Cited by 239Advanced Drug Delivery SystemsRNA Interference and Gene DeliveryNanoparticle-Based Drug Delivery

Nose-to-brain delivery of BACE1 siRNA loaded in solid lipid nanoparticles for Alzheimer’s therapy

Rassu, Giovanna, Soddu, Elena, Posadino, Anna Maria, Pintus, Gianfranco, Sarmento, Bruno, Giunchedi, Paolo, Gavini, Elisabetta·2017·Colloids and Surfaces B: Biointerfaces

Abstract

We designed a delivery system to obtain an efficient and optimal nose-to-brain transport of BACE1 siRNA, potentially useful in the treatment of Alzheimer's disease. We selected a cell-penetrating peptide, the short peptide derived from rabies virus glycoprotein known as RVG-9R, to increase the transcellular pathway in neuronal cells. The optimal molar ratio between RVG-9R and BACE1 siRNA was elucidated. The complex between the two was then encapsulated. We propose chitosan-coated and uncoated solid lipid nanoparticles (SLNs) as a nasal delivery system capable of exploiting both olfactory and trigeminal nerve pathways. The coating process had an effect on the zeta potential, obtaining positively-charged nanoparticles, and on siRNA protection. The positive charge of the coating formulation ensured mucoadhesiveness to the particles and also prolonged residence time in the nasal cavity. We studied the cellular transport of siRNA released from the SLNs using Caco-2 as a model of epithelial-like phenotypes. We found that siRNA permeates the monolayer to a greater extent when released from any of the studied formulations than from bare siRNA, and primarily from chitosan-coated SLNs.

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Crossref · 10.1016/j.colsurfb.2017.01.031

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  • Different kinds of nanocarriers used to prepare nasal formulations able to target the brain include polymer-based and lipid-based nanoparticles.

    “According to the present literature, different kinds of nanocarriers are used to prepare nasal formulations able to target the brain, constituted by polymer-based and lipid-based nanoparticles [21,22,23].”

    From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [21]

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Authors
Rassu, G., Soddu, E., Posadino, A. M., Pintus, G., Sarmento, B., Giunchedi, P., & Gavini, E.
Affiliations
  • University of Sassari (IT)
  • Qatar University (QA)
  • Cooperativa de Ensino Superior Politécnico e Universitário (PT)
Corresponding author
Gavini, Elisabetta
Venue
Colloids and Surfaces B: Biointerfaces
Publisher
Elsevier BV
Published
2017-04
Volume
152
Pages
296-301
ISSN
0927-7765 (ISSN-L)
OpenAlex
W2579344533
Cited by
239
References
40
Citations by year
2026: 16 · 2025: 24 · 2024: 35 · 2023: 34 · 2022: 26 · 2021: 35 · 2020: 30 · 2019: 17 · 2018: 20 · 2017: 2
FWCI
9.70
Type
journal article
Language
en
Open access
closed
Locations
  • Colloids and Surfaces B Biointerfaces (publishedVersion)
  • PubMed (publishedVersion)
  • UnissResearch (Università degli Studi di Sassari) (submittedVersion)
  • Qatar University QSpace (Qatar University) (submittedVersion)
Funders
Prof Paola Rapelli for donating the Caco-2 cells
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords
nose-to-brain delivery, solid lipid nanoparticles, Alzheimer's disease, cell-penetrating peptides, chitosan coating, intranasal drug delivery, mucoadhesion, Caco-2 cells, zeta potential
MeSH terms
Alzheimer Disease, Brain, Drug Carriers, Humans, Nasal Mucosa, Aspartic Acid Endopeptidases, Caco-2 Cells, RNA, Small Interfering, Chitosan, Nanoparticles, Amyloid Precursor Protein Secretases, Cell-Penetrating Peptides

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