title: Design and development of multiple emulsion for enhancement of oral bioavailability of acyclovir.
abstract: The objective of this investigation was to design and develop water-in-oil-in-water type multiple emulsions (w/o/w emulsions) entrapping acyclovir for improving its oral bioavailability. Multiple emulsions (MEs) were prepared and optimized using Span-80 and Span-83 as lipophilic surfactant and Brij-35 as hydrophilic surfactant. The physio-chemical properties of the w/o/w emulsions - particle size, viscosity, phase separation (centrifugation test) and entrapment efficiency were measured and evaluated along with macroscopic and microscopic observations to confirm multiple nature, homogeneity and globule size. Stability study, in vitro and ex vivo release studies were performed followed by in vivo studies in rats. Stable w/o/w emulsions with a particle size of 33.098 ± 2.985 µm and 85.25 ± 4.865% entrapment efficiency were obtained. Stability studies showed that the concentration of lipophilic surfactant was very important for stability of MEs. Drug release from the prepared formulations showed initial rapid release followed by a much slower release. In vivo studies in rats indicated prolonged release and better oral bioavailability as compared to drug solution. The overall results of this study show the potential of the w/o/w emulsions as promising drug delivery systems for acyclovir.
authors.affiliation: Drug Delivery Research Laboratory, TIFAC Center of Relevance and Excellence in NDDS, Pharmacy Department, G. H. Patel Building, Donor's Plaza, The M. S. University of Baroda , Fatehgunj, Vadodara-390002, Gujarat , India.
authors.forename: Sumita
authors.initials: S
authors.lastname: Paul
authors.forename: Abhinesh
authors.initials: A
authors.lastname: Kumar
authors.forename: Pramod
authors.initials: P
authors.lastname: Yedurkar
authors.forename: Krutika
authors.initials: K
authors.lastname: Sawant
mesh_terms: D000212:Acyclovir / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D000284:Administration, Oral; D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D055598:Chemical Phenomena; D004337:Drug Carriers / Q000008:administration & dosage / Q000032:analysis / Q000737:chemistry / Q000493:pharmacokinetics*; D004339:Drug Compounding; D016503:Drug Delivery Systems; D004355:Drug Stability; D004356:Drug Storage; D004655:Emulsions; D005079:Excipients / Q000737:chemistry*; D006601:Hexoses / Q000737:chemistry; D057927:Hydrophobic and Hydrophilic Interactions; D008297:Male; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D051381:Rats; D013501:Surface-Active Agents / Q000737:chemistry*; D014783:Viscosity
chemical_list: D000998:Antiviral Agents; D004337:Drug Carriers; D004655:Emulsions; D005079:Excipients; D006601:Hexoses; D013501:Surface-Active Agents; C018665:sorbitan monooleate; C058854:sorbitan sesquioleate; D011092:Polyethylene Glycols; C515901:Brij 35; D000212:Acyclovir