In‐vitro and in‐vivo evaluation of pH‐responsive polymeric micelles in a photodynamic cancer therapy model
Identifieur interne : 002366 ( Main/Exploration ); précédent : 002365; suivant : 002367In‐vitro and in‐vivo evaluation of pH‐responsive polymeric micelles in a photodynamic cancer therapy model
Auteurs : J. Taillefer ; N. Brasseur ; J. E. Van Lier ; V. Lenaerts [Canada] ; D. Le Garrec ; J. Leroux [Canada]Source :
- Journal of Pharmacy and Pharmacology [ 0022-3573 ] ; 2001-02.
Abstract
pH‐sensitive polymeric micelles of randomly and terminally alkylated N‐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 μmol kg−1 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.
Url:
DOI: 10.1211/0022357011775352
Affiliations:
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Leroux</name><affiliation></affiliation><affiliation wicri:level="1"><country wicri:rule="url">Canada</country></affiliation></author></analytic><monogr></monogr><series><title level="j" type="main">Journal of Pharmacy and Pharmacology</title><title level="j" type="alt">JOURNAL OF PHARMACY AND PHARMACOLOGY</title><idno type="ISSN">0022-3573</idno><idno type="eISSN">2042-7158</idno><imprint><biblScope unit="vol">53</biblScope><biblScope unit="issue">2</biblScope><biblScope unit="page" from="155">155</biblScope><biblScope unit="page" to="166">166</biblScope><biblScope unit="page-count">12</biblScope><publisher>Blackwell Publishing Ltd</publisher><pubPlace>Oxford, UK</pubPlace><date type="published" when="2001-02">2001-02</date></imprint><idno type="ISSN">0022-3573</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0022-3573</idno></seriesStmt></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">pH‐sensitive polymeric micelles of randomly and terminally alkylated N‐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 μmol kg−1 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.</div></front></TEI><affiliations><list><country><li>Canada</li></country></list><tree><noCountry><name sortKey="Brasseur, N" sort="Brasseur, N" uniqKey="Brasseur N" first="N." last="Brasseur">N. Brasseur</name><name sortKey="Garrec, D Le" sort="Garrec, D Le" uniqKey="Garrec D" first="D. Le" last="Garrec">D. Le Garrec</name><name sortKey="Taillefer, J" sort="Taillefer, J" uniqKey="Taillefer J" first="J." last="Taillefer">J. Taillefer</name><name sortKey="Van Lier, J E" sort="Van Lier, J E" uniqKey="Van Lier J" first="J. E." last="Van Lier">J. E. 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