Abstract
A challenge regarding the design of nanocarriers for drug delivery is to prevent their recognition by the immune system. To improve the blood residence time and prevent their capture by organs, nanoparticles can be designed with stealth properties using polymeric coating. In this study, we focused on the influence of surface modification with polyethylene glycol and/or mannose on the stealth behavior of porous silicon nanoparticles (pSiNP, ~200 nm). In vivo biodistribution of pSiNPs formulations were evaluated in mice 5 h after intravenous injection. Results indicated that the distribution in the organs was surface functionalization-dependent. Pristine pSiNPs and PEGylated pSiNPs were distributed mainly in the liver and spleen, while mannose-functionalized pSiNPs escaped capture by the spleen, and had higher blood retention. The most efficient stealth behavior was observed with PEGylated pSiNPs anchored with mannose that were the most excreted in urine at 5 h. The biodegradation kinetics evaluated in vitro were in agreement with these in vivo observations. The biocompatibility of the pristine and functionalized pSiNPs was confirmed in vitro on human cell lines and in vivo by cytotoxic and systemic inflammation investigations, respectively. With their biocompatibility, biodegradability, and stealth properties, the pSiNPs functionalized with mannose and PEG show promising potential for biomedical applications.
Highlights
The emergence of nanomedicine has opened up opportunities for the development of more efficient anti-cancer agents that induce fewer side effects
We focused on the influence of surface modification with polyethylene glycol and/or mannose on the stealth behavior of porous silicon nanoparticles
The Bloch decay and cross-polarization magic angle spinning (CP-MAS) pulse sequences were used for the collection of 29Si nuclear magnetic resonance (NMR) (Figure S2)
Summary
The emergence of nanomedicine has opened up opportunities for the development of more efficient anti-cancer agents that induce fewer side effects. With respect to NPs’ clearance by the MPS, the liver and the spleen are the most active organs because of phagocytic cells as macrophages that act by surface opsonization [25] and generally express similar membrane receptors to those of tumors [26]. Given other constraints, such as the heterogeneities of tumors in terms of enhanced permeability and retention (EPR) and the multifactor impact such as electrolytes, proteins and lipids onto colloidal stability of nanocarriers, less than 10% of the total administered drug dose reaches the tumor [2]. There is a need to develop stealth nanocarriers with reduced uptake by the MPS and optimized for the EPR effect
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