Investigations on Alternate Approach to Target Mannose Receptors on Macrophages using 4-Sulfated N-Acetyl Galactosamine more Efficiently as Compared to Mannose Decorated Liposomes: an Application in Drug Delivery

Abstract

In the present study the targeting potential of two different ligands i.e palmitoyl mannose (Man-Lip) and 4-SO4GalNAc (Sulf-Lip) to resident macrophages have been investigated after having decorated on the surface of Amphotericin B (AmB) loaded liposomes. In case of Sulf-Lip, the 4-SO4GalNAc was adsorbed through electrostatic interaction on cationic liposomes, which was confirmed by change in zeta potential from +48.2 ± 3.7 mV for Lip to +12.2 ± 1.3 mV for Sulf-Lip. The mean particle size of Sulf-Lip and Man-Lip was found to be 139.4 ± 7.4 nm and 147.4 ± 8.6 nm respectively. Flow cytometric data reveals enhanced uptake of Sulf-Lip in both J774 and RAW cell lines as compared to Man-Lip. Intracellular localization studies indicate that the fluorescence intensity of Sulf-Lip was much higher as compared to Man-Lip and Lip formulations. Sulf-Lip and Man-Lip showed significantly higher localization of AmB at all time points compared to Lip (P<0.05) after i.v. administration. The studies provides evidences that 4-SO4GalNAc possess promising feature for targeting resident macrophages and its application in the conditions of leishmaniasis is in offing.