title: Targeted brain delivery of AZT via transferrin anchored pegylated albumin nanoparticles.
abstract: Hydrophilic drugs/peptides have poor cross Blood-brain permeability. Various drug delivery systems with diverse surfacial characteristics have been reported for effective translocation of drugs across Blood-brain barrier. In present investigation, the potential of engineered albumin nanoparticles was evaluated for brain specific delivery after intravenous administration. Long circulatory PEGylated albumin nanoparticles encapsulating water-soluble antiviral drug azidothymidine (AZT) were prepared by ultra-emulsification method using chemical cross-linking by glutaraldehyde. Surface of the PEGylated nanoparticles was modified by anchoring transferrin as a ligand for brain targeting. Nanoparticles were characterized for their size, polydispersity, surfacial charge, drug loading and in vitro drug release. Fluorescence studies revealed the enhanced uptake of transferrin-anchored nanoparticles in the brain tissues when compared with unmodified nanoparticles. In vivo evaluation was carried out on albino rats to evaluate tissue distribution of engineered nanoparticles after intravenous administration. A significant ((*)P < 0.01) enhancement of brain localization of AZT was observed for transferrin anchored pegylated albumin nanopariticles (Tf-PEG-NPs). Hence, the specific role of transferrin ligand on nanoparticles for brain targeting was confirmed.
authors.affiliation: Dr Hari Singh Gour Vishvavidyalaya, Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Sagar, (M.P.), 470 002, India.
authors.forename: Vivek
authors.initials: V
authors.lastname: Mishra
authors.forename: Sunil
authors.initials: S
authors.lastname: Mahor
authors.forename: Amit
authors.initials: A
authors.lastname: Rawat
authors.forename: Prem N
authors.initials: PN
authors.lastname: Gupta
authors.forename: Praveen
authors.initials: P
authors.lastname: Dubey
authors.forename: Kapil
authors.initials: K
authors.lastname: Khatri
authors.forename: Suresh P
authors.initials: SP
authors.lastname: Vyas
mesh_terms: D000212:Acyclovir / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000269:Adhesives; D000278:Administration, Buccal; D000465:Algorithms; D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004058:Diffusion; D004285:Dogs; D006863:Hydrogen-Ion Concentration; D015233:Models, Statistical; D009061:Mouth Mucosa / Q000378:metabolism; D012995:Solubility; D013607:Tablets
chemical_list: D000269:Adhesives; D000998:Antiviral Agents; D003692:Delayed-Action Preparations; D013607:Tablets; D000212:Acyclovir