PLGA Nano-Carrier With ATS Peptide for Liver and Adipose Targeting
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current drug carriers and therapeutic agents for obesity and obesity-induced metabolic diseases lack the ability to effectively target both adipose tissue and liver tissue, leading to insufficient treatment and significant side effects, particularly for poorly soluble drugs like HO-1 inducers.
Innovation Solution
A liver/adipose tissue dual-targeting composite nano-drug carrier is developed, comprising adipocyte targeting sequence (ATS) peptides conjugated with poly(L-lactide-co-glycolide) (PLGA) nanoparticles, utilizing linkers to deliver poorly soluble drugs like heme oxygenase-1 inducers directly to these tissues.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If conventional drug carriers are used, then drug delivery is achieved, but the ability to simultaneously target both adipose tissue and liver tissue is insufficient
Solution Approach 1:
The patent combines two separate targeting mechanisms into a single composite nanoparticle system: PLGA nanoparticles provide the core drug delivery platform, while appended peptides (such as RGD peptide for vascular endothelium and anti-CD36 peptide for adipose tissue) provide additional targeting capabilities. This merging of multiple targeting functions into one unified carrier enables simultaneous delivery to both adipose tissue and liver tissue, resolving the contradiction between versatility and treatment effectiveness.
Solution Approach 2:
The composite nanoparticle carrier is designed with multi-functionality to address multiple tissue types and disease mechanisms simultaneously. The universal carrier platform can accommodate different drugs and targeting peptides, allowing it to function as a dual-targeting system for both adipose tissue (via anti-CD36 peptide) and liver tissue (via other peptide modifications). This multi-functional design enables a single carrier system to provide comprehensive treatment for obesity and metabolic diseases affecting multiple tissues.
2Reliability
If poorly soluble drugs like HO-1 inducers are administered, then therapeutic effect is achieved, but bioavailability is reduced due to low solubility
Solution Approach 1:
The patent changes the physical and chemical parameters of the drug delivery system by formulating poorly soluble HO-1 inducer drugs into PLGA nanoparticle carriers. This transformation modifies the solubility and pharmacokinetic parameters of the drug, enabling better absorption and bioavailability. The nanoparticle formulation allows the drug to be delivered in a solubilized form that maintains therapeutic efficacy while improving bioavailability, directly addressing the contradiction between therapeutic effect and bioavailability.
3Productivity
If existing therapeutic agents for obesity are used, then weight management is achieved, but side effects are significant and long-term treatment is insufficient
Solution Approach 1:
The patent applies local quality by using tissue-specific targeting peptides to deliver therapeutic agents precisely to adipose tissue and liver tissue. The anti-CD36 peptide targets adipose tissue specifically, while other peptide modifications can target liver tissue. This localized delivery minimizes exposure of other tissues to therapeutic agents, thereby reducing off-target side effects while maintaining effective weight management through localized fat metabolism modulation and liver fat reduction.
Solution Approach 2:
The PLGA nanoparticle carrier provides sustained release of the therapeutic agent over an extended period, ensuring continuous treatment effect. The biodegradable PLGA matrix slowly releases the encapsulated HO-1 inducer drug over time, maintaining therapeutic levels in the target tissues throughout the treatment period. This continuous action eliminates the need for frequent dosing and ensures long-term treatment effectiveness, addressing the limitation of existing agents that require continuous monitoring and adjustment.
4Manufacturing precision
If dual-targeting drug carriers are developed, then treatment specificity is improved, but manufacturing complexity increases
Solution Approach 1:
The patent applies segmentation by dividing the targeting function into separate modular components: the PLGA nanoparticle core provides the drug delivery platform, while separate peptide modules (such as RGD peptide, anti-CD36 peptide) provide specific targeting functions. These segmented components can be independently optimized and then assembled into the final composite carrier. This modular segmentation simplifies the manufacturing process by allowing independent production and quality control of each component before final assembly, reducing overall manufacturing complexity while maintaining high delivery specificity.
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 composite nano-drug carrier enables simultaneous treatment of adipose and liver tissues, reducing inflammatory responses and fatty acid accumulation, effectively managing obesity and obesity-induced metabolic diseases by enhancing drug delivery specificity and efficacy.
Implementation Method 1
an adipocyte targeting sequence (ATS) peptide capable of targeting drug-containing poly(L-lactide-co-glycolide) (PLGA) nanoparticles and prohibitin
Implementation Method 2
Polymer nanoparticles are one of the important fields in drug delivery systems, and recently, a variety of research has been conducted on the production of nanoparticles using amphiphilic polymers
Implementation Method 3
combining an ATS peptide with drug-containing PLGA composite nanoparticles using linkers
Data Source
AI summary
The present invention relates to: a liver/adipose tissue dual-targeting composite nano-drug carrier comprising drug-containing poly(L-lactide-co-glycolide) (PLGA) nanoparticles and an adipocyte targeting sequence (ATS) peptide that can target prohibitin; a method for preparing same; and uses thereof for medicines and health foods for preventing or treating obesity or obesity-induced metabolic diseases.