Novel pegylated liposomal formulations of apelin for treatment of cardiovascular-related diseases

A technology of liposomes and therapeutic agents, applied in the field of treatment of cardiovascular-related diseases and diseases, can solve problems such as short plasma half-life

Pending Publication Date: 2019-07-30
AVIVE INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The therapeutic use of apelin has been limited by its significantly short plasma half-life due to the rapid metabolism of the bioactive peptide in the body

Method used

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  • Novel pegylated liposomal formulations of apelin for treatment of cardiovascular-related diseases
  • Novel pegylated liposomal formulations of apelin for treatment of cardiovascular-related diseases
  • Novel pegylated liposomal formulations of apelin for treatment of cardiovascular-related diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Example 1: Pharmacodynamics of Apelin Preparations in a Mouse Model of Myocardial Hypertrophy and Heart Failure

[0096] Animals. C57BL / 6J mice aged 6 to 8 weeks and 8 to 10 weeks were used as pharmacodynamic animal models of transverse aortic constriction (TAC)-induced cardiac hypertrophy and heart failure. Mice were grouped accordingly into treatment groups as shown in Table 3 below. Mice received intraperitoneal injections of 100 μL of PBS (sham group), vehicle-only (liposome) control group, apaline only (formulation B group), or apaline-liposome (formulation C group) .

[0097] Table 3: Mouse Treatment Groups

[0098] therapy group number of animals mock surgical group 6 Control group – liposomes only 6 Formulation Group B – Apelene only 7 Formulation C only – Apelin Liposomes 7

[0099] TAC procedure. Sterilize the surgical field for binocular stereoscopic manipulation. Prepare the incision to reveal the heart and left...

Embodiment 2

[0113] Embodiment 2: Apelin preparation for the treatment of myocardial infarction

[0114] Protocol for animal experiments. Male Sprague-Dawley rats (age, 8 years) weighing 180-220 g were obtained from standard sources. Rats were maintained in a temperature-controlled (20-22° C.) environment on a 12-hour light-dark cycle. Rats were divided into three groups (n=6 / group) as follows: sham operation; left anterior descending artery (LAD) ligation group; and LAD+apalene group. The Apelene group received Apelene liposomes according to the formulation illustrated in Table 4 below.

[0115] Table 4: Therapeutic formulations

[0116]

[0117] Rats in the LAD group underwent LAD ligation (Patten 1998; Ahn 2004). Briefly, rats were anesthetized with 10% chloral hydrate (3.5 ml / kg) via intraperitoneal injection. In the supine position, endotracheal intubation was performed and rats were ventilated using a rodent ventilator (rate, 80 breaths / min; tidal volume, 6-8 ml / kg). The c...

Embodiment 3

[0119] Embodiment 3: Apelene preparation is for the treatment of pulmonary arterial hypertension (PAH)

[0120] Twenty patients with PAH will participate in a randomized, double-blind, placebo-controlled study of Apelin liposomes and matching saline placebo injections during right heart catheterization (Vestbo 2013; Vestbo 2015). The Apelene group received Apelene liposomes according to the same formulation as illustrated in Table 4 above.

[0121] Measure mean pulmonary artery pressure, pulmonary artery wedge pressure, and cardiac output. Treatment with liposomal apelene is expected to result in an increase in cardiac output.

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Abstract

The disclosure relates generally to compositions comprising pegylated liposomal formulations of apelin for the treatment of cardiovascular-related diseases.

Description

[0001] priority statement [0002] This application claims priority to US Provisional Application 62 / 410,160, filed October 19, 2016, and US Provisional Application 62 / 464,594, filed February 28, 2017, which are hereby incorporated by reference in their entirety. technical field [0003] The present disclosure provides compositions of apelin, eg, pegylated liposomal formulations of apelin, and methods for treating cardiovascular-related diseases and disorders. Background technique [0004] Apelin is the endogenous ligand for G-protein-coupled APJ receptors that regulate various biological functions, including fluid homeostasis, blood pressure, cardiac development and function, and multivascular remodeling. The therapeutic use of apelin has been limited by its significantly short plasma half-life due to the rapid metabolism of the bioactive peptide in vivo. [0005] Therefore, there remains a need for formulations of apelene with enhanced stability and therapeutic efficacy. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7088A61K38/10A61K38/16
CPCA61K45/06A61K9/1271A61K9/19A61K38/1709A61P11/00A61P13/12A61P15/10A61P3/10A61P9/00A61P9/04A61P9/10A61P9/12A61K47/28A61K47/10A61K9/1277A61K47/24
Inventor J·拉贾达斯
Owner AVIVE INC
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