Method of preparation of pharmaceutical compositions
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United States of America Patent
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Feb 4, 1997
Grant Date -
N/A
app pub date -
May 27, 1994
filing date -
May 27, 1994
priority date (Note) -
Expired
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Abstract
A method of preparing a pharmaceutically beneficial, pH-sensitive amphipathic drug compound is disclosed. The pH-sensitive amphipathic parent drug compound is converted to a lipophilic derivative which is then combined with a lipophilic carrier for delivery to the lysosomes of target cells. The lipophilic derivative of the parent compound is acted upon by lysosomal enzymes to yield the parent compound. The method is demonstrated for pharmaceutically beneficial porphyrins that may be used as photosensitizers in photodynamic therapy (PDT). In particular, the method is demonstrated for the esterification of chlorin e.sub.6 and pheophorbide a for the photocytotoxic treatment of human bladder tumor cells.
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