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Cited by 90Advanced Drug Delivery SystemsNanoparticle-Based Drug DeliveryDrug Solubulity and Delivery Systems

In vitro and in vivo evaluation of WGA–carbopol modified liposomes as carriers for oral peptide delivery

Makhlof, Abdallah, Fujimoto, Shiho, Tozuka, Yuichi, Takeuchi, Hirofumi·2011·European Journal of Pharmaceutics and Biopharmaceutics
DOI 10.1016/j.ejpb.2010.12.008
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Abstract

Surface modification of liposomal nanocarriers with a novel polymer-lectin conjugate was proposed for enhancing the systemic uptake of encapsulated peptide and protein therapeutics after oral administration. Wheat germ agglutinin (WGA) was covalently attached to carbopol (CP) using the carbodiimide method. The prepared WGA-CP conjugate retained the biological cell binding activity of WGA without any evidence of cytotoxicity to Caco-2 monolayers. Cationic liposomes in the size range of 100 nm were prepared by the lipid film hydration method followed by probe sonication and surface modification with negatively charged WGA-CP. The uptake of WGA-CP liposomes by Caco-2 cells was significantly higher than that of non-modified or CP liposomes. The uptake was dependent on the surface concentration of WGA, temperature, and incubation period and was significantly inhibited in the presence of chlorpromazine and 10-fold excess of free WGA. These results suggest the involvement of active transport mechanism for the cellular uptake of the modified liposomes, mediated mainly by binding of WGA to its specific cell membrane receptors. Dual channel confocal microscopy confirmed the simultaneous association and internalization of the polymer conjugate and the liposomal carrier by Caco-2 cells and intestinal membrane of rats. In addition, the pharmacological efficacy of calcitonin, a model peptide drug, was enhanced by more than 20- and 3-fold following peroral administration of calcitonin-loaded WGA-CP liposomes when compared to non-modified and CP liposomes, respectively.

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  • WGA attached to carbopol used for surface modification of liposomes significantly increased receptor-mediated binding to Caco-2 cells and enhanced pharmacological efficacy of calcitonin loaded into nanocarriers.

    “WGA attached to carbopol has recently been used for surface modification of liposomes, which significantly increased the receptor mediated binding to Caco-2 cells and further enhanced the pharmaco logical efficacy of calcitonin, when loaded into the nanocarriers [109].”

    From Use of lectin-functionalized particles for oral immunotherapy (2012) · cites this paper as [109]

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Authors
Makhlof, A., Fujimoto, S., Tozuka, Y., & Takeuchi, H.
Affiliations
Gifu Pharmaceutical University (JP)
Corresponding author
Takeuchi, Hirofumi
ORCID
Venue
European Journal of Pharmaceutics and Biopharmaceutics
Publisher
Elsevier BV
Published
2011-02
Volume
77
Issue
2
Pages
216-224
ISSN
0939-6411 (ISSN-L)
DOI
10.1016/j.ejpb.2010.12.008
OpenAlex
W2032856871
Cited by
90
References
33
Citations by year
2026: 1 · 2025: 2 · 2024: 4 · 2023: 3 · 2022: 2 · 2021: 6 · 2020: 10 · 2019: 6 · 2018: 3 · 2017: 10 · 2016: 11 · 2015: 4 · 2014: 5 · 2013: 9 · 2012: 7
FWCI
5.14
Type
journal article
Language
en
Open access
closed
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • European Journal of Pharmaceutics and Biopharmaceutics (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
Keywords
wheat germ agglutinin, Carbopol, liposome surface modification, oral peptide delivery, cationic liposomes, Caco-2 cell uptake, active transport, calcitonin, oral bioavailability
MeSH terms
Acrylic Resins, Administration, Oral, Animals, Calcitonin, Calcium, Cell Survival, Humans, Intestine, Small, Liposomes, Male, Particle Size, Polymers, Polyvinyls, Wheat Germ Agglutinins, Rats, Wistar, Caco-2 Cells, Lectins, Rats

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