Niosomes and polymeric chitosan based vesicles bearing transferrin and glucose ligands for drug targeting.

TitleNiosomes and polymeric chitosan based vesicles bearing transferrin and glucose ligands for drug targeting.
Publication TypeJournal Article
Year of Publication2000
AuthorsDufès C, Schätzlein AG, Tetley L, Gray AI, Watson DG, Olivier JC, Couet W, Uchegbu IF
JournalPharm Res
Date Published2000 Oct
KeywordsCarcinoma, Squamous Cell, Chitin, Chitosan, Concanavalin A, Dextrans, Drug Carriers, Drug Delivery Systems, Fluorescein-5-isothiocyanate, Glucose, Glycolipids, Gold, Humans, Ligands, Surface-Active Agents, Transferrin, Tumor Cells, Cultured

PURPOSE: 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.

Alternate JournalPharm. Res.
PubMed ID11145231