Solubilization of poorly soluble PDT agent, meso-tetraphenylporphin, in plain or immunotargeted PEG-PE micelles results in dramatically improved cancer cell killing in vitro

Roby A., Erdogan S. , Torchilin V.

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, vol.62, no.3, pp.235-240, 2006 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 62 Issue: 3
  • Publication Date: 2006
  • Doi Number: 10.1016/j.ejpb.2005.09.010
  • Page Numbers: pp.235-240


Poorly soluble photodynamic therapy (PDT) agent, meso-tetratphenylporphine (TPP), was effectively solubilized using non-targeted and tumor-targeted polymeric micelles prepared of polyethylene glycol/phosphatidyl ethanolamine conjugate (PEG-PE). Encapsulation of TPP into PEG-PE-based micelles and inimunomicelles (bearing an anti-cancer monoclonal 2C5 antibody) resulted in significantly improved anticancer effects of the drug at PDT conditions against murine (LLC, B 16) and human (MCF-7, BT20) cancer cells in vitro. For this purpose, the cells were incubated for 6 or 18 h with the TPP or TPP-loaded PEG-PE micelles/immunomicelles and then light-irradiated for 30 min. The phototoxic effect depended on the TPP concentration and specific targeting by immunomicelles. An increased level of apoptosis was shown in the PDT-treated cultures. The attachment of the anti-cancer 2C5 antibodies to TPP-loaded micelles provided the maximum level of cell killing at a given time. The results of this study showed that TPP-containing PEG-PE micelles may represent a useful formulation of the photosensitizer for practical PDT. (c) 2006 Elsevier B.V. All rights reserved.