Positively-charged, porous, polysaccharide nanoparticles loaded with anionic molecules behave as 'stealth' cationic nanocarriers

载有阴离子分子的带正电、多孔、多糖纳米粒子可充当“隐形”阳离子纳米载体

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作者:Archibald Paillard, Catherine Passirani, Patrick Saulnier, Maya Kroubi, Emmanuel Garcion, Jean-Pierre Benoît, Didier Betbeder

Conclusion

These nanoparticles are able to absorb large amounts of phospholipids or proteins without change in their size or zeta potential. Complement studies showed that stealth behaviour is observed when they are loaded and saturated either with anionic phospholipid or proteins.

Methods

NP(+)s were characterised in terms of size, zeta potential (zeta) and static light scattering (SLS). Complement consumption was assessed in normal human serum (NHS) by measuring the residual haemolytic capacity of the complement system.

Purpose

Stealth nanoparticles are generally obtained after modifying their surface with hydrophilic polymers, such as PEG. In this study, we analysed the effect of a phospholipid (DG) or protein (BSA) inclusion in porous cationic polysaccharide (NP(+)) on their physico-chemical structure and the effect on complement activation.

Results

DG loading did not change their size or zeta, whereas progressive BSA loading lightly decreased their zeta. An electrophoretic mobility analysis study showed the presence of two differently-charged sublayers at the NP(+) surface which are not affected by DG loading. Complement system activation, studied via a CH50 test, was suppressed by DG or BSA loading. We also demonstrated that NP(+)s could be loaded by a polyanionic molecule, such as BSA, after their preliminary filling by a hydrophobic molecule, such as DG.

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