AI Article Synopsis

  • The study investigates the effectiveness of two ligands, palmitoyl mannose (Man-Lip) and 4-SO(4)GalNAc (Sulf-Lip), in targeting resident macrophages with Amphotericin B (AmB) loaded liposomes.
  • Using electrostatic interactions to modify cationic liposomes, Sulf-Lip showed a notable change in zeta potential and higher fluorescence intensity in cell uptake compared to Man-Lip.
  • The results indicated that both ligands significantly enhanced AmB localization in macrophages after intravenous administration, suggesting Sulf-Lip could be particularly useful for treating conditions like leishmaniasis.

Article Abstract

Unlabelled: In this study the potential of 2 different ligands, i.e., palmitoyl mannose (Man-Lip) and 4-SO(4)GalNAc (Sulf-Lip) to target resident macrophages was investigated after surface decoration of Amphotericin B (AmB) loaded liposomes. In the case of Sulf-Lip, the 4-SO(4)GalNAc 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 reveal enhanced uptake of Sulf-Lip in both J774 and RAW cell lines in comparison with the uptake of Man-Lip. Intracellular localization studies indicate that the fluorescence intensity of Sulf-Lip was much higher in comparison with that of Man-Lip and Lip formulations. Sulf-Lip and Man-Lip showed significantly higher localization of AmB at all time points in comparison with Lip (P < 0.05) after intravenous (IV) administration. The studies provide evidence that 4-SO(4)GalNAc possesses a promising feature for targeting resident macrophages and its application in the conditions of leishmaniasis is in the offing.

From The Clinical Editor: This in vivo study compares two different ligands to deliver Amphotericin B l(AmB) loaded liposomes to resident macrophages. Targeted approaches showed significantly higher localization of AmB at all time points in comparison to non-targeted liposomes, and future applications in leishmaniasis are already under preparation.

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http://dx.doi.org/10.1016/j.nano.2011.07.002DOI Listing

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