Niosomes and polymeric chitosan based vesicles bearing transferrin and glucose ligands for drug targeting.
OBJECTIVE
To prepare polymeric vesicles and niosomes bearing glucose or transferrin ligands for drug targeting.


METHODS
A glucose-palmitoyl glycol chitosan (PGC) conjugate was synthesised and glucose-PGC polymeric vesicles prepared by sonication of glucose-PGC/cholesterol. N-palmitoylglucosamine (NPG) was synthesised and NPG niosomes also prepared by sonication of NPG/ sorbitan monostearate/ cholesterol/ cholesteryl poly-24-oxyethylene ether. These 2 glucose vesicles were incubated with colloidal concanavalin A gold (Con-A gold), washed and visualised by transmission electron microscopy (TEM). Transferrin was also conjugated to the surface of PGC vesicles and the uptake of these vesicles investigated in the A431 cell line (over expressing the transferrin receptor) by fluorescent activated cell sorter analysis.


RESULTS
TEM imaging confirmed the presence of glucose units on the surface of PGC polymeric vesicles and NPG niosomes. Transferrin was coupled to PGC vesicles at a level of 0.60+/-0.18 g of transferrin per g polymer. The proportion of FITC-dextran positive A431 cells was 42% (FITC-dextran solution), 74% (plain vesicles) and 90% (transferrin vesicles).


CONCLUSIONS
Glucose and transferrin bearing chitosan based vesicles and glucose niosomes have been prepared. Glucose bearing vesicles bind Con-A to their surface. Chitosan based vesicles are taken up by A431 cells and transferrin enhances this uptake.
Dufes
C
C
Department of Pharmaceutical Sciences, University of Strathclyde, Strathclyde Institute for Biomedical Sciences, Glasgow, United Kingdom.
Schätzlein
A G
AG
Tetley
L
L
Gray
A I
AI
Watson
D G
DG
Olivier
J C
JC
Couet
W
W
Uchegbu
I F
IF
D002294:Carcinoma, Squamous Cell / Q000378:metabolism; D002686:Chitin / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000737:chemistry / Q000378:metabolism; D048271:Chitosan; D003208:Concanavalin A / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D003911:Dextrans / Q000008:administration & dosage / Q000493:pharmacokinetics; D004337:Drug Carriers; D016503:Drug Delivery Systems; D016650:Fluorescein-5-isothiocyanate / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D005947:Glucose / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D006017:Glycolipids / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D006046:Gold / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D008024:Ligands; D013501:Surface-Active Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D014168:Transferrin / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D014407:Tumor Cells, Cultured
D003911:Dextrans; D004337:Drug Carriers; D006017:Glycolipids; D008024:Ligands; C000594385:N-palmitoylglucosamine; D013501:Surface-Active Agents; D014168:Transferrin; C015219:fluorescein isothiocyanate dextran; D003208:Concanavalin A; D002686:Chitin; D006046:Gold; D048271:Chitosan; D016650:Fluorescein-5-isothiocyanate; D005947:Glucose