Stearic acid based, systematically designed oral lipid nanoparticles for enhanced brain delivery of dimethyl fumarate

Paliperidone is an antipsychotic drug having poor water solubility and bioavailability. Solid lipid nanoparticles of stearic acid loaded with paliperidone were prepared to enhance the bioavailability.

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Effect of pH and electrolytes on the colloidal stability of stearic acid–based lipid nanoparticles

Journal of Nanoparticle Research ◽

10.1007/s11051-018-4425-x ◽

2018 ◽

Vol 20 (12) ◽

Cited By ~ 3

Author(s):

Alexander F. Ife ◽

Ian H. Harding ◽

Rohan M. Shah ◽

Enzo A. Palombo ◽

Daniel S. Eldridge

Keyword(s):

Stearic Acid ◽

Colloidal Stability ◽

Lipid Nanoparticles ◽

Effect Of Ph

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Inhalation of Dimethyl Fumarate-encapsulated solid lipid nanoparticles attenuate clinical signs of Experimental Autoimmune Encephalomyelitis and pulmonary inflammatory dysfunction in mice

Clinical Science ◽

10.1042/cs20210792 ◽

2021 ◽

Author(s):

Bárbara Fernandes Pinto ◽

Lorena Natasha Brito Ribeiro ◽

Gisela Bevilacqua Rolfsen Ferreira da Silva ◽

Camila Simões Freitas ◽

Lucas Kraemer ◽

...

Keyword(s):

Spinal Cord ◽

Experimental Autoimmune Encephalomyelitis ◽

Solid Lipid Nanoparticles ◽

Clinical Signs ◽

Dimethyl Fumarate ◽

Lipid Nanoparticles ◽

Oral Drug ◽

Autoimmune Encephalomyelitis ◽

Solid Lipid ◽

Experimental Autoimmune

Rationale: The FDA approved Dimethyl Fumarate (DMF) as an oral drug for Multiple Sclerosis treatment based on its immunomodulatory activities. However, it also caused severe adverse effects mainly related to the gastrointestinal system. Objective: Investigated the potential effects of solid lipid nanoparticles (SLN) containing DMF, administered by inhalation on the clinical signs, central nervous system (CNS) inflammatory response, and lung function changes in mice with experimental autoimmune encephalomyelitis (EAE). Materials and Methods: EAE was induced using MOG35-55 peptide in female C57BL/6J mice and were treated via inhalation with DMF-encapsulated SLN (CTRL/SLN/DMF and EAE/SLN/DMF), empty SLN (CTRL/SLN and EAE/SLN), or saline solution (CTRL/saline and EAE/saline), every 72 hours during 21 days. Results: After 21 days post-induction, EAE mice treated with DMF-loaded SLN, when compared to EAE/saline and EAE/SLN, showed decreased clinical score and weight loss, reduction in brain and spinal cord injury and inflammation, also related to the increased influx of Foxp3+ cells into the spinal cord and lung tissues. Moreover, our data revealed that EAE mice showed signs of respiratory disease, marked by increased vascular permeability, leukocyte influx, production of TNF-α and IL-17, perivascular and peribronchial inflammation, with pulmonary mechanical dysfunction associated with loss of respiratory volumes and elasticity, which DMF-encapsulated reverted in SLN nebulization. Conclusion: Our study suggests that inhalation of DMF-encapsulated SLN is an effective therapeutic protocol that reduces not only the CNS inflammatory process and disability progression, characteristic of EAE disease, but also protects mice from lung inflammation and pulmonary dysfunction.

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Solid lipid nanoparticles for nose to brain delivery of haloperidol: in vitro drug release and pharmacokinetics evaluation

Acta Pharmaceutica Sinica B ◽

10.1016/j.apsb.2014.10.005 ◽

2014 ◽

Vol 4 (6) ◽

pp. 454-463 ◽

Cited By ~ 49

Author(s):

Mohd Yasir ◽

Udai Vir Singh Sara

Keyword(s):

Drug Release ◽

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Brain Delivery ◽

In Vitro Drug Release ◽

Solid Lipid

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Lipid Nanoparticles Improve the Uptake of α-Asarone Into the Brain Parenchyma: Formulation, Characterization, In Vivo Pharmacokinetics, and Brain Delivery

AAPS PharmSciTech ◽

10.1208/s12249-020-01832-8 ◽

2020 ◽

Vol 21 (8) ◽

Author(s):

Prakash Ramalingam ◽

Palanivel Ganesan ◽

D. S. Prabakaran ◽

Pardeep K. Gupta ◽

Sriramakamal Jonnalagadda ◽

...

Keyword(s):

Lipid Nanoparticles ◽

Brain Parenchyma ◽

Brain Delivery ◽

The Brain ◽

In Vivo Pharmacokinetics

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Stearic Acid, Beeswax and Carnauba Wax as Green Raw Materials for the Loading of Carvacrol into Nanostructured Lipid Carriers

Applied Sciences ◽

10.3390/app10186267 ◽

2020 ◽

Vol 10 (18) ◽

pp. 6267

Author(s):

Juliana G. Galvão ◽

Raquel L. Santos ◽

Ana Amélia M. Lira ◽

Renata Kaminski ◽

Victor H. Sarmento ◽

...

Keyword(s):

Stearic Acid ◽

Essential Oils ◽

Antioxidant Activities ◽

Polarized Light ◽

Lipid Nanoparticles ◽

Nanostructured Lipid Carriers ◽

Chemical Degradation ◽

Thymus Vulgaris ◽

Scanning Calorimetry ◽

Carnauba Wax

The use of lipid nanoparticles as drug delivery systems has been growing over recent decades. Their biodegradable and biocompatible profile, capacity to prevent chemical degradation of loaded drugs/actives and controlled release for several administration routes are some of their advantages. Lipid nanoparticles are of particular interest for the loading of lipophilic compounds, as happens with essential oils. Several interesting properties, e.g., anti-microbial, antitumoral and antioxidant activities, are attributed to carvacrol, a monoterpenoid phenol present in the composition of essential oils of several species, including Origanum vulgare, Thymus vulgaris, Nigellasativa and Origanum majorana. As these essential oils have been proposed as the liquid lipid in the composition of nanostructured lipid carriers (NLCs), we aimed at evaluating the influence of carvacrol on the crystallinity profile of solid lipids commonly in use in the production of NLCs. Different ratios of solid lipid (stearic acid, beeswax or carnauba wax) and carvacrol were prepared, which were then subjected to thermal treatment to mimic the production of NLCs. The obtained binary mixtures were then characterized by thermogravimetry (TG), differential scanning calorimetry (DSC), small angle X-ray scattering (SAXS) and polarized light microscopy (PLM). The increased concentration of monoterpenoid in the mixtures resulted in an increase in the mass loss recorded by TG, together with a shift of the melting point recorded by DSC to lower temperatures, and the decrease in the enthalpy in comparison to the bulk solid lipids. The miscibility of carvacrol with the melted solid lipids was also confirmed by DSC in the tested concentration range. The increase in carvacrol content in the mixtures resulted in a decrease in the crystallinity of the solid bulks, as shown by SAXS and PLM. The decrease in the crystallinity of lipid matrices is postulated as an advantage to increase the loading capacity of these carriers. Carvacrol may thus be further exploited as liquid lipid in the composition of green NLCs for a range of pharmaceutical applications.

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