title: Comparative receptor based brain delivery of tramadol-loaded poly(lactic-co-glycolic acid) nanoparticles.
abstract: Receptor mediated endocytosis or transcytosis has been reported for drug delivery across Blood-brain barrier (BBB) and hence, the aim of the present investigations was to prepare and compare brain targeting efficiency of tramadol-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles surface modified with transferrin (Tf) and lactoferrin (Lf). Nanoparticles of tramadol were prepared using nanoprecipitation technique and surface conjugated with Tf and Lf using epoxy linker. Prepared nanoparticles were characterized for their size, surface charge, drug entrapment, transmission electron microscopy and in vitro drug release. The surface density of Tf and Lf was estimated by protein estimation. The drug distribution in blood, brain and other tissues was studied in mice after intravenous administration. Tf and Lf anchored nanoparticles exhibit enhanced uptake with 2.38 and 3.85 folds higher targeting respectively in the brain when compared with unconjugated nanoparticles. The brain targeting observed for Lf anchored PLGA nanoparticles (Lf-TMD-PLGA-NP) was 1.62 folds that of Tf anchored PLGA nanoparticles (Tf-TMD-PLGA-NP). Hence, the study revealed Tf and specially Lf as promising ligand for enhanced brain deposition of tramadol.
authors.affiliation: Faculty of Technology and Engineering, Drug Delivery Laboratory, TIFAC Centre of Relevance and Excellence in NDDS, Pharmacy Department, The Maharaja Sayajirao University of Baroda, Vadodara 390002, India.
authors.forename: Jigar
authors.initials: J
authors.lastname: Lalani
authors.forename: Yogesh
authors.initials: Y
authors.lastname: Raichandani
authors.forename: Rashi
authors.initials: R
authors.lastname: Mathur
authors.forename: Manisha
authors.initials: M
authors.lastname: Lalan
authors.forename: Krishna
authors.initials: K
authors.lastname: Chutani
authors.forename: Anil Kumar
authors.initials: AK
authors.lastname: Mishra
authors.forename: Ambikanandan
authors.initials: A
authors.lastname: Misra
mesh_terms: D000818:Animals; D001812:Blood-Brain Barrier / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D002352:Carrier Proteins / Q000737:chemistry; D003102:Colloids / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D004705:Endocytosis; D019344:Lactic Acid / Q000008:administration & dosage*; D051379:Mice; D050997:Nanomedicine / Q000379:methods; D053758:Nanoparticles / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000008:administration & dosage*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D013499:Surface Properties; D013997:Time Factors; D014018:Tissue Distribution; D014147:Tramadol / Q000008:administration & dosage*
chemical_list: D002352:Carrier Proteins; D003102:Colloids; D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D014147:Tramadol