Injectable Composition for Localized Fat Reduction via Selective Adipocyte Apoptosis
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Solution Overview
Problem
Current methods for reducing localized fat, such as PPC injections solubilized with DCA, cause significant pain and side effects like necrosis, edema, and inflammation due to non-selective cell lysis, affecting muscle cells, fibroblasts, and vascular endothelial cells, leading to discomfort and low compliance.
Innovation Solution
A composition comprising phosphatidylcholine and glycocholic acid or taurocholic acid at a specific molar ratio of 0.7 to 3.0, which selectively induces apoptosis in adipocytes without damaging other cell types, reducing pain and side effects by stabilizing the formulation and ensuring safe subcutaneous injection.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If PPC injection solubilized with deoxycholic acid is used for localized fat reduction, then fat cell loss is induced, but significant pain and side effects occur including necrosis, edema, and inflammation of muscle cells, fibroblasts, and vascular endothelial cells
Solution Approach 1:
The patent changes the chemical parameter by replacing deoxycholic acid with glycocholic acid or taurocholic acid as the solubilizing agent. This parameter change maintains the solubility function while eliminating the harmful non-selective cell lysis effect, thereby resolving the contradiction between fat reduction efficacy and harmful side effects
Solution Approach 2:
The patent uses phosphatidylcholine as a biocompatible, naturally occurring substance that degrades safely in the body. This replaces the more aggressive deoxycholic acid with a substance that provides the necessary solubility and fat-cell targeting function without causing prolonged harmful effects, effectively using a 'softer' alternative that achieves the goal without the severe side effects
2Productivity
If conventional PPC injection is used, then localized fat is reduced, but non-selective cell lysis causes necrosis and inflammation of surrounding tissues
Solution Approach 1:
The patent achieves local quality by making the solubilizing agent (glycocholic acid or taurocholic acid) selectively act on adipocytes while sparing other cell types. This selective action is achieved through the specific biochemical properties of these bile acids that allow them to solubilize phosphatidylcholine and target fat cells without causing the non-selective lysis that occurs with deoxycholic acid, thus maintaining productivity while eliminating harmful factors
3Ease of operation
If deoxycholic acid is used as solubilizing agent, then phosphatidylcholine becomes injectable, but severe pain and edema occur at administration sites
Solution Approach 1:
The patent uses glycocholic acid or taurocholic acid as an intermediary substance that mediates between phosphatidylcholine and the aqueous environment. These bile acids form micelles with phosphatidylcholine, making it injectable, while their specific chemical structure prevents the severe pain and edema reactions caused by deoxycholic acid. The intermediary acts as a bridge that provides solubility without the harmful side effects
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The composition effectively reduces localized fat without pain or edema, significantly minimizing side effects, improving patient compliance and maintaining formulation stability, with an adipocyte-specific action comparable to Kybella's efficacy but with reduced adverse reactions.
Implementation Method 1
The PPC solubilized with the DCA is stably dispersed as a mixed micelles system of less than 10 nm
Implementation Method 2
the composition selectively induces apoptosis in adipocytes without damaging other cell types
Data Source
Figure 1A~1B
Figure 2A~2B
Figure 2C~2D
AI summary
The present invention relates to a composition for reducing localized fat without a pain, edema, and side effect, and a method for preparing the same. More specifically, the present invention relates to a composition comprising glycocholic acid (or a salt thereof) or taurocholic acid (or a salt thereof) and phosphatidylcholine (PPC) at a particular mixing ratio for reducing localized fat without side effects such as a pain, edema, necrosis of muscle cells, fibroblasts and vascular endothelial cells other than adipocytes, anesthesia of administration sites, extensive swelling, erythema, induration, paresthesia, nodule, pruritus, burning sensation, nerve injury, and dysphagia, and a method for preparing the same. The DCA single injectable preparation or PPC injectable preparation in which DCA is mixed as a solubilizing agent, which is the conventional injectable preparations for reducing localized fat, has been known to accompany such side effects as a pain, anesthesia, extensive swelling, localized edema, erythema, induration, paresthesia, nodule, pruritus, burning sensation, dysphagia, and the like due to necrosis of cells caused inevitably by lysing not only adipocytes but also fibroblasts, vascular endothelial cells and skeletal muscle cells. Thereby, patients have been complaining of pain, discomfort and anxiety, with low compliance. On the other hand, the injectable composition for reducing localized fat according to the present invention is a safe and stable formulation, selectively lyses adipocytes, and has an excellent effect on inducing apoptosis of adipocytes, so that it is an excellent composition improving the compliance and quality of patient's life without above-mentioned side effects.