A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/40 (2006.01) A61K 9/127 (2006.01) A61K 41/00 (2006.01)
Patent
CA 2047969
TLC-182 ABSTRACT This invention relates to benzoporphyrin containing vesicles which are suitable for pharmaceutical application., In particular, the present invention relates to a liposomal prepara- tion of benzoporphyrin (BPD) incorporated into vesicles compris- ing a liposome forming lipid such as EPC or DMPC at a drug to lipid ratio of greater than 100 ug/umole lipid which will allow adequate drug dosing with relatively low lipid concentration. In an additional aspect of the present invention, sized liposomes are described which are storage stable. Certain sized BPD- containing vesicles (no greater than about 120 nm in diameter) permit sterilization by terminal filtration. Further, a lyophil- ized preparation of the BPD lipid mixture can be obtained from aqueous buffer under conditions which do not result in vesicle fusion/aggregation or BPD precipitation. Liposomes according to the present invention are able to accommodate surprisingly large amounts of BPD within the bilayer of the liposome, rather than in the encapsulated buffer. The advantages of this surprising aspect of the present invention includes the ease of manufacture and the cost savings associated with an efficient use of BPD are also presented.
Osler Hoskin & Harcourt Llp
The Liposome Company Inc.
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