Korea Advanced Institute of Science and Technology

Kaist IP Co., Ltd.

Other

Bioneer Corporation

Samyang Corporation

Samyang Biopharmaceuticals Corporation

Innotherapy Inc.

Tae Gwan Park

Haeshin Lee

Moon Sue Lee

Hye Jung Mok

Soo Hyeon Lee

Yoon Sung Nam

Jong Eun Oh

Keon Hyoung Lee

Ji Hoon Jeong

Sun-Hwa Kim

Hyuk Sang Yoo

In Taek Song

The present invention relates to a multi-conjugate of small interfering RNA (siRNA) and a preparing method of the same, more precisely a multi-conjugate of siRNA prepared by direct binding of double stranded sense/antisense siRNA monomers or indirect covalent bonding mediated by a cross-linking agent or a polymer, and a preparing method of the same. The preparing method of a siRNA multi-conjugate of the present invention is characterized by simple and efficient reaction and thereby the prepared siRNA multi-conjugate of the present invention has high molecular weight multiple times the conventional siRNA, so that it has high negative charge density, suggesting that it has excellent ionic interaction with a cationic gene carrier and high gene delivery efficiency.

Multi-conjugate of SiRNA and preparing method thereof

Multi-conjugate of siRNA and preparing method thereof

The present invention is related to hybrid conjugates formed by covalently bonding siRNA (small interfering RNA) molecules to hydrophilic polymers for improving stability of the siRNA molecules effective for delivering the siRNA in vivo, and polyelectrolyte complex micelles formed by ionic interactions between the conjugates and multifunctional cationic compounds. The siRNA-hydrophilic polymer conjugates and polyelectrolyte complex micelles derived therefrom can be used for improving stability of the siRNA molecules in vivo. Consequently, the delivery of siRNA molecules for therapeutic applications into cells can be facilitated, and the siRNA is still active even though a small dose of the siRNA is used.

SiRNA-hydrophilic polymer conjugates for intracellular delivery of siRNA and method thereof

Disclosed is a conjugate for gene transfer, which is capable of being used for treatment of incurable diseases, comprising an oligonucleotide intended to be transferred into target cells and a hydrophilic polymer, wherein an end of the oligonucleotide is covalently conjugated to the hydrophilic polymer. Also, the present invention discloses polyelectrolyte complex micelles formed from such a conjugate and a cationic polymer or cationic peptide. Such polyelectrolyte complex micelles can effectively transfer oligonucleotides as therapeutic agents into target cells, making it possible to obtain desired activities of the delivered oligonucleotides in target cells even when the micelles are clinically applied at a relatively low concentration. Therefore, the conjugate and the polyelectrolyte complex micelle are very useful in basic life science research and the medical field.

Conjugate for gene transfer comprising oligonucleotide and hydrophilic polymer, polyelectrolyte complex micelles formed from the conjugate, and methods for preparation thereof

The present invention relates to the molecular sustained controlled release system constructed by the conjugation of molecules to be released with biodegradable polyester polymer via covalent bond and method for preparation thereof. In accordance with the present invention, the system may be formulated into microspheres, nanoparticles, or films. The molecular release rate from the above system can be regulated to be proportional to the chemical degradation rate of the biodegradable polyester polymers, resulting in near zero order kinetics profile of release without showing a burst effect. Moreover, the high loading efficiency of hydrophilic drugs can be achieved.

Controlled drug delivery system using the conjugation of drug to biodegradable polyester

The present invention relates to a process of preparing a sustained release micelle by copolymerizing a biodegradable polyester hydrophobic polymer and a hydrophilic polyethylene glycol (PEG) to obtain a block copolymer, reacting the block copolymer with a linker to the hydroxyl group of the block copolymer and conjugating the linker-bound block copolymer to a drug to obtain a micelle monomer, and dispersing the micelle monomer an aqueous solution. The drug-micelle conjugate of the present invention has practical application in anticancer therapy.

Process for preparing sustained release micelle employing conjugate of anticancer drug and biodegradable polymer

The present invention relates to a molecular sustained controlled release system constructed by the conjugation of molecules to be released with biodegradable polyester polymer via covalent bond and method for preparation thereof. In accordance with the present invention, the system may be formulated into microspheres, nanoparticles, or films. The molecular release rate from the above system can be regulated to be proportional to the chemical degradation rate of the biodegradable polyester polymers, resulting in near zero order kinetics profile of release without showing a burst effect, Moreover, a high loading efficiency of hydrophilic drugs can be achieved.

Growing community of inventors

Daejeon, South Korea

Tae Gwan Park