Immunoliposomes bearing polyethyleneglycol‐coupled Fab′ fragment show prolonged circulation time and high extravasation into targeted solid tumors in vivo

We have developed a new type of long‐circulating immunoliposome (Fab′–PEG immunoliposomes) which is efficiently extravasated into the targeted solid tumor in vivo. Small unilamellar liposomes (100–130 nm in diameter) were prepared from distearoylphosphatidylcholine (DSPC), cholesterol (CHOL) and a dipalmitoylphosphatidylethanolamine derivative of PEG with a terminal maleimidyl group (DPPE‐PEG‐Mal), and conjugated Fab′ fragment of antibody. Inclusion of DPPE‐PEG‐Mal and linkage of the Fab′ fragment instead of intact antibody to PEG terminals allowed the liposomes to evade RES uptake and remain in the circulation for a long time, resulting in enhanced accumulation of the liposomes in the solid tumor. Because of the ability of such Fab′–PEG immunoliposomes to target solid tumors, they appear highly attractive as carriers of not only chemotherapeutic agents, but also of macromolecular drugs.

• Publication year

  1997

• Venue

  FEBS Letters

• Publication date

  1997-08-11

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/S0014-5793(97)00905-8PMID 9287139
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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