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

Christine Dufès, A.G. Schätzlein, L. Tetley, A.I. Gray, D.G. Watson, J.C. Olivier, W. Couet, I.F. Uchegbu

Research output: Contribution to journalArticle

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Abstract

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.
LanguageEnglish
Pages1250-1258
Number of pages9
JournalPharmaceutical Research
Volume17
Issue number10
DOIs
StatePublished - 2000

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Bearings (structural)
Chitosan
Drug Delivery Systems
Transferrin
Liposomes
Ligands
Glucose
Sonication
Transmission Electron Microscopy
Cholesterol
Transmission electron microscopy
Transferrin Receptors
Ether
palmitoyl glycol chitosan
Polymers
Cells

Keywords

  • polymeric vesicles
  • glucose vesicles
  • transferrin vesicles

Cite this

Dufès, C., Schätzlein, A. G., Tetley, L., Gray, A. I., Watson, D. G., Olivier, J. C., ... Uchegbu, I. F. (2000). Niosomes and polymeric chitosan based vesicles bearing transferrin and glucose ligands for drug targeting. Pharmaceutical Research, 17(10), 1250-1258. DOI: 10.1023/A:1026422915326
Dufès, Christine ; Schätzlein, A.G. ; Tetley, L. ; Gray, A.I. ; Watson, D.G. ; Olivier, J.C. ; Couet, W. ; Uchegbu, I.F./ Niosomes and polymeric chitosan based vesicles bearing transferrin and glucose ligands for drug targeting. In: Pharmaceutical Research. 2000 ; Vol. 17, No. 10. pp. 1250-1258
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abstract = "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.",
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Dufès, C, Schätzlein, AG, Tetley, L, Gray, AI, Watson, DG, Olivier, JC, Couet, W & Uchegbu, IF 2000, 'Niosomes and polymeric chitosan based vesicles bearing transferrin and glucose ligands for drug targeting' Pharmaceutical Research, vol. 17, no. 10, pp. 1250-1258. DOI: 10.1023/A:1026422915326

Niosomes and polymeric chitosan based vesicles bearing transferrin and glucose ligands for drug targeting. / Dufès, Christine; Schätzlein, A.G.; Tetley, L.; Gray, A.I.; Watson, D.G.; Olivier, J.C.; Couet, W.; Uchegbu, I.F.

In: Pharmaceutical Research, Vol. 17, No. 10, 2000, p. 1250-1258.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Niosomes and polymeric chitosan based vesicles bearing transferrin and glucose ligands for drug targeting

AU - Dufès,Christine

AU - Schätzlein,A.G.

AU - Tetley,L.

AU - Gray,A.I.

AU - Watson,D.G.

AU - Olivier,J.C.

AU - Couet,W.

AU - Uchegbu,I.F.

PY - 2000

Y1 - 2000

N2 - 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.

AB - 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.

KW - polymeric vesicles

KW - glucose vesicles

KW - transferrin vesicles

U2 - 10.1023/A:1026422915326

DO - 10.1023/A:1026422915326

M3 - Article

VL - 17

SP - 1250

EP - 1258

JO - Pharmaceutical Research

T2 - Pharmaceutical Research

JF - Pharmaceutical Research

SN - 0724-8741

IS - 10

ER -