopol 974P). Films were characterized for physico-mechanical properties, mucoadhesive strength, hydration, drug release and ex vivo permeation. In vivo studies were carried out on rabbits to assess the pharmacokinetic profile of buccal film (A3) as compared to oral therapy. The prepared films demonstrated excellent physical properties, adequate hydration and buccoadhesive strength. In vitro drug release data inferred that the drug release was dependent on the composition of film. Ex vivo permeation studies indicated greater flux in film A3. In vivo studies revealed a significant enhancement in absorption of acyclovir (P<0.0001) with Cmax (~3 folds) and AUC0-α (~8 folds, P<0.0001) when compared to oral dosing. Moreover, the extended Tmax value (6h) signifies the potential of the prepared film to prolong acyclovir delivery. Given the promising results, the study concludes that the developed buccal film (A3) impregnated with acyclovir loaded nanospheres could be a promising approach for effective delivery of acyclovir.
authors.affiliation: Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia. Electronic address: baldhubiab@kfu.edu.sa.
authors.forename: Bandar E
authors.initials: BE
authors.lastname: Al-Dhubiab
authors.affiliation: Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia.
authors.forename: Anroop B
authors.initials: AB
authors.lastname: Nair
authors.affiliation: Swift School of Pharmacy, Village-Ghaggar Sarai, Rajpura, Patiala, Punjab, India.
authors.forename: Rachna
authors.initials: R
authors.lastname: Kumria
authors.affiliation: Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia.
authors.forename: Mahesh
authors.initials: M
authors.lastname: Attimarad
authors.affiliation: Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia.
authors.forename: Sree
authors.initials: S
authors.lastname: Harsha
mesh_terms: D000212:Acyclovir / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001682:Biological Availability; D002610:Cheek; D016503:Drug Delivery Systems; D008297:Male; D036103:Nanotechnology; D011817:Rabbits
chemical_list: D000998:Antiviral Agents; D000212:Acyclovir
keywords: Acyclovir; Biodegradable polymers; Buccal; Film; In vivo; Nanospheres