Nasal administration of nanoencapsulated geraniol/ursodeoxycholic acid conjugate: Towards a new approach for the management of Parkinson's disease

Oliveira, Edilson Ribeiro de; Truzzi, Eleonora; Ferraro, Luca; Fogagnolo, Marco; Pavan, Barbara; Beggiato, Sarah; Rustichelli, Cecilia; Maretti, Eleonora; Lima, Eliana Martins; Leo, Eliana Grazia; Dalpiaz, Alessandro

doi:10.1016/j.jconrel.2020.02.033

Cited by 64 publications

(55 citation statements)

References 52 publications

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“…Geraniol is a plant metabolite proposed for the therapy of Parkinson’s disease. Its delivery in the CNS via nose-to-brain transport caused strong nasal mucosae damages when an emulsified formulation was used [ 40 ]. Considering these aspects, β-CD and HP-β-CD were proposed as geraniol carriers for the geraniol delivery in the brain after nasal administration.…”

Section: Cyclodextrin As Excipient In Nasal Formulationsmentioning

confidence: 99%

Versatile Nasal Application of Cyclodextrins: Excipients and/or Actives?

et al. 2021

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Cyclodextrins (CDs) are oligosaccharides widely used in the pharmaceutical field. In this review, a detailed examination of the literature of the last two decades has been made to understand the role of CDs in nasal drug delivery systems. In nasal formulations, CDs are used as pharmaceutical excipients, as solubilizers and absorption promoters, and as active ingredients due to their several biological activities (antiviral, antiparasitic, anti-atherosclerotic, and neuroprotective). The use of CDs in nasal formulations allowed obtaining versatile drug delivery systems intended for local and systemic effects, as well as for nose-to-brain transport of drugs. In vitro and in vivo models currently employed are suitable to analyze the effects of CDs in nasal formulations. Therefore, CDs are versatile pharmaceutical materials, and due to the continual synthesis of new CDs derivatives, the research on the new nasal applications is an interesting field evolving in the coming years, to which Italian research will still contribute.

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Section: Cyclodextrin As Excipient In Nasal Formulationsmentioning

confidence: 99%

Versatile Nasal Application of Cyclodextrins: Excipients and/or Actives?

et al. 2021

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“…Very recently, the volatile geraniol was efficiently encapsulated in solid lipid nanoparticles (SLNs) only as a prodrug obtained by its ester conjugation with ursodeoxycholic acid (GER-UDCA). In this case, the nasal administration of the nanoparticles induced selective SNC targeting of the prodrug [ 96 ] (see Section 5 ).…”

Section: The Use Of Nanoparticulate Systems For Drug Delivery Into the Brainmentioning

confidence: 99%

“…This approach was then developed and is currently applied for the brain uptake of low molecular weight neuroactive drugs [ 125 ], proteins [ 126 ] and cells [ 127 ]. Several neuroprotective agents have been studied concerning their brain delivery nasally, including anti-ischemic, anti-inflammatory, anti-Parkinson, antiepileptic and antimigraine drugs [ 96 , 128 , 129 , 130 , 131 , 132 , 133 , 134 , 135 ], as well as antibiotics [ 136 , 137 , 138 ] and antivirals [ 68 ].…”

Section: Nasal Administration As An Alternative Way To Target the Brain: The Opportunities Offered By The Prodrug Approachmentioning

confidence: 99%

“…Geraniol is a natural compound proposed for the treatment of Parkinson’s disease [ 152 ]. Even if geraniol is characterized by a relative high lipophilicity, its volatility hampers its encapsulation in polymeric or solid lipid nanoparticles [ 96 ]. The nasal administration of geraniol as a water suspension caused serious damage to the nasal mucosae [ 96 ].…”

Section: Nasal Administration As An Alternative Way To Target the Brain: The Opportunities Offered By The Prodrug Approachmentioning

confidence: 99%

“…Even if geraniol is characterized by a relative high lipophilicity, its volatility hampers its encapsulation in polymeric or solid lipid nanoparticles [ 96 ]. The nasal administration of geraniol as a water suspension caused serious damage to the nasal mucosae [ 96 ]. It is known that ursodeoxycholic acid (UDCA) is effective in rescuing mitochondrial function in Parkinson’s disease patients [ 153 ].…”

Section: Nasal Administration As An Alternative Way To Target the Brain: The Opportunities Offered By The Prodrug Approachmentioning

confidence: 99%

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Targeting Systems to the Brain Obtained by Merging Prodrugs, Nanoparticles, and Nasal Administration

2021

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About 40 years ago the lipidization of hydrophilic drugs was proposed to induce their brain targeting by transforming them into lipophilic prodrugs. Unfortunately, lipidization often transforms a hydrophilic neuroactive agent into an active efflux transporter (AET) substrate, with consequent rejection from the brain after permeation across the blood brain barrier (BBB). Currently, the prodrug approach has greatly evolved in comparison to lipidization. This review describes the evolution of the prodrug approach for brain targeting considering the design of prodrugs as active influx substrates or molecules able to inhibit or elude AETs. Moreover, the prodrug approach appears strategic in optimization of the encapsulation of neuroactive drugs in nanoparticulate systems that can be designed to induce their receptor-mediated transport (RMT) across the BBB by appropriate decorations on their surface. Nasal administration is described as a valuable alternative to obtain the brain targeting of drugs, evidencing that the prodrug approach can allow the optimization of micro or nanoparticulate nasal formulations of neuroactive agents in order to obtain this goal. Furthermore, nasal administration is also proposed for prodrugs characterized by peripheral instability but potentially able to induce their targeting inside cells of the brain.

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Revitalizing Ancient Mitochondria with Nano‐Strategies: Mitochondria‐Remedying Nanodrugs Concentrate on Disease Control

Long,

Liu,

Nan

et al. 2024

Advanced Materials

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Mitochondria, widely known as the energy factories of eukaryotic cells, have a myriad of vital functions across diverse cellular processes. Dysfunctions within mitochondria serve as catalysts for various diseases, prompting widespread cellular demise. Mounting research on remedying damaged mitochondria indicates that mitochondria constitute a valuable target for therapeutic intervention against diseases. But the less clinical practice and lower recovery rate imply the limitation of traditional drugs, which need a further breakthrough. Nanotechnology has approached favorable regiospecific biodistribution and high efficacy by capitalizing on excellent nanomaterials and targeting drug delivery. Mitochondria‐remedying nanodrugs have achieved ideal therapeutic effects. In this review, we have elucidated the significance of mitochondria in various cells and organs, while also compiling mortality data for related diseases. Correspondingly, nanodrug‐mediate therapeutic strategies and applicable mitochondria‐remedying nanodrugs in disease were detailed, with a full understanding of the roles of mitochondria dysfunction and the advantages of nanodrugs. In addition, the future challenges and directions have been widely discussed. In conclusion, this review provides comprehensive insights into the design and development of mitochondria‐remedying nanodrugs, aiming to help scientists who desire to extend their research fields and engage in this interdisciplinary subject.This article is protected by copyright. All rights reserved

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Nasal administration of nanoencapsulated geraniol/ursodeoxycholic acid conjugate: Towards a new approach for the management of Parkinson's disease

Cited by 64 publications

References 52 publications

Versatile Nasal Application of Cyclodextrins: Excipients and/or Actives?

Versatile Nasal Application of Cyclodextrins: Excipients and/or Actives?

Targeting Systems to the Brain Obtained by Merging Prodrugs, Nanoparticles, and Nasal Administration

Revitalizing Ancient Mitochondria with Nano‐Strategies: Mitochondria‐Remedying Nanodrugs Concentrate on Disease Control

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