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Cited by 63Advanced Drug Delivery SystemsNanoparticle-Based Drug DeliveryInhalation and Respiratory Drug Delivery

Nasal chitosan microparticles target a zidovudine prodrug to brain HIV sanctuaries

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Dalpiaz, Alessandro, Fogagnolo, Marco, Ferraro, Luca, Capuzzo, Antonio, Pavan, Barbara, Rassu, Giovanna, Salis, Andrea, Giunchedi, Paolo +1 more·2015·Antiviral Research
DOI 10.1016/j.antiviral.2015.09.013
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Abstract

Zidovudine (AZT) is an antiretroviral drug that is a substrate of active efflux transporters (AETs) that extrude the drug from the central nervous system (CNS) and macrophages, which are considered to be sanctuaries of HIV. The conjugation of AZT to ursodeoxycholic acid is known to produce a prodrug (UDCA-AZT) that is able to elude the AET systems, indicating the potential ability of this prodrug to act as a carrier of AZT in the CNS and in macrophages. Here, we demonstrate that UDCA-AZT is able to permeate and remain in murine macrophages with an efficiency twenty times higher than that of AZT. Moreover, we propose the nasal administration of this prodrug in order to induce its uptake into the CNS. Chitosan chloride-based microparticles (CP) were prepared by spray-drying and were characterized with respect to size, morphology, density, water uptake and the dissolution profile of UDCA-AZT. The CP sample was then nasally administered to rats. All in vitro and in vivo measurements were also performed for a CP parent physical mixture. The CP sample was able to increase the dissolution rate of UDCA-AZT and to reduce water uptake with respect to its parent physical mixture, inducing better uptake of UDCA-AZT into the cerebrospinal fluid of rats, where the prodrug can act as an AZT carrier in macrophages.

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  • Because of the direct connection provided by the olfactory and trigeminal nerves between the olfactory epithelium and the brain, drug targeting can be achieved by administering formulations onto the nasal mucosa.

    “Thanks to the direct connection provided by the olfactory and trigeminal nerves present between the olfactory epithelium and the brain, drug targeting can be achieved with the administration of formulations onto nasal mucosa [10,11,12].”

    From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [12]

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Authors
Dalpiaz, A., Fogagnolo, M., Ferraro, L., Capuzzo, A., Pavan, B., Rassu, G., Salis, A., Giunchedi, P., & Gavini, E.
Affiliations
  • University of Ferrara (IT)
  • University of Sassari (IT)
Corresponding author
Rassu, Giovanna
ORCID
Venue
Antiviral Research
Publisher
Elsevier BV
Published
2015-11
Volume
123
Pages
146-157
ISSN
0166-3542 (ISSN-L)
DOI
10.1016/j.antiviral.2015.09.013
OpenAlex
W1804367766
Cited by
63
References
60
Citations by year
2026: 2 · 2025: 5 · 2024: 5 · 2023: 8 · 2022: 5 · 2021: 5 · 2020: 5 · 2019: 8 · 2018: 9 · 2017: 8 · 2016: 3
FWCI
3.72
Type
journal article
Language
en
Open access
Licence
Locations
  • Antiviral Research (publishedVersion)
  • PubMed (publishedVersion)
  • UnissResearch (Università degli Studi di Sassari) (submittedVersion, cc-by-nc-nd)
  • Institutional Research Information System University of Ferrara (University of Ferrara) (submittedVersion, cc-by-nc-nd)
Funders
Ministero dell’Istruzione, dell’Università e della Ricerca
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
  • Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
Keywords
zidovudine, prodrugs, chitosan microspheres, intranasal drug delivery, macrophages, cerebrospinal fluid, spray drying, dissolution rate, water absorption, antiretroviral drug delivery
MeSH terms
Administration, Intranasal, Animals, Antiviral Agents, Brain Chemistry, Capsules, Drug Carriers, Male, Prodrugs, Ursodeoxycholic Acid, Zidovudine, Rats, Wistar, Chitosan

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