Patent classifications
A61K47/61
AMPHOTERICIN B CONJUGATED STABILIZED GOLD NANOPARTICLES AND USES THEREOF
The present invention relates to conjugates of amphotericin B and gold nanoparticles stabilized with thiohexoses or thiopentoses, and a method to produce said nanoparticles. As the conjugates of amphotericin B to the stabilized gold nanoparticles show several advantages over amphotericin B alone, the present invention is also directed to pharmaceutical compositions comprising said nanoparticles, and to their use for treat fungal and leishmanial infection. These amphotericin B stabilized gold nanoparticles are dispersible in water and are not toxic for mammalian cells differently from free amphotericin B and other currently used amphotericin B preparations. Importantly, the conjugates of amphotericin B and stabilized gold nanoparticles are more efficacious in treating all forms of Cryptococcal infections (planktonic, intracellular and biofilms) than amphotericin B. Additionally, the conjugates are more effective against extracellular and intracellular forms of Leishmania mexicana and Leishmania major. Therefore, amphotericin B conjugated to thiohexose or thiopentose stabilized gold nanoparticles offer safer and better treatment option than free amphotericin B, and in particular for Cryptococcal and Leishmanial infections.
HYALURONIC ACID DERIVATIVE, PHARMACEUTICAL COMPOSITION, AND HYALURONIC ACID DERIVATIVE-DRUG COMPLEX
The present invention provides a hyaluronic acid derivative having a steryl group introduced therein, wherein a ratio Mw/Mn of a weight-average molecular weight Mw to a number-average molecular weight Mn of the hyaluronic acid derivative is 1.11 or more and 10.0 or less.
HYALURONIC ACID DERIVATIVE, PHARMACEUTICAL COMPOSITION, AND HYALURONIC ACID DERIVATIVE-DRUG COMPLEX
The present invention provides a hyaluronic acid derivative having a steryl group introduced therein, wherein a ratio Mw/Mn of a weight-average molecular weight Mw to a number-average molecular weight Mn of the hyaluronic acid derivative is 1.11 or more and 10.0 or less.
HEPARIN NANO DRUG CARRIER SYSTEM LOADED WITH AMINO ANTI-TUMOR DRUG AND PREPARATION METHOD THEREOF
The present invention discloses a heparin nano drug carrier system loaded with an amino anti-tumor drug. The drug carrier system is a conjugate formed by loading the amino anti-tumor drug on a PEGylated heparin molecule. A natural polysaccharide heparin that is biodegradable and has good compatibility and high availability is used as a drug carrier, and by combining PEG modification and the amino anti-tumor drug, nanoparticles have a significantly enhanced anti-tumor therapeutic index and biological safety in in-vivo therapy when compared with free drugs.
HEPARIN NANO DRUG CARRIER SYSTEM LOADED WITH AMINO ANTI-TUMOR DRUG AND PREPARATION METHOD THEREOF
The present invention discloses a heparin nano drug carrier system loaded with an amino anti-tumor drug. The drug carrier system is a conjugate formed by loading the amino anti-tumor drug on a PEGylated heparin molecule. A natural polysaccharide heparin that is biodegradable and has good compatibility and high availability is used as a drug carrier, and by combining PEG modification and the amino anti-tumor drug, nanoparticles have a significantly enhanced anti-tumor therapeutic index and biological safety in in-vivo therapy when compared with free drugs.
SYSTEM FOR CORNEAL CROSS-LINKING AND CORRECTING VISION BY USING LED CONTACT LENS AND EYE DYE
The present invention relates to a system for corneal crosslinking of injured corneas, treating keratoconus, or correcting vision, the system comprising: a hyaluronic acid-dye conjugate; and a contact lens including an LED light source.
In the present invention, a dye is activated by receiving light irradiated from the LED light source of the contact lens so as to generate radicals, thereby generating a covalent bond between amino acid radicals of corneal collagen, and strengthening a collagen layer. In the present invention, the hyaluronic acid-dye conjugate, in which hyaluronic acid is bound to the dye, is used to improve penetration of the dye in the cornea, and the contact lens is used together with the hyaluronic acid-dye conjugate to further improve the penetration of the dye. In addition, the structure of the lens which presses the center of the cornea deforms the shape of the cornea, thereby having a vision correction effect.
Antibody-drug conjugates
An antibody-drug conjugate (ADC) has a structure represented by Formula (I): a pharmaceutically acceptable salt thereof wherein Ab is an antibody without glycans (i.e., the protein portion an antibody); G.sub.1 and G.sub.2 are glycan moieties, which may be the same or different; C.sub.n1 and C.sub.n2 are conjugation moieties, which may be the same or different; L.sub.1 and L.sub.2 are linker moieties, which may be the same or different; D.sub.1 and D.sub.2; are drug units which may be the same or different; and x and y are independently an integer from 0 to 8, provided that x+y≠0.
Antibody-drug conjugates
An antibody-drug conjugate (ADC) has a structure represented by Formula (I): a pharmaceutically acceptable salt thereof wherein Ab is an antibody without glycans (i.e., the protein portion an antibody); G.sub.1 and G.sub.2 are glycan moieties, which may be the same or different; C.sub.n1 and C.sub.n2 are conjugation moieties, which may be the same or different; L.sub.1 and L.sub.2 are linker moieties, which may be the same or different; D.sub.1 and D.sub.2; are drug units which may be the same or different; and x and y are independently an integer from 0 to 8, provided that x+y≠0.
PHOSPHINE-MEDIATED AMINE-AZIDE COUPLING IN IONIC LIQUID FOR BIOCONJUGATION REACTIONS
The use of ionic liquids as a solvent for chemoselective bioconjugation reactions is described. For example, methods of preparing bioconjugates in ionic liquids via a phosphine-mediated azide-amine reaction to form a urea linkage between a biomolecule substrate and a second molecule are described. Methods of preparing bioconjugates with amide or enamine linkages in ionic liquids are also described. The methods can be used to prepare tagged biomolecules, such as dye-tagged proteins, peptides, nucleic acids, or saccharides (e.g., aminosaccharides), for use in various applications; to form biomolecule-polymer conjugates; or to form biomolecule-therapeutic agent conjugates, such as antibody-drug conjugates.
COMPOSITIONS AND METHODS OF PROMOTING CELLULAR HYDRATION
A beverage composition promotes cellular hydration when ingested by a multicellular organism, and includes a carbohydrate clathrate component that includes cyclodextrin, in a concentration of 0.01-5% w/w. A complex-forming compound is also included in a concentration that is less than the clathrate component, and there is an aqueous liquid component, such as still and carbonated aqueous liquids. An inclusion complex is formed with at least some of the clathrate component and at least some of the complex-forming compound and the composition promotes cellular hydration of the multicellular organism when the multicellular organism ingests it. There is also a beverage composition that increases lifespan in the multicellular organism, and methods of promoting cellular hydration and increasing lifespan of the multicellular organism according to a mechanism of action.