Boron-loaded liposomes in the treatment of hepatic metastases: Preliminary investigation by autoradiography analysis

Franca Pavanetto, Paola Perugini, Ida Genta, Claudio Minoia, Anna Ronchi, Ubaldo Prati, Laura Roveda, Rosanna Nano

Research output: Contribution to journalArticle

Abstract

Boronophenylalanine (BPA)-loaded conventional and stabilized liposomes were prepared by the reversed phase evaporation method to treat liver metastases by boron neutron capture therapy. Conventional vesicles were composed of phosphatidylcholine and cholesterol, molar ratio 1:1. To obtain stealth liposomes, GM1 or PEG were included in the lipidic bilayer at a concentration of 6.67 or 5 mol%, respectively. Large unilamellar vesicles were formulated encapsulating BPA in the liposome aqueous compartment as a complex with fructose; BPA free base also was embedded into the lipidic bilayer. In vivo experiments were carried out after intravenous injection of liposome suspensions in BD-IX strain rats in which liver metastases had been induced. Alpha particle spectroscopy associated with histological analysis was performed to visualize boron spatial distribution in liver. Simultaneously, tissue boron concentrations were determined using inductively coupled plasma-mass spectroscopy. Results showed that PEG-modified liposomes accumulated boron in therapeutic concentrations (>30 μg boron/g tissue) in metastatic tissue. The PEG-liposomes could be further explored in enhancing boron delivery to tumor cells.

Original languageEnglish
Pages (from-to)97-103
Number of pages7
JournalDrug Delivery
Volume7
Issue number2
Publication statusPublished - 2000

Keywords

  • Antitumor Therapy
  • Boron Neutron Capture Therapy (BNCT)
  • Boronophenylalanine
  • Liposomes

ASJC Scopus subject areas

  • Pharmacology

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    Pavanetto, F., Perugini, P., Genta, I., Minoia, C., Ronchi, A., Prati, U., Roveda, L., & Nano, R. (2000). Boron-loaded liposomes in the treatment of hepatic metastases: Preliminary investigation by autoradiography analysis. Drug Delivery, 7(2), 97-103.