N-.omega.,(.omega.-1)-dialkyloxy)- and N-(.omega.,(.omega.-1)-dialkenyloxy)Alk-1-YL-N,N,N-tetrasubstituted ammonium lipids and uses therefor
AssigneeSyntex (U.S.A.) Inc.
InventorsDeborah A. Eppstein, Philip L. Felgner, Thomas R. Gadek, Gordon H. Jones, Richard B. Roman
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Abstract
This invention relates to compounds of the formula ##STR1## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.
Claims8
A method for the transdermal, topical or ocular delivery of a drug to the skin or to a mucous membrane of a human or animal subject, comprising the steps of:
- (1) forming a liposome comprising a therapeutically effective amount of a drug and a compound of Formula I:
- ##STR8## or an optical isomer thereof, wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms;
- R.sup.3, R.sup.4 and R.sup.5 are such that:
- (i) they are the same or different and are each alkyl of 1 to 8 carbon atoms, aryl, or aralkyl of 7 to 11 carbon atoms, or
- (ii) two taken together form pyrrolidino, piperidino, or morpholino, and the third is alkyl of 1 to 8 carbon atoms, aryl, or aralkyl of 7 to 11 carbon atoms, or
- (iii) all three together form quinuclidino;
- n is 1 to 8;
- and
- X is a pharmaceutically acceptable anion;
- and
- (2) applying the liposome to the skin or a mucous membrane of said subject.
A method for the transdermal, topical or ocular delivery of a polyanion, comprising the steps of:
- (1) forming a polyanion-liposome complex comprising a polyanion and a compound of Formula I ##STR9## or an optical isomer thereof, wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms;
- R.sup.3, R.sup.4 and R.sup.5 are such that:
- (i) they are the same or different and are each alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or
- (ii) two taken together form pyrrolidino, piperidino, or morpholino, and the third is alkyl of 1 to 8 carbon atoms, aryl, or aralkyl of 7 to 11 carbon atoms, or (iii) all three together from quinuclidino;
- n is 1 to 8;
- and
- X is a pharmaceutically acceptable anion;
- and
- (2) applying the complex to the skin or mucous membrane of a subject in need thereof.
Dependencies are inferred from the claim text.