A61K49/0082

Targeted Shell for Use in Drug Delivery System Utilizing Carbosilane Dendrimer
20180362718 · 2018-12-20 ·

The present invention is related to a targeted type shell for drug delivery system. The object of the present invention is to provide the targeted type shell for DDS, which comprises a carbosilane dendrimer containing a silole produced by which is formed by utilizing the reaction between thiol group and alkyl halide, and a targeted protein containing a labeled proteins such as green fluorescent protein with a target recognition site. The shell may incorporate compounds having a variety of molecular weight and biopolymers, and selectively deliver them into targeted cells.

HYPOXIA-TARGETED POLYMERIC MICELLES FOR CANCER THERAPY AND IMAGING

The present invention provides a composition and method for targeting hypoxic tumor areas for detection or treatment or a treatment adjuvant for cancer. Specifically, a hypoxia targeting moiety is conjugated to a polymeric micelle containing imaging agents, therapeutic agents, or therapeutic adjuvants.

Uniform, Functionalized, Cross-Linked Nanostructures for Monitoring pH

Fluorescence methods and systems that use an optical agent for measuring the pH of a fluid. The optical agent is a photonic nanostructure having a supramolecular structure, such as a shell cross-linked micelle that incorporates at least one linking group that includes one or more photoactive moieties.

Fluorocoxib A loading into ROS-responsive nanoparticles

Disclosed are compositions that comprise a cyclooxygenase-2-selective therapeutic and/or diagnostic agent having a therapeutic and/or diagnostic agent conjugated to a NSAID drug; and a ROS-responsive nanoparticle. Methods of making and using these compositions for drug encapsulation and delivery are also disclosed.

NOVEL BLOCK COPOLYMER AND MICELLE COMPOSITIONS AND METHODS OF USE THEREOF

Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises

##STR00001##

wherein R is H or CH.sub.3, wherein R is NR.sup.1R.sup.2, wherein R.sup.1 and R.sup.2 are alkyl groups, wherein R.sup.1 and R.sup.2 are the same or different, wherein R.sup.1 and R.sup.2 together have from 5 to 16 carbons, wherein R.sup.1 and R.sup.2 may optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.

Methylene blue nanoparticle for bioimaging and photodynamic therapy and use thereof
10086075 · 2018-10-02 · ·

The present invention relates to a methylene blue nanoparticle for bioimaging and photodynamic therapy, and a use thereof as a cancer therapeutic agent and a contrast agent. The methylene blue nanoparticle of the present invention for use as a topical cancer targeting photo therapeutic agent is composed of only a material of which the composition is clinically used or derived from human bodies, and thus a nanopreparation in which a barrier to clinical entry is low and the possibility of commercialization is very high, exhibits near-infrared fluorescence along with cancer targeting property, capacity of generating singlet oxygen and the like, and thus may be used for both bioimaging diagnosis such as optical imaging, and cancer targeting photodynamic therapy.

Block copolymer and micelle compositions and methods of use thereof

Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises ##STR00001##
wherein R is H or CH.sub.3, wherein R is NR.sup.1R.sup.2, wherein R.sup.1 and R.sup.2 are alkyl groups, wherein R.sup.1 and R.sup.2 are the same or different, wherein R.sup.1 and R.sup.2 together have from 5 to 16 carbons, wherein R.sup.1 and R.sup.2 may optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.

Surfactant microbubbles compositions and process for preparing thereof

The present invention provides methods for preparing acoustically-sensitive microbubbles. The method includes the steps of: i) preparing a first surfactant solution comprising a first micelle-forming surfactant at a concentration above the critical micelle concentration (CMC); ii) adding one or more pharmaceutical compounds in a solvent to the first surfactant solution, thereby loading the micelles with the one or more pharmaceutical compounds; iii) preparing a second surfactant solution comprising a second surfactant, wherein the second surfactant comprises one or more matrix forming surfactants; iv) adding heat to the second surfactant solution to melt the surfactant and allowing the mixture to cool under rapid stirring; v) combining the second surfactant solution with the loaded micelles; vi) purging the surfactant mixture with a purging gas; vii) agitating the purged mixture under a constant stream of the purging gas; and, viii) separating the formed microbubbles by size.

ENZYME-RESPONSIVE POLYMER PEPTIDE AMPHIPHILES FOR TARGETED DRUG DELIVERY TO TREAT LOCAL AND SYSTEMIC INFLAMMATION

Micellar particles formed of a plurality of block copolymers, compositions comprising same, copolymers used to form the particles, and polymeric aggregates formed therefrom are provided. The micellar particles are for use in the treatment of inflammation, including chronic inflammation. The block copolymers forming the particles include at least a first block and a second block. The first block has an anti-inflammatory agent covalently attached, directly or via a linking moiety or group, to at least a portion of its backbone units; and the second block has a hydrophilic moiety that comprises an amino acid sequence that is capable of interacting with an inflammatory biomarker covalently attached to at least a portion of its backbone units, and the particle features a core made of the first block and a hydrophilic shell made of the second block.

Micelles for Mucoadhesive Drug Delivery

Biocompatible block copolymer micelles for use in mucoadhesive drug delivery are provided. The micelles comprise a degradable hydrophobic polymer, a degradable synthetic hydrophilic polymer and a mucoadhesive polymer. The micelles are particularly useful for ophthalmic uses.