Lipid nanoparticles for administration of poorly water soluble neuroactive drugs

Esposito, Elisabetta; Drechsler, Markus; Mariani, Paolo; Carducci, Federica; Servadio, Michela; Melancia, Francesca; Ratano, Patrizia; Campolongo, Patrizia; Trezza, Viviana; Cortesi, Rita; Nastruzzi, Claudio

doi:10.1007/s10544-017-0188-x

Cited by 23 publications

(22 citation statements)

References 41 publications

(34 reference statements)

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“…To enhance neuroprotective potentials of HE after acute seizures, utilizing nanodelivery systems can be considered, especially when the essential bioactive component of HE is established. There are two types of lipid nanoparticles called solid lipid nanoparticles and nanostructured lipid carriers, depending on the function of the lipids forming nanoparticle matrix [45]. By mixing lyotropic lipid, monoolein, with assorted emulsifiers and water, various types of liquid crystalline nanocarriers can be generated [46,47,48,49,50].…”

Section: Discussionmentioning

confidence: 99%

The Neuroprotective Effect of Hericium erinaceus Extracts in Mouse Hippocampus after Pilocarpine-Induced Status Epilepticus

Jang

Kim

Jeong

et al. 2019

IJMS

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Hericium erinaceus (HE), a culinary-medicinal mushroom, has shown therapeutic potential in many brain diseases. However, the role of HE in status epilepticus (SE)-mediated neuronal death and its underlying mechanisms remain unclear. We investigated the neuroprotective effects of HE using a pilocarpine-induced SE model. Male C57BL/6 mice received crude extracts of HE (60 mg/kg, 120 mg/kg, or 300 mg/kg, p.o.) for 21 d from 14 d before SE to 6 d after SE. At 7 d after SE, cresyl violet and immunohistochemistry of neuronal nuclei revealed improved hippocampal neuronal survival in animals treated with 60 mg/kg and 120 mg/kg of HE, whereas those treated with 300 mg/kg of HE showed similar neuronal death to that of vehicle-treated controls. While seizure-induced reactive gliosis, assessed by immunohistochemistry, was not altered by HE, the number of hippocampal cyclooxygenase 2 (COX2)-expressing cells was significantly reduced by 60 and 120 mg/kg of HE. Triple immunohistochemistry demonstrated no overlap of COX2 labeling with Ox42, in addition to a decrease in COX2/GFAP-co-immunoreactivity in the group treated with 60 mg/kg HE, suggesting that the reduction of COX2 by HE promotes neuroprotection after SE. Our findings highlight the potential application of HE for preventing neuronal death after seizures.

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Section: Discussionmentioning

confidence: 99%

The Neuroprotective Effect of Hericium erinaceus Extracts in Mouse Hippocampus after Pilocarpine-Induced Status Epilepticus

Jang

Kim

Jeong

et al. 2019

IJMS

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“…Lipid nanoparticles were prepared by a hot homogenization technique based on ultrasound treatment. In both cases the dispersing phase was an aqueous solution of poloxamer 188 (2.5% w/w) [37]. In the case of SLN the disperse phase was constituted of one solid lipid (i.e., tristearin, precirol, compritol or suppocire), while in the case of NLC, a mixture between one solid lipid and the liquid lipid caprylic/capric triglycerides (miglyol) (1:1 w/w ratio) was employed.…”

Section: Methodsmentioning

confidence: 99%

Lipid nanostructures for antioxidant delivery: a comparative preformulation study

Esposito¹,

Sguizzato²,

Drechsler³

et al. 2019

Beilstein J. Nanotechnol.

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This investigation is a study of new lipid nanoparticles for cutaneous antioxidant delivery. Several molecules, such as α-tocopherol and retinoic acid, have been shown to improve skin condition and even counteract the effects of exogenous stress factors such as smoking on skin aging. This work describes the design and development of lipid nanoparticles containing antioxidant agents (α-tocopherol or retinoic acid) to protect human skin against pollutants. Namely, solid lipid nanoparticles and nanostructured lipid carriers were prepared using different lipids (tristearin, compritol, precirol or suppocire) in the presence or absence of caprylic/capric triglycerides. The formulations were characterized by particle size analysis, cryogenic transmission electron microscopy, small-angle X-ray diffraction, encapsulation efficiency, preliminary stability, in vitro cytotoxicity and protection against cigarette smoke. Nanostructured lipid carriers were found to reduce agglomerate formation and provided better dimensional stability, as compared to solid lipid nanoparticles, suggesting their suitability for antioxidant loading. Based on the preformulation study, tristearin-based nanostructured lipid carriers loaded with α-tocopherol were selected for ex vivo studies since they displayed superior physico-chemical properties as compared to the other nanostructured lipid carriers compositions. Human skin explants were treated with α-tocopherol-loaded nanostructured lipid carriers and then exposed to cigarette smoke, and the protein levels of the stress-induced enzyme heme oxygenase were analyzed in skin homogenates. Interestingly, it was found that pretreatment with the nanoformulation resulted in significantly reduced heme oxygenase upregulation as compared to control samples, suggesting a protective effect provided by the nanoparticles.

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“…PEG chains are also able to increase residence time, thus another suitable material for nose to brain delivery could be different types of copolymers derivatized with PEG [74,75]. Lipid NPs obtained with tristearin in association with gliceryl monoolein were produced to load neuroactive drugs such as dimethylfumarate, retinyl palmitate, progesterone, and the endocannabinoid hydrolysis inhibitor URB597 [76]. Dimethyl fumarate was loaded in three different types of SLN for potential treatment of multiple sclerosis.…”

Section: “3n” Rule: Nasal Route Nanomedicine and Neurotherapymentioning

confidence: 99%

“…Dimethyl fumarate was loaded in three different types of SLN for potential treatment of multiple sclerosis. Esposito et al studied the biodistribution of polysorbate 80 treated SLN by fluorescent imaging after intraperitoneal or IN administration in mice [76]. Shah et al studied rivastigmine loaded SLN optimized by design of experiment (DoE) using different lipids (Apifil, Compritol glycerylmonostearate, stearic acid).…”

Section: “3n” Rule: Nasal Route Nanomedicine and Neurotherapymentioning

confidence: 99%

Epilepsy Disease and Nose-to-Brain Delivery of Polymeric Nanoparticles: An Overview

2019

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Epilepsy is the fourth most common global neurological problem, which can be considered a spectrum disorder because of its various causes, seizure types, its ability to vary in severity and the impact from person to person, as well as its range of co-existing conditions. The approaches to drug therapy of epilepsy are directed at the control of symptoms by chronic administration of antiepileptic drugs (AEDs). These AEDs are administered orally or intravenously but alternative routes of administration are needed to overcome some important limits. Intranasal (IN) administration represents an attractive route because it is possible to reach the brain bypassing the blood brain barrier while the drug avoids first-pass metabolism. It is possible to obtain an increase in patient compliance for the easy and non-invasive route of administration. This route, however, has some drawbacks such as mucociliary clearance and the small volume that can be administered, in fact, only drugs that are efficacious at low doses can be considered. The drug also needs excellent aqueous solubility or must be able to be formulated using solubilizing agents. The use of nanomedicine formulations able to encapsulate active molecules represents a good strategy to overcome several limitations of this route and of conventional drugs. The aim of this review is to discuss the innovative application of nanomedicine for epilepsy treatment using nose-to-brain delivery with particular attention focused on polymeric nanoparticles to load drugs.

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Lipid nanoparticles for administration of poorly water soluble neuroactive drugs

Cited by 23 publications

References 41 publications

The Neuroprotective Effect of Hericium erinaceus Extracts in Mouse Hippocampus after Pilocarpine-Induced Status Epilepticus

The Neuroprotective Effect of Hericium erinaceus Extracts in Mouse Hippocampus after Pilocarpine-Induced Status Epilepticus

Lipid nanostructures for antioxidant delivery: a comparative preformulation study

Epilepsy Disease and Nose-to-Brain Delivery of Polymeric Nanoparticles: An Overview

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