The invention relates to amphiphilic derivatives of a triazamacrocyclic compound, as well as to said derivatives as active molecule transporters. The invention also relates to a nanodrug including at least one amphiphilic derivative of a triazamacrocyclic compound and at least one active molecule of a protein such as an antibody, in particular for the treatment of autoimmune diseases or for the treatment of cancer.

The present invention discloses a liposome formulation, its preparation method, and its application in the treatment of diseases caused by abnormal gene expression. The liposome formulation comprises complementary cationic lipid pairs, phospholipids, and long-circulating lipids. The method of preparing the liposome formulation comprises: mixing the complementary cationic lipid pairs with the phospholipid and the long-circulating lipid to generate pre-formed vesicles; and then mixing the pre-formed vesicles with the nucleic acid solution to generate the liposome-nucleic acid formulation. This liposome formulation provided by the present invention is easily prepared; and in the treatment of diseases caused by abnormal gene expression, the liposome formulation can be used to deliver in vivo therapeutic agents, including nucleic acids.

The invention relates to a method of detoxifying a lipopolysaccharide (LPS) or a lipid A from a Gram-negative bacterium, which comprises mixing the LPS or the lipid A with a cationic lipid so as to form a complex in which the LPS or the lipid A is associated with the cationic lipid. According to the conventional preparation modes, the cationic lipid with the co-lipid, if this latter is present, get(s) structured into complexes i.a. liposomes. When preparing lipidic complexes, the addition of LPS or Lipid A leads to an association of this latter with the cationic lipid and as a result, the LPS or lipid A is substantially detoxified. The LPS or lipid A detoxified by the complexes, e.g. when incorporated into liposomes, can be used as vaccinal antigen or as adjuvant.

The present invention provides compositions comprising mRNA molecules encapsulated within lipid particles. The lipid particles comprise a cationic lipid, a non-cationic lipid, and an mRNA molecule that is encapsulated within the lipid particle. The compositions are useful, for example, to introduce the mRNA molecules into a human subject where they are translated to produce a polypeptide that functions to ameliorate one or more symptoms of a disease. The invention also provides cationic lipids that are useful for preparing the compositions of the invention.

The invention provides a class of sucrose ester based cationic lipids and preparation method thereof. The vector prepared using the cationic lipid can be used to deliver nucleic acid. The sucrose ester based cationic lipid is prepared by using a chemical synthesis method in the invention, wherein the synthesis method is simple, and has a relatively high product yield. A composition, including suspension, emulsion, micelle and liposome and the like, can be prepared by mixing the sucrose ester based cationic lipid compound of the invention with a co-lipid. Sucrose ester based cationic lipid complex can be prepared by using the said composition and nucleic acid, which has advantages such as simple preparation, low toxicity and high transfection efficiency, and is a novel and highly efficient gene vector.

A preparation method for a liposome having the ability to stably encapsulate an active ingredient is provided. The preparation method includes providing a mixture and homogenizing the mixture at 300 bar-400 bar to form a liposome suspension. The mixture includes 0.1 wt % of lecithin, 2 wt %-5 wt % of Arabic gum and 63.9125 wt %-97.9 wt % of a solvent. The liposome suspension includes a plurality of liposomes.

Some embodiments pertain to nanoparticle-based compositions and their use in methods for the delivery of CBD to subjects. In some embodiments, the compositions are stable for prolonged periods of time and provide enhanced bioavailability.

Provided are vaccines for eliciting an immune response. The vaccines for eliciting an immune response comprise RNA encoding an immunogen, which is delivered in a liposome for the purposes of immunisation. The liposome includes lipids which have a pKa in the range of 5.0 to 7.6 and, preferably, a tertiary amine. These liposomes can have essentially neutral surface charge at physiological pH and are effective for immunisation.

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

The present invention relates to a carrier for delivering a substance to extracellular matrix-producing cells in the intestine, the carrier containing a retinoid as a targeting agent, and an agent for treating fibrosis of the intestine utilizing the carrier.