Cited by 95Advanced Drug Delivery SystemsNanoparticle-Based Drug DeliveryHIV/AIDS Research and Interventions

Nanoparticles-in-film for the combined vaginal delivery of anti-HIV microbicide drugs

Cunha-Reis, Cassilda, Machado, Alexandra, Barreiros, Luísa, Araújo, Francisca, Nunes, Rute, Seabra, Vítor, Ferreira, Domingos, Segundo, Marcela A. +2 more·2016·Journal of Controlled Release

Abstract

Combining two or more antiretroviral drugs in one medical product is an interesting but challenging strategy for developing topical anti-HIV microbicides. We developed a new vaginal delivery system comprising the incorporation of nanoparticles (NPs) into a polymeric film base - NPs-in-film - and tested its ability to deliver tenofovir (TFV) and efavirenz (EFV). EFV-loaded poly(lactic-co-glycolic acid) NPs were incorporated alongside free TFV into fast dissolving films during film manufacturing. The delivery system was characterized for physicochemical properties, as well as genital distribution, local and systemic 24h pharmacokinetics (PK), and safety upon intravaginal administration to mice. NPs-in-film presented suitable technological, mechanical and cytotoxicity features for vaginal use. Retention of NPs in vivo was enhanced both in vaginal lavages and tissue when associated to film. PK data evidenced that vaginal drug levels rapidly decreased after administration but NPs-in-film were still able to enhance drug concentrations of EFV. Obtained values for area-under-the-curve for EFV were around one log10 higher than those for the free drugs in aqueous vehicle (phosphate buffered saline). Film alone also contributed to higher and more prolonged local drug levels as compared to the administration of TFV and EFV in aqueous vehicle. Systemic exposure to both drugs was low. NPs-in-film was found to be safe upon once daily vaginal administration to mice, with no significant genital histological changes or major alterations in cytokine/chemokine profiles being observed. Overall, the proposed NPs-in-film system seems to be an interesting delivery platform for developing combination vaginal anti-HIV microbicides.

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Crossref · 10.1016/j.jconrel.2016.09.020

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  • The improved tissue concentrations from film-embedded nanoparticles were observed only within the first hour of administration, and not at later times.

    “However, the improved tissue concentrations were observed only within the first hour of administration, and not at later times.”

    From Nanotechnology approaches for global infectious diseases (2021) · cites this paper as [25]

  • Cunha-Reis et al. demonstrated that nanoparticles loaded with efavirenz and embedded in a water-soluble film showed lower leakage and enabled higher tissue concentrations than nanoparticle dispersions.

    “Cunha-Reis et al. demonstrated that nanoparticles loaded with an anti-HIV drug (efavirenz) and embedded in a water-soluble film showed lower leakage and enabled higher tissue concentrations than nanoparticle dispersions 25 .”

    From Nanotechnology approaches for global infectious diseases (2021) · cites this paper as [25]

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Authors
Cunha-Reis, C., Machado, A., Barreiros, L., Araújo, F., Nunes, R., Seabra, V., Ferreira, D., Segundo, M. A., Sarmento, B., & das Neves, J.
Affiliations
  • Cooperativa de Ensino Superior Politécnico e Universitário (PT)
  • Universidade do Porto (PT)
Venue
Journal of Controlled Release
Publisher
Elsevier BV
Published
2016-12
Volume
243
Pages
43-53
ISSN
0168-3659 (ISSN-L)
OpenAlex
W2522640295
Cited by
95
References
76
Citations by year
2026: 1 · 2025: 4 · 2024: 5 · 2023: 8 · 2022: 12 · 2021: 13 · 2020: 15 · 2019: 10 · 2018: 14 · 2017: 10 · 2016: 3
FWCI
7.05
Type
journal article
Language
en
Open access
closed
Locations
  • Journal of Controlled Release (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • Fundação para a Ciência e a Tecnologia
  • FEDER
  • Institute for Research and Innovation in Health Sciences (POCI-01-0145-FEDER-007274)
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 › Infectious Diseases › HIV/AIDS Research and Interventions
Keywords
vaginal drug delivery, tenofovir, efavirenz, PLGA nanoparticles, fast dissolving films, highly active antiretroviral therapy, vaginal histology
MeSH terms
Tenofovir, Polylactic Acid-Polyglycolic Acid Copolymer, Administration, Intravaginal, Alkynes, Animals, Chemistry, Pharmaceutical, Cyclopropanes, Drug Carriers, Drug Combinations, Female, Polyglycolic Acid, Tissue Distribution, Drug Delivery Systems, Lactic Acid, Anti-HIV Agents, Benzoxazines, Mice, Nanoparticles

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