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Nanomaterials 2016, 6(5), 87; doi:10.3390/nano6050087

Rapamycin Loaded Solid Lipid Nanoparticles as a New Tool to Deliver mTOR Inhibitors: Formulation and in Vitro Characterization

1
Department of Chemistry, Biology and Biotechnology, University of Perugia, Via del Giochetto, 06126 Perugia, Italy
2
NanoBioMedical Centre, Faculty of Physics, Adam Mickiewicz University in Poznań, 61614 Poznań, Poland
3
Molecular Biophysics Division, Faculty of Physics, Adam Mickiewicz University in Poznań, 61614 Poznań, Poland
4
Department of Pharmaceutical Sciences, University of Perugia, 06123 Perugia, Italy
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Academic Editor: Ilaria Armentano
Received: 29 January 2016 / Revised: 27 April 2016 / Accepted: 29 April 2016 / Published: 9 May 2016
(This article belongs to the Special Issue Nanomaterials for Tissue Engineering)
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Abstract

Recently, the use of mammalian target of rapamycin (mTOR) inhibitors, in particular rapamycin (Rp), has been suggested to improve the treatment of neurodegenerative diseases. However, as Rp is a strong immunosuppressant, specific delivery to the brain has been postulated to avoid systemic exposure. In this work, we fabricated new Rp loaded solid lipid nanoparticles (Rp-SLN) stabilized with polysorbate 80 (PS80), comparing two different methods and lipids. The formulations were characterized by differential scanning calorimetry (DSC), nuclear magnetic resonance (NMR), wide angle X-ray scattering (WAXS), cryo-transmission electron microscopy (cryo-TEM), dynamic light scattering (DLS) and particle tracking. In vitro release and short-term stability were assessed. Biological behavior of Rp-SLN was tested in SH-SY5Y neuroblastoma cells. The inhibition of mTOR complex 1 (mTORC1) was evaluated over time by a pulse-chase study compared to free Rp and Rp nanocrystals. Compritol Rp-SLN resulted more stable and possessing proper size and surface properties with respect to cetyl palmitate Rp-SLN. Rapamycin was entrapped in an amorphous form in the solid lipid matrix that showed partial crystallinity with stable Lβ, sub-Lα and Lβ′ arrangements. PS80 was stably anchored on particle surface. No drug release was observed over 24 h and Rp-SLN had a higher cell uptake and a more sustained effect over a week. The mTORC1 inhibition was higher with Rp-SLN. Overall, compritol Rp-SLN show suitable characteristics and stability to be considered for further investigation as Rp brain delivery system. View Full-Text
Keywords: rapamycin; solid lipid nanoparticles; drug delivery; formulation; SH-SY5Y neuroblastoma cells rapamycin; solid lipid nanoparticles; drug delivery; formulation; SH-SY5Y neuroblastoma cells
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MDPI and ACS Style

Polchi, A.; Magini, A.; Mazuryk, J.; Tancini, B.; Gapiński, J.; Patkowski, A.; Giovagnoli, S.; Emiliani, C. Rapamycin Loaded Solid Lipid Nanoparticles as a New Tool to Deliver mTOR Inhibitors: Formulation and in Vitro Characterization. Nanomaterials 2016, 6, 87.

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