Nanoparticle Drug Delivery System Targeting Estrogen Receptors
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Solution Overview
Problem
Current drug delivery systems lack specificity in targeting estrogen receptor-overexpressed cells, such as those in breast, ovarian, and prostate cancers, leading to inefficiencies and side effects due to non-specific binding and immunogenicity concerns with antigen/antibody conjugation.
Innovation Solution
A drug delivery system utilizing nanoparticles composed of lipids, surfactants, charged peptides/proteins, and polymers, conjugated with tamoxifen or its derivatives as ligands to bind specifically with estrogen receptors on cell membranes, triggering endocytosis for targeted drug delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional drugs or nanoparticle drug delivery systems are used, then drugs can be administered to patients, but they cannot specifically target target cells, resulting in low drug efficiency and high side effects
Solution Approach 1:
The patent applies local quality by equipping nanoparticles with specific ligands (tamoxifen or its derivatives) on their surface that can specifically recognize and bind to estrogen receptors on target cells. This localized functional differentiation enables the drug delivery system to selectively target breast cancer cells overexpressing estrogen receptors, thereby improving drug delivery efficiency while reducing side effects through selective accumulation at the disease site.
2Reliability
If antigen/antibody conjugation is used for targeted delivery, then drugs can be delivered to target cells, but the antigen/antibody may induce immunogenicity in the host, resulting in unpredictable consequences
Solution Approach 1:
The patent employs small molecule ligands (tamoxifen and its derivatives) instead of large antigen/antibody conjugates. These small molecules serve as effective targeting ligands without inducing significant immunogenic responses, thus achieving targeted delivery while avoiding the immunogenicity problems associated with antigen/antibody-based approaches.
3Reliability
If ligands are used to bind with specific target receptors on target cells, then drugs can be specifically delivered into target cells, but the ligands must be located on the surface and trigger endocytosis, which limits the choice of ligands
Solution Approach 1:
The patent utilizes tamoxifen and its derivatives, which are well-established antiestrogen drugs with known pharmacological properties. These compounds serve dual functions: they maintain their therapeutic activity against estrogen receptor-positive breast cancer while simultaneously acting as effective targeting ligands that bind to estrogen receptors and trigger endocytosis. This multi-functionality expands the versatility of ligand selection beyond traditional targeting molecules.
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 system significantly enhances drug delivery efficiency into estrogen receptor-overexpressed cells, reducing side effects and improving therapeutic outcomes by specifically targeting and entering cells through receptor-mediated endocytosis.
Implementation Method 1
a plurality of ligand derivatives being able to bind with estrogen receptors on the surface of target cells... capable of inducing endocytosis so as to deliver certain specific matters into target cells
Data Source
AI summary
A vector for targeted delivery of drugs into estrogen receptors over-expressed cells is disclosed. The vector of the present invention is mainly about an active targeting delivery carrier which consists of a plurality of nanoparticles including: (i) a plurality of targeted moiety conjugated to the outer surface of the nanoparticles, the moiety being capable of binding with the estrogen receptor of a target cell, and (ii) bioactive agents encapsulated in the nanoparticles or forming complex with the nanoparticles. The targeted moiety of the present invention can also be conjugated to parent drugs for prodrug design.