@article {Taillefer:1 February 2001:0022-3573:155,
	author = "Taillefer J.",
	author = "Brasseur N.",
	author = "van Lier J.E.",
	author = "Lenaerts V.",
	author = "Le Garrec D.",
	author = "Leroux J.C.",
	title = "In-vitro and in-vivo evaluation of pH-responsive polymeric micelles in a photodynamic cancer therapy model",
	journal = "Journal of Pharmacy and Pharmacology",
	volume = "53",
	year = "1 February 2001",
	abstract = "pH-sensitive polymeric micelles of randomly and terminally alkylated <I>N</I>-isopropylacrylamide copolymers were prepared and characterized. Aluminium chloride phthalocyanine (AlClPc), a second generation sensitizer for the photodynamic therapy of cancer, was incorporated in the micelles by dialysis. Their photodynamic activities were evaluated in-vitro against EMT-6 mouse mammary tumour cells and in-vivo against EMT-6 tumours implanted intradermally on each hind thigh of Balb/c mice. pH-sensitive polymeric micelles were found to exhibit greater cytotoxicity in-vitro than control Cremophor EL formulations. In the presence of chloroquine, a weak base that raises the internal pH of acidic organelles, in-vitro experiments demonstrated the importance of endosomal/lysosomal acidity for the pH-sensitive polymeric micelles to be fully effective. Biodistribution was assessed by fluorescence of tissue extracts after intravenous injection of 2 <IMG SRC="/iso-ents/isogrk32/mu-s.gif" ALT="mu">mol kg<SUP>-1</SUP> AlClPc. The results revealed accumulation of AlClPc polymeric micelles in the liver, spleen and lungs, with a lower tumour uptake than AlClPc Cremophor EL formulations. However, polymeric micelles exhibited similar activity in-vivo to the control Cremophor EL formulations, demonstrating the higher potency of AlClPc polymeric micelles when localized in tumour tissue. It was concluded that polymeric micelles represent a good alternative to Cremophor EL preparations for the vectorization of hydrophobic drugs.",
	pages = "155-166(12)",
	url = "http://www.ingentaconnect.com/content/rpsgb/jpp/2001/00000053/00000002/art00003"
	doi = "doi:10.1211/0022357011775352"
}