PHEA-BIB-pButMA Nanoparticles for Sorafenib Controlled Release
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Solution Overview
Problem
Sorafenib, a drug used to treat various tumor diseases, has low bioavailability and causes significant gastrointestinal irritation due to its poor water solubility and strong first-pass effect, limiting its clinical application.
Innovation Solution
The development of polymeric nanoparticles, specifically PHEA-BIB-pButMA nanoparticles, loaded with Sorafenib or its derivatives, which are designed for controlled release and targeted delivery to tumor sites, thereby enhancing bioavailability and reducing side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If Sorafenib is administered as orally administered tablets, then the drug can be delivered to patients, but its bioavailability is low due to poor water solubility and strong first-pass effect
Solution Approach 1:
The patent uses polymeric nanoparticles as an intermediary carrier to deliver Sorafenib. The nanoparticles protect the drug from first-pass metabolism and improve its solubility through encapsulation, thereby enhancing bioavailability while reducing the harmful effects of poor water solubility
Solution Approach 2:
The patent changes the physical and chemical parameters of Sorafenib by formulating it within polymeric nanoparticles. This transformation alters the drug's solubility characteristics and absorption profile, improving bioavailability without changing the drug's molecular structure
2Reliability
If Sorafenib is administered as orally administered tablets, then the drug can be delivered to patients, but significant gastrointestinal irritation is associated with administration
Solution Approach 1:
The polymeric nanoparticle acts as a protective intermediary between the drug and the gastrointestinal tract. This carrier system reduces direct contact between Sorafenib and gastric mucosa, thereby minimizing gastrointestinal irritation while maintaining drug delivery efficacy
Solution Approach 2:
The patent employs a polymeric shell structure that encapsulates Sorafenib. This flexible polymeric layer protects the drug from direct interaction with gastrointestinal tissues, reducing irritation while allowing controlled drug release at the target site
3Duration of action of moving object
If Sorafenib is incorporated into dextran/poly(dl-lactide-co-glycolide) copolymer nanoparticles, then controlled release is achieved, but there is no preferential distribution in tumor tissue
Solution Approach 1:
The patent modifies the nanoparticle surface with specific ligands or functional groups that provide local recognition properties for tumor cells. This local quality enhancement enables preferential accumulation in tumor tissue through active targeting mechanisms while maintaining controlled release characteristics
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 Sorafenib-loaded nanoparticles demonstrate improved bioavailability and enhanced efficacy in inhibiting tumor growth, with preferential accumulation in tumor tissues, leading to increased drug efficacy and reduced side effects compared to free Sorafenib.
Implementation Method 1
loaded nanoparticles of Sorafenib (Sorafenib PBB) or Sorafenib derivatives (Sorafenib PBB derivatives), where said nanoparticles are polymeric PBB nanoparticles
Implementation Method 2
controlled release formulation of Sorafenib or Sorafenib derivatives, which comprises Sorafenib PBB or Sorafenib PBB derivatives
Implementation Method 3
The nanoparticles thus obtained were loaded with the drug by means of the dialysis method
Implementation Method 4
preferential accumulation in tumor tissues, leading to increased drug efficacy
Implementation Method 5
designed for controlled release and targeted delivery to tumor sites
Implementation Method 6
The nanoparticles thus obtained were loaded with the drug by means of the dialysis method
Implementation Method 7
loaded with the drug by means of the dialysis method, without the use of surfactants
Data Source
Figure 1
Figure 2A~2C
Figure 3A~3B
AI summary
The present invention relates to loaded nanoparticles of Sorafenib (Sorafenib PBB) or Sorafenib derivatives (Sorafenib PBB derivatives), wherein said nanoparticles are polymeric PBB nanoparticles, (PHEA-BIB-pButMA, α, β-poly (N-2-hydroxyethyl ) -co- {N- 2-ethylene- [2- (poly (butylmethacrylate ) -isobutyrate ] } -D, L- aspartamide, and to a method for obtaining them. The present invention further relates to a controlled release formulation of Sorafenib or Sorafenib, derivatives which comprises Sorafenib PBB or Sorafenib PBB derivatives, and to the use of said formulation in the treatment of tumor diseases of the kidney, liver, thyroid, colon, breast, pancreas, lungs and/or recurrent glioblastoma.