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Cited by 124Drug Solubulity and Delivery SystemsAdvanced Drug Delivery SystemsNanoparticle-Based Drug Delivery

The DOI matches its Crossref record; 48 of the 48 references it cites were found in a registry or an index.

Oral pharmacokinetics of the anti-HIV efavirenz encapsulated within polymeric micelles

Chiappetta, Diego A., Hocht, Christian, Taira, Carlos, Sosnik, Alejandro·2011·Biomaterials
DOI 10.1016/j.biomaterials.2010.11.082
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Abstract

Aiming to improve the pediatric pharmacotherapy of the human immunodeficiency virus (HIV) infection, our group has recently developed a concentrated formulation of the first-line antiretroviral efavirenz by means of encapsulation within polymeric micelles. The aqueous solubility of the drug was increased more than 8400 times (up to 34mg/mL) and preliminary preclinical data suggested the significantly greater oral bioavailability with respect to an extemporaneous suspension and an oleous solution (similar to the only "commercially available" pediatric formulation). As the preamble to a bioequivalence trial to evaluate the micellar system in adult healthy volunteers, the present work investigated the effect of parameters such as dose per body weight and drug concentration on the oral pharmacokinetics of the drug. The non-linear pharmacokinetics of the drug was confirmed for all the formulations. Despite the drug concentration and dose, micelles consistently resulted in significantly greater absorption rates, PK parameters increasing up to 3-fold. For example, C(max) values increased from 687, 1789 and 2657ng/mL for the oily system to 1145, 2856 and 7056ng/mL for the micellar one, for EFV doses between 20 and 80mg/kg. Data clearly showed that the smaller the micellar size, the higher the bioavailability attained. The effect of micellar size was also assessed. In addition, a comparison between in vitro dissolution rates of EFV for the different micelles and AUC values suggested that micelles releasing faster in vitro lead to a less pronounced absorption in vivo. These findings would suggest the involvement of additional absorption mechanisms.

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Crossref · 10.1016/j.biomaterials.2010.11.082

Cites

48 of 48 references verified0 citation errors · 0 not checkable

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  • Targeting moieties such as specific surface receptors, transporter proteins, or phage fusion proteins can be conjugated with nanomicelles to bestow desirable delivery capabilities.

    “Targeting moieties such as specific surface receptors, transporter proteins or phage fusion proteins can be conjugated with nanomicelles to bestow them with desirable delivery capabilities [11].”

    From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [11]

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Research works printed but not linked: 2

  1. Medécins sans frontières, Press release, http://www.msf.org/; 2009. [accessed November 2010].
  2. Cuestas ML, Mathet VL, Sosnik A. Poloxamines as inhibitors of the ABC pumps superfamily and their role to optimize the pharmacotherapy. I Latin American Symposium of Nanomedicines, La Plata, Argentina, October 2010.

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Metadata

Authors
Chiappetta, D. A., Hocht, C., Taira, C., & Sosnik, A.
Affiliations
Consejo Nacional de Investigaciones Científicas y Técnicas (AR)
Corresponding author
Sosnik, Alejandro
ORCID
Venue
Biomaterials
Publisher
Elsevier BV
Published
2011-03
Volume
32
Issue
9
Pages
2379-2387
ISSN
0142-9612 (ISSN-L)
DOI
10.1016/j.biomaterials.2010.11.082
OpenAlex
W2001902661
Cited by
124
References
48
Citations by year
2026: 3 · 2025: 9 · 2024: 2 · 2023: 5 · 2022: 13 · 2021: 11 · 2020: 5 · 2019: 3 · 2018: 8 · 2017: 8 · 2016: 11 · 2015: 13 · 2014: 12 · 2013: 9 · 2012: 9
FWCI
4.69
Type
journal article
Language
en
Open access
closed
Licence
Locations
  • Biomaterials (publishedVersion)
  • PubMed (publishedVersion)
Funders
Universidad de Buenos Aires
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords
efavirenz, polymeric micelles, oral pharmacokinetics, pediatric HIV, antiretroviral drug delivery, bioavailability, micelle size, nonlinear pharmacokinetics, drug absorption, in vitro dissolution, bioequivalence, drug solubility enhancement
MeSH terms
Administration, Oral, Alkynes, Animals, Cyclopropanes, Dosage Forms, Dose-Response Relationship, Drug, Male, Micelles, Particle Size, Polymers, Rats, Wistar, Anti-HIV Agents, Area Under Curve, Benzoxazines, Rats

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