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

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

Abstract: A method for the production of nano- or microcapsules having a diameter of from 20 nm to 40 ?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.

Abstract: Nucleic acids comprising a nucleic acid moiety and two or more transfection enhancer elements (TEE's) according to the general formula (I): Hydrophobic moiety—pH-responsive hydrophilic moiety, wherein said pH sensitive hydrophilic moiety of said TEE is independently a weak acid having a pka of between 4 and 6.5 or is a zwitterionic structure comprising a combination of acidic groups with weak basis having a pKa of between 4.5 and 7.

Abstract: 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.

Abstract: Lipid assemblies, such as liposomes, comprising transfection enhancer elements (TEE's), which are complexed with the lipid assemblies by means of ionic interactions, or lipids incorporating such TEE's are disclosed for enhancing the fusogenicity of the lipid assemblies. The TEE's have the formula: hydrophobic moiety-pH sensitive hydrophilic moiety??(II) The pH sensitive hydrophilic moiety of each TEE is a weak acid having a pka of between 2 and 6 or a zwitterionic structure comprising a combination of acidic groups with weak bases having a pKa of between 3 and 8.

Abstract: 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.

Abstract: This disclosure describes structural elements that enhance fusogenicity of lipids and lipid assemblies (e.g. liposomes) with biological membranes, in particular cell membranes, and use of such structures. The elements are pH sensitive in terms of charge and hydrophilicity and undergo a polar—apolar transition when exposed to low pH.

Abstract: A sterol derivative with a pKa value of between 3.5 and 8, according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent linking groups, is suggested, as well as liposomes comprising such sterol derivatives.

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

Abstract: An amphoteric liposome composed of a mixture of lipids, said mixture comprising a cationic amphiphile, an anionic amphiphile and optionally one or more neutral amphiphiles, at least one of said cationic and anionic amphiphiles being chargeable and the respective amounts of said cationic and anionic amphiphiles being selected such there is a stoichiometric excess of positively charged cationic amphiphile at a first lower pH, a stoichiometric excess of negatively charged anionic amphiphile at a second higher pH and said mixture has an isoelectric point intermediate said first and second pHs; characterised in that said positively charged cationic and negatively charged anionic amphiphiles are adapted to form a lipid salt with one another at said isoelectric point. Also disclosed are methods of predicting the fusogenicity of an amphoteric liposome at a given pH, formulating an amphoteric liposome and loading an amphoteric liposome with a cargo moiety.

Abstract: An amphoteric liposome composed of a mixture of lipids, said mixture comprising a cationic amphiphile, an anionic amphiphile and optionally one or more neutral amphiphiles, at least one of said cationic and anionic amphiphiles being chargeable and the respective amounts of said cationic and anionic amphiphiles being selected such there is a stoichiometric excess of positively charged cationic amphiphile at a first lower pH, a stoichiometric excess of negatively charged anionic amphiphile at a second higher pH and said mixture has an isoelectric point intermediate said first and second pHs; characterised in that said positively charged cationic and negatively charged anionic amphiphiles are adapted to form a lipid salt with one another at said isoelectric point. Also disclosed are methods of predicting the fusogenicity of an amphoteric liposome at a given pH, formulating an amphoteric liposome and loading an amphoteric liposome with a cargo moiety.

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

Abstract: 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.

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

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

Abstract: 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.

Abstract: The invention relates to formulations of liposomes and polymers for the production of an injectable depot of active substances, which has sustained release and effect in a mammal organism.

Abstract: The invention relates to liposomal formulations for the production of an injectable depot of peptide, protein and oligonucleotide active substances for sustained release and effect in a mammal body.

Abstract: A pharmaceutical composition is disclosed, which composition comprises an oligonucleotide as an active agent, the oligonucleotide being adapted to target nucleic acids encoding CD40 thereby to modulate the expression of CD40 in mammalian cells, and a liposome as an excipient. Said liposome is an amphoteric liposome. Also disclosed is a method for the treatment or prophylaxis of a disease or condition associated with the expression of CD40 in a human or non-human animal patient by administering to said patient a therapeutically or prophylactically effective amount of such a composition.