Steroidal liposomes
First Claim
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1. A method for preparing a pharmaceutical composition which comprises liposomes having bilayers comprising a lipid which consists essentially of a salt form of an organic acid sterol derivative capable of forming closed bilayers, the method comprising:
- (i) mixing an amount of the salt form of the organic acid sterol derivative sufficient to form closed vesicles with an aqueous phase so as to form a mixture comprising the aqueous phase and the sterol derivative, wherein the mixture is essentially free of organic solvent; and
(ii) agitating the mixture until vesicles are formed, wherein when the sterol derivative is negatively charged at neutral pH the mixture is substantially free of multivalent cations or when the derivative is positively charged at neutral pH the mixture is substantially free of multivalent anions.
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Abstract
Methods and compositions are described for the preparation of bioactive agents entrapped in lipid vesicles the bilayers of which comprise a salt form of an organic acid derivative of a sterol, such as the tris-salt form of a sterol hemisuccinate, and to bompositions comprising a mixtue of tris(hydroxymethyl)aminomethane salt of cholesteryl hemisuccinate with either an antifungal compound or a peptide. These compositions have various applications in vivo.
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Citations
18 Claims
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1. A method for preparing a pharmaceutical composition which comprises liposomes having bilayers comprising a lipid which consists essentially of a salt form of an organic acid sterol derivative capable of forming closed bilayers, the method comprising:
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(i) mixing an amount of the salt form of the organic acid sterol derivative sufficient to form closed vesicles with an aqueous phase so as to form a mixture comprising the aqueous phase and the sterol derivative, wherein the mixture is essentially free of organic solvent; and
(ii) agitating the mixture until vesicles are formed, wherein when the sterol derivative is negatively charged at neutral pH the mixture is substantially free of multivalent cations or when the derivative is positively charged at neutral pH the mixture is substantially free of multivalent anions. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)
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Specification