Method of amphiphatic drug loading in liposomes by pH gradient

Details Method of amphiphatic drug loading in liposomes by pH gradient Method of amphiphatic drug loading in liposomes by pH gradient

1989-09-27

1993-03-09

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Liposomes

264 41, 264 43, 264 46, 424710, 4284022, 436829, A61K 3722

Patent

active

051925494

ABSTRACT:
An improved simple, efficient, safe, economical, and fast transmembrane loading procedure for efficient active loading of weak amphiphatic drugs into liposomes using the transmenbrane gradient. The resulting liposomes loaded with the amphiphatic drug are stable and safe. A storageable form of loadable liposomes has extended period of stability. The reversed procedure is applicable for sustained release of liposome encapsulated drugs from ammonium liposomes.

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Deamer et al, "The Response of . . . Membranes" Biochimica Et Biophysica a, vol. 274 (1972), pp. 323-335.
Nichols et al. "Catecholamine . . . pH Gradients" Biochimica Et Biophysica Acta, vol. 455 (1976), pp. 269-271.
Mayer, L., et al., Biochim. Biophys. Acta 857:123 (1986).
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Cancer Res. 42:4734 (1982).
Chem. Phys. Lipids 40:333 (1986).
J. Biol. Chem. 260:802 (1985).
Biochim. Biophys. Acta 816:294 (1985).

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