Dataset Information

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

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 L?, sub-L? and L?' 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.

SUBMITTER: Polchi A

PROVIDER: S-EPMC5302501 | biostudies-literature | 2016 May

REPOSITORIES: biostudies-literature

ACCESS DATA

Publications

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

Polchi Alice A Magini Alessandro A Mazuryk Jarosław J Tancini Brunella B Gapiński Jacek J Patkowski Adam A Giovagnoli Stefano S Emiliani Carla C

Nanomaterials (Basel, Switzerland) 20160509 5

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 d ...[more]

PMID: 28335215

Similar Datasets

Project description:Cymbopogon citratus (DC) stapf. (Gramineae) is a herb known worldwide as lemongrass. The oil obtained, i.e., lemongrass oil has emerged as one among the most relevant natural oils in the pharmaceutical industry owing to its extensive pharmacological and therapeutic benefits including antioxidant, antimicrobial, antiviral and anticancer properties. However, its usage in novel formulations is constrained because of its instability and volatility. To address these concerns, the present study aims to formulate lemongrass-loaded SLN (LGSLN) using hot water titration technique. In the Smix, Tween 80 was selected as a surfactant component, while ethanol was taken as a co-surfactant. Different ratios of Smix (1:1, 1:2, 1:3, 2:1 and 3:1) were utilized to formulate LG-loaded SLN. The results indicated the fact that the LGSLN formulation (abbreviated as LGSLN1), containing lipid phase 10% w/w (i.e., LG 3.33% and SA 6.67%), Tween 80 (20% w/w), ethanol (20% w/w) and distilled water (50% w/w), revealed suitable nanometric size (142.3 ± 5.96 nm) with a high zeta potential value (- 29.12 ± 1.7 mV) and a high entrapment efficiency (77.02 ± 8.12%). A rapid drug release (71.65 ± 5.33%) was observed for LGSLN1 in a time span of 24 h. Additionally, the highest values for steady-state flux (Jss; 0.6133 ± 0.0361 mg/cm2/h), permeability coefficient (Kp; 0.4573 ± 0.0141 (cm/h) × 102) and enhancement ratio (Er; 13.50) was also conferred by LGSLN1. Based on in vitro study results, the developed SLN appeared as a potential carrier for enhanced topical administration of lemongrass oil. The observed results also indicated the fact that the phyto-cosmeceutical prospective of the nanolipidic carrier for topical administration of lemongrass oil utilizing pharmaceutically acceptable components can be explored further for widespread clinical applicability.Supplementary informationThe online version contains supplementary material available at 10.1007/s13205-023-03726-5.

Dataset Information

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

Publications

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

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Tweets