Biodistribution of 125I-labeled polymeric vaccine carriers after subcutaneous injection

Riki Toita, Yasukazu Kanai, Hiroshi Watabe, Kenshi Nakao, Seiichi Yamamoto, Jun Hatazawa, Mitsuru Akashi

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)

Abstract

Polymeric nanoparticles (NPs) comprised of hydrophilic poly(γ- glutamic acid) in the main chain and hydrophobic phenylalanine in the side chain (γ-PGA-Phe) are a promising vaccine carrier for various kinds of diseases. However, little is known about the fate of subcutaneously administered γ-PGA-Phe NPs. Therefore, we newly synthesized γ-PGA graft phenylalanine and tyrosine conjugates (γ-PGA-Phe-Tyr), and then γ-PGA-Phe-Tyr NPs were labeled with 125I for monitoring their biodistribution (γ-PGA-Phe-Tyr(125I) NPs). Dynamic light scattering (DLS) measurements showed that γ-PGA-Phe-Tyr(125I) NPs showed 200 nm in diameter and a negative ζ-potential, which was comparable to those of their precursors. γ-scintigraphic images showed that in mice, subcutaneously injected γ-PGA-Phe-Tyr(125I) NPs were mainly observed at the site of injection (SOI), but not other organs 1 h after administration. However, γ-PGA-PheTyr(125I) NPs were almost undetectable at the SOI and other organs at 11 days postinjection. Similar results were observed when γ-PGA-Phe-Tyr(125I) NPs were subcutaneously injected into rats. Furthermore, at 11 days postinjection, 73 ± 3% of the injected dose of γ-PGA-Phe-Tyr(125I) NPs was detected in the feces (14 ± 1%) and urine (59 ± 1%). These results clearly showed that subcutaneously injected γ-PGA-Phe-Tyr( 125I) NPs were cleared from the body, and γ-PGA-Phe NPs were safe and effective vaccine carriers.

Original languageEnglish
Pages (from-to)5310-5315
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume21
Issue number17
DOIs
Publication statusPublished - 2013 Sep 1
Externally publishedYes

Keywords

  • Biodegradable polymers
  • Biodistribution
  • I radiolabeled
  • Polymeric nanocarriers
  • γ-Scintigraphy

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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