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Large anti-HER2/neu liposomes for potential targeted intraperitoneal therapy of micrometastatic cancer
Stavroula Sofou1, Richard Enmon, Stig Palm
1Department of Chemical and Biological Engineering, Polytechnic Institute of New York University, Brooklyn, NY 11201, USA. ssofou@poly.edu
Unlabelled:
Effective targeting and killing of intraperitoneally disseminated micrometastases remains a challenge.
Objective/Methods:
In this work, we evaluated the potential of antibody-labeled PEGylated large liposomes as vehicles for direct intraperitoneal (i.p.) drug delivery with the aim to enhance the tumor-to-normal organ ratio and to improve the bioexposure of cancer cells to the delivered therapeutics while shifting the toxicities toward the spleen. These targeted liposomes are designed to combine: (1) specific targeting to and internalization by cancer cells mediated by liposome-conjugated tumor-specific antibodies, (2) slow clearance from the peritoneal cavity, and (3) shift of normal organ toxicities from the liver to the spleen due to their relatively large size.
Results:
Conjugation of anti-HER2/neu antibodies to the surface of large (approximately 600 nm in diameter) PEGylated liposomes results in fast, specific binding of targeted liposomes to cancer cells in vitro, followed by considerable cellular internalization. In vivo, after i.p. administration, these liposomes exhibit fast, specific binding to i.p. cancerous tumors. Large liposomes are slowly cleared from the peritoneal cavity, and they exhibit increased uptake by the spleen relative to the liver, while targeted large liposomes demonstrate specific tumor uptake at early times. Although tissue and tumor uptake are greater for cationic liposomes, the tumor-to-liver and spleen-to-liver ratios are similar for both membrane compositions, suggesting a primary role for the liposome's size, compared to the liposome's surface charge.
Conclusions:
The findings of this study suggest that large targeted liposomes administered i.p. could be a potent drug-delivery strategy for locoregional therapy of i.p. micrometastatic tumors.
Insights
Targeted large liposomes show promise for treating intraperitoneal (i.p.) micrometastases. Antibody-labeled liposomes enhance drug delivery to tumors, improving cancer cell exposure and reducing systemic toxicity.
Area of Science:
- Nanotechnology in Medicine
- Cancer Therapeutics
- Drug Delivery Systems
Background:
- Intraperitoneal (i.p.) micrometastases are challenging to target effectively.
- Current drug delivery methods often lack specificity and can cause systemic toxicity.
Purpose of the Study:
- To evaluate antibody-labeled PEGylated large liposomes for direct i.p. drug delivery.
- To enhance tumor-to-normal organ drug ratios and cancer cell bioexposure.
- To shift toxicities from the liver to the spleen.
Main Methods:
- Conjugation of anti-HER2/neu antibodies to large (approx. 600 nm) PEGylated liposomes.
- In vitro assessment of cancer cell binding and internalization.
- In vivo evaluation of liposome biodistribution, clearance, and tumor targeting after i.p. administration.
Main Results:
- Targeted liposomes demonstrated fast, specific binding and internalization by cancer cells in vitro.
- In vivo, liposomes showed specific binding to i.p. tumors and slow clearance from the peritoneal cavity.
- Increased spleen uptake relative to the liver was observed, with targeted liposomes showing early tumor uptake.
Conclusions:
- Large, antibody-targeted liposomes administered i.p. represent a potent strategy for locoregional therapy.
- This approach effectively targets intraperitoneal micrometastases.
- Liposome size plays a key role in biodistribution and toxicity profiles.
