A61K9/1277

NANODROPLET WITH LAYER-BY-LAYER ASSEMBLY
20220409750 · 2022-12-29 ·

The present disclosure provides novel modified nanodroplets with a layerby-layer (LBL) assembly formulation (“LBLnNDs”). The LBLnNDs of the present disclosure comprise gaseous perfluorocarbon core, polymer shell, and multiple alternating positively and negatively charged biopolymer layers dispersed layerby-layer onto the shell of the LBLnNDs. Methods of making and use of the LBLnNDs are also provided.

Methods for the preparation of a pharmaceutical-vesicle formulation and associated products and uses

The invention relates to methods for the preparation of a pharmaceutical-vesicle formulation comprising steps of: preparing and processing vesicle components and a pharmaceutical agent to entrap the pharmaceutical agent in the vesicle and form a pharmaceutical-vesicle formulation, wherein the pharmaceutical-vesicle formulation is reconstituted in a known quantity of the pharmaceutical agent dissolved in a pharmaceutically-acceptable carrier to provide a biphasic pharmaceutical-vesicle formulation. The invention also relates to the associated pharmaceutical-vesicle formulations, pharmaceutical kits and uses as a medicament, in particular for the prevention or treatment of infection by bacteria such as Burkholderia pseudomallei and Francisella tularensis, and viruses such as Venezuelan Equine Encephalitis Virus (VEEV).

TRANSMEMBRANE PORES FORMED BY AROMATIC OLIGOAMIDE FOLDAMERS AND USES OF SAME
20220380301 · 2022-12-01 ·

Provided are aromatic oligoamide foldamers and self-assembled compositions of the same. The aromatic oligoamide foldamers and compositions can form tube-like structures that can form pores in membranes. The pores can be used to transport ions and molecules, such as, for example, cryoprotective agents or therapeutic agents, through the membrane. The tube-like structures exhibit desirable stability at low temperatures.

CABAZITAXEL WEAKLY- ALKALINE DERIVATIVE AND FORMULATION THEREOF

A cabazitaxel weakly-alkaline derivative, preparation, and synthesis thereof, a liposome preparation containing the cabazitaxel weakly-alkaline derivative and application of the cabazitaxel weakly-alkaline derivative in a drug delivery system are provided. Cabazitaxel is connected with a weakly-alkaline intermediate through an ester bond, the ester bond can be broken under the action of esterase in vivo, and an active drug is released. A connecting group is C.sub.1-C.sub.4 alkyl, C.sub.3-C.sub.6 naphthenic base or phenyl; [N] is an N-methyl piperazinyl group, a piperidinyl group, a 4-(1-piperidinyl) piperidinyl group, a morpholinyl group, a pyrrolidine group or other tertiary amine structures. The cabazitaxel weakly-alkaline derivative can be prepared into the liposome preparation having high drug loading capacity, high encapsulation efficiency, and good stability. The in-vivo circulation time of the drug can be greatly prolonged, the accumulation amount of the drug at a tumor part is increased, and the anti-tumor effect and the tolerance dose are improved.

Vesicles comprising epidermal growth factor and compositions thereof

The invention relates to vesicles comprising Epidermal Growth Factor (EGF), a cationic surfactant and cholesterol or derivatives thereof. The invention also discloses a procedure for their preparation, based on compressed fluid technology (CFs). The vesicles of the invention are useful in the manufacture of drugs and cosmetics and in tissue engineering.

In vivo targeting of extracellular vesicles

A method for chemically induced homing of extracellular vesicles (EVs) to a specific tissue or organ in a subject for either treatment or diagnosis of a medical condition, the method comprising administering to the subject an amount of a homing agent. The homing agent is at least one of a derivative of poly(ethylene glycol), or a derivative of phenothiazine. The EVs are homed to the homing agent in the subject.

Method for preparing liposome comprising ultrasound reactive microbubble for drug delivery and liposome using same

Provided are a method for preparing liposomes comprising ultrasound reactive microbubbles for drug delivery, comprising (a) a step of producing ultrasound reactive microbubbles comprising an inert gas therein and having a first shell formed on the outer surface thereof, followed by forming a uniform size distribution of the ultrasound reactive microbubbles through an extruder; and (b) a step of producing liposomes comprising the ultrasound reactive microbubbles distributed in a uniform size and a medicament therein and having a second shell formed on the outer surface thereof, followed by forming a uniform size distribution of the liposomes through an extruder; and a liposome using same.

CAPE-LOADED TARGETED MICROVESICULAR CANCER DRUG AND METHOD FOR DEVELOPING THE SAME

A method of producing a caffeic acid phenethyl ester loaded microvesicular cancer drug targeting SH-SY5Y neuroblastoma cancer. The method includes seeding a plurality of skin stem cells in a medium; enabling the plurality of skin stem cells in the medium to reach a confluency of 70-80% to be seeded in a plurality of culture plates; preparing a caffeic acid phenethyl ester stock solution by dissolving the caffeic acid phenethyl ester in dimethyl sulfoxide DMSO; performing a microvesicle isolation from specialized skin cells; adding the caffeic acid phenethyl ester into a plurality of microvesicles; and separating the caffeic acid phenethyl ester loaded microvesicles from the caffeic acid phenethyl ester which is free in the solution and not loaded to a microvesicle.

DRY LIPOSOME FORMULATIONS AND RELATED METHODS THEREOF

Described herein are dry powder compositions of liposomes. Formulations containing a cryoprotectant can be converted to dry powders using, e.g., thin-film freeze-drying (TFFD) to obtain stabilized composition that show improved properties.

Remote loading of sparingly water-soluble drugs into lipid vesicles

The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL). In the preferred embodiment the drug in the solubilizing agent is mixed with the liposomes in aqueous suspension so that the concentration of solubilizing agent is lowered to below its capacity to completely solubilize the drug. This results in the drug precipitating but remote loading is capability retained. The process is scalable and the resulting drug-loaded liposomes are characterized by a high drug-to-lipid ratios and predictable drug retention when the liposome encapsulated drug is administered in patients.