Appeal No. 2001-1044 Page 6
Application No. 08/881,216
both topically and orally (abstract) and that it has high lipophilicity (page 785).
Birnbaum does not suggest liposomal formulations of terbinafine.
Lopez-Berestein discloses liposomal formulations of nystatin. In the most
preferred embodiment, the liposomes consist essentially of dimyristoyl-
phosphatidylcholine and dimyristoylphosphatidylglycerol in a ratio of about 7:3.
Column 6, lines 10-14. Lopez-Berestein teaches that nystatin was a known
antifungal agent of the polyene class (see Table 2) that is tolerated well both
orally and topically but could not be used intravenously because of its presumed
high toxicity and aqueous insolubility. Column 4, lines 50-53. See also column
5, lines 33-36: “Nystatin . . . has high hydrophobicity, which has precluded its
effective systemic administration. It has been used as suspensions . . .
administered to the patients orally. However, these studies have generally failed
to document a beneficial effect of nystatin administration against systemic fungal
infections.”
Lopez-Berestein teaches that “[l]iposome-encapsulated nystatin (L-Nys)
has a lowered systemic toxicity and an enhanced therapeutic efficacy as
compared to free-Nys.” Column 6, lines 61-63. Lopez-Berestein also teach that
L-Nys can be administered topically “near to sites of localized fungal infection,”
and that “[a]lthough Nys has been topically used, L-Nys should more effectively
inhibit fungal proliferation.” Column 8, lines 28-35.
Janoff teaches vesicles (i.e., liposomes) which can contain “[b]ioactive
agents, for example, antifungal compounds.” Column 12, lines 50-53.
“Antifungal agents which may be present in the formulations of the instant
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