Synergistic encapsulation of the anti-HIV agent efavirenz within mixed poloxamine/poloxamer polymeric micelles
Open accessAbstract
This study investigated the synergistic performance of mixed polymeric micelles made of linear and branched poly(ethylene oxide)-poly(propylene oxide) for the more effective encapsulation of the anti-HIV drug efavirenz. The co-micellization process of 10% binary systems combining different weight ratios of a highly hydrophilic poloxamer (Pluronic F127) and a more hydrophobic poloxamine counterpart (Tetronic T304 and T904) was investigated by means of dynamic light scattering, cloud point and electronic spin resonance experiments. Then, the synergistic solubilization capacity of the micelles was shown. Findings revealed a sharp solubility increase from 4 μg/ml up to more than 33 mg/ml, representing a 8430-fold increase. Moreover, the drug-loaded mixed micelles displayed increased physical stability over time in comparison with pure poloxamine ones. Overall findings confirmed the enormous versatility of the poloxamer/poloxamine systems as Trojan nanocarriers for drug encapsulation and release by the oral route and they entail a relevant enhancement of the previous art towards a more compliant pediatric HIV pharmacotherapy.
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Poloxamer-poloxamine mixed micelles are successfully prepared to solubilize the antiretroviral drug efavirenz (EFV), resulting in a significant increase (8400-fold) in apparent solubility and achieving high encapsulation efficiency when adding the drug directly to the dispersed copolymers in aqueous medium.
“For instance, poloxamer-poloxamine mixed micelles are successfully prepared to solubilize the antiretroviral drug efavirenz (EFV), resulting in a significant increase (8400-fold) in apparent solubility and achieving high encapsulation efficiency when adding the drug directly to the dispersed copolymers in aqueous medium [99].”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [99]
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References 41 · Cited by 96
Research works printed but not linked: 6
- Panel of clinical practices for treatment of HIV infection. Pan Am J Public Health 2001;10:426-35.
- Brown E. Antiretroviral therapy in children, HIV/AIDS primary care guide. Chapter 30. AIDS Educ Train Centers Natl Resource Center 2007:419.
- Barrueco N, Castillo I, Ais A, Martínez C, Sanjurjo M. Program of pharmaceutic attention to pediatric patients in antiretroviral therapy. Farm Hosp 2005;29:367-74.
- Wintergerst U, Hoffmann F, Jansson A, Notheis G, Huss K, Kurowski M, et al. Antiviral efficacy, tolerability and pharmacokinetics of efavirenz in an unselected cohort of HIV-infected children. J Antimicrob Chemother 2008;61:1336-9.
- Chiappetta DA, Hocht C, Taira C, Sosnik A. Oral pharmacokinetics of efavirenz-loaded polymeric micelles. Biomaterials 2011;32:2379-87.
- Peroni RN, Hocht C, Chiappetta DA, Di Gennaro SS, Rubio MC, Sosnik A, et al. The anti-HIV drug efavirenz is substrate and modulates the expression of the efflux transporter BCRP (ABCG2) in rats. First World Conference on Nanomedicine and Drug Delivery (WCN2010). India: Kottayam; 2010.
- Authors
- Chiappetta, D. A., Facorro, G., Rubin de Celis, E., & Sosnik, A.
- Affiliations
- Consejo Nacional de Investigaciones Científicas y Técnicas (AR)
- Universidad de Buenos Aires (AR)
- Corresponding author
- Sosnik, Alejandro
- Venue
- Nanomedicine Nanotechnology Biology and Medicine
- Publisher
- Elsevier BV
- Published
- 2011-10
- Volume
- 7
- Issue
- 5
- Pages
- 624-637
- ISSN
- 1549-9634 (ISSN-L)
- OpenAlex
- W2035716618
- Cited by
- 96
- References
- 41
- Citations by year
- 2026: 3 · 2025: 3 · 2024: 3 · 2023: 4 · 2022: 5 · 2021: 12 · 2020: 12 · 2019: 5 · 2018: 4 · 2017: 11 · 2016: 5 · 2015: 10 · 2014: 6 · 2013: 8 · 2012: 5
- FWCI
- 3.71
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Nanomedicine Nanotechnology Biology and Medicine (publishedVersion)
- PubMed (publishedVersion)
- Conicet (submittedVersion, cc-by-nc-sa)
- Funders
- Consejo Nacional de Investigaciones Científicas y Técnicas (PIP 11220090100220)
- Universidad de Buenos Aires (UBACyT 20020090200016)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Physical Sciences › Chemistry › Organic Chemistry › Surfactants and Colloidal Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- efavirenz, poloxamine, poloxamer, polymeric micelles, mixed micelles, drug encapsulation, oral drug delivery, HIV antiretroviral drugs, physical stability, Pluronic F127
- MeSH terms
- Acquired Immunodeficiency Syndrome, Alkynes, Cyclopropanes, Drug Synergism, Ethylenediamines, HIV, Humans, Micelles, Solubility, Drug Delivery Systems, Anti-HIV Agents, Poloxamer, Benzoxazines, Nanocapsules
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