Marina Biotech, Inc.

Novosom Ag

Pronai Therapeutics, Inc.

Capsulution Pharma Ag

Gerold Endert

Steffen Panzner

Frank Essler

Yvonne Kerwitz

Silke Lutz

Cornelia Panzner

Stefan Fankhänel

Una Rauchhaus

Stefan Fankhaenel

Anja Behrens

Neal Goodwin

Wendi Rodrigueza

Natalie Herzog

Monika Fellermeier

Nasr El-Mokdad

Neal Clifford Goodwin

A serum-stable mixture of lipids capable of encapsulating an active agent to form a liposome, said mixture comprising phosphatidylcholine and phosphatidylethanolamine in a ratio in the range of about 0.5 to about 8. The mixture may also include pH sensitive anionic and cationic amphiphiles, such that the mixture is amphoteric, being negatively charged or neutral at pH 7.4 and positively charged at pH 4. Amphoteric liposomes comprising such a mixture may be used for encapsulating nucleic acid therapeutics, such as oligonucleotides and DNA plasmids. The drug/lipid ratio may be adjusted to target the liposomes to particular organs or other sites in the body.

Amphoteric liposomes

The invention suggests amphoteric lipids wherein one or more amphoteric groups having an isoelectric point between 4 and 9 are substituted on a membranous or membrane-forming amphiphilic substance, as well as liposomes containing such compounds.

Components for producing amphoteric liposomes

The invention relates to compositions and methods to inhibit gene expression. In particular, the invention provides DNAi oligonucleotides sequestered by amphoteric liposomes for the treatment of cancer.

Amphoteric liposome formulation

The invention relates to amphoteric liposomal formulations which are provided with great serum stability and are suitable for the intracellular delivery of oligonucleotides.

Serum-stable amphoteric liposomes

The invention suggests a pH-sensitive cationic lipid with a pKvalue between 3.5 and 8, according to the general formulacation-spacer-Y-spacer-X-lipid,wherein Y and X represent linking groups. Furthermore, liposomes are described, which liposomes include said optionally cationic lipids.

pH-sensitive cationic lipids, and liposomes and nanocapsules containing the same

Amphoteric liposomes are proposed, which comprise positive and negative membrane-based or membrane-forming charge carriers as well as the use of these liposomes.

Amphoteric liposomes and their use

A method for the production of nano- or microcapsules having a diameter of from 20 nm to 40 &#x3bc;m is suggested, wherein template particles are supplied in an aqueous medium, electrically recharged with a polyelectrolyte, re-recharged without separation or washing steps using a second polyelectrolyte having a complementary charge with respect to the first polyelectrolyte, and said process is optionally continued with alternately charged polyelectrolytes.

Nanocapsules having a polyelectrolyte envelope

An amphoteric compound based on a sterol skeleton, the 3-position of the sterol ring system being substituted by one or more amphoteric groups having an isoelectric point of between about 4 and 9, together with liposomes containing such compounds and their uses.

Amphoteric sterols and the use thereof

Disclosed is a sterol derivative having a pKa value of 3.5-8 according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent bonding groups. The invention also relates to liposomes containing said sterol derivatives.

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Halle, Germany

Gerold Endert