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Evaluation of amphiphilic PEG derivatives as surface modifiers for the production of stealth liposomes

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Abstract

Some amphiphilic conjugates of amino- or carboxy-mPEG2000 or mPEG5000 with a series of lipoamino acids as a lipid anchor (PEG-LAA), recently synthetized as novel surface modifiers for drug nanocarriers, were used to decorate the surface of multilamellar liposomes (MLV). For comparison, MLV were also prepared using commercial PEG lipid derivatives (DSPE-PEG and PEG 40 monostearate), commonly used to produce stealth nanocarriers. Two experimental models were used to check the ability of the PEG-LAA conjugates to organize themselves on the surface of liposomes: an in vitro uptake study, using murine macrophage cultures, that confirmed the ability of PEG-LAA conjugates to hinder or retard the cellular internalization of the vesicles. Second, the measurement of the zeta potential values of negatively charged MLV produced with the various PEG-LAAs, which confirmed their shielding effect on the MLV surface charge, linearly to their molar concentration and as a function of the structures of PEG and LAA used.

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Acknowledgments

This study was in part supported by the University of Catania (Ricerca di Ateneo) and by the Italian Minister of University (PRIN2010-11 Project no. 2010H834LS).

Conflict of interest

No conflict of interest must be declared by all the authors.

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Authors and Affiliations

  1. Section of Pharmaceutical Technology, Department of Drug Sciences, University of Catania, viale A. Doria, 6, 95125, Catania, Italy

    Sarha Cupri, Teresa Musumeci & Rosario Pignatello

  2. Section of Physiology, Department of Bio-medical Sciences, University of Catania, viale A. Doria, 6, 95125, Catania, Italy

    Adriana C. E. Graziano, Silvia Caggia & Venera Cardile

Authors
  1. Sarha Cupri
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  2. Teresa Musumeci
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  3. Adriana C. E. Graziano
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  4. Silvia Caggia
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  5. Venera Cardile
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  6. Rosario Pignatello
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Correspondence to Rosario Pignatello.

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Cupri, S., Musumeci, T., Graziano, A.C.E. et al. Evaluation of amphiphilic PEG derivatives as surface modifiers for the production of stealth liposomes. Colloid Polym Sci 293, 1083–1092 (2015). https://doi.org/10.1007/s00396-014-3465-8

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  • DOI: https://doi.org/10.1007/s00396-014-3465-8

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