Hydrogen-Bonded Carboplatin Complex for Stable Low-Toxicity Delivery
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Solution Overview
Problem
Existing platinum-based anticancer drugs face issues with stability in aqueous solutions, toxicity, and drug resistance, which hinder their clinical applications and effectiveness in tumor treatment.
Innovation Solution
A carboplatin complex is formed through self-assembly with 1,1-cyclobutanedicarboxylic acid via hydrogen bonds, enhancing stability, reducing toxicity, and improving bioavailability, while maintaining antitumor efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If carboplatin is used as an anticancer drug, then antitumor efficacy is improved compared to cisplatin, but water solubility and stability are reduced
Solution Approach 1:
The patent creates a supramolecular composite material by combining carboplatin with 1,1-cyclobutanedicarboxylic acid through hydrogen bonding. This composite structure (carboplatin 4.0) integrates the antitumor properties of carboplatin with the solubility-enhancing characteristics of the cyclobutanedicarboxylic acid component, thereby improving water solubility while maintaining therapeutic efficacy.
Solution Approach 2:
The 1,1-cyclobutanedicarboxylic acid acts as an intermediary molecule that mediates between the hydrophobic carboplatin core and the aqueous environment. Through hydrogen bonding interactions, this intermediary component facilitates better solubility and stability in water without compromising the antitumor activity of the carboplatin moiety.
2Adaptability or versatility
If platinum-based drugs are administered to overcome drug resistance, then treatment options are expanded, but toxic side effects increase
Solution Approach 1:
The patent applies local quality modification by selectively enhancing the solubility and stability properties of specific regions of the drug molecule through hydrogen bonding with 1,1-cyclobutanedicarboxylic acid. This localized modification improves pharmacokinetic properties and reduces systemic toxicity while preserving the DNA-binding antitumor activity at the molecular level.
3Object-affected harmful factors
If carboplatin is modified to reduce toxicity, then side effects are decreased, but drug stability in aqueous solutions worsens
Solution Approach 1:
The patent resolves this contradiction by forming a supramolecular composite where carboplatin is associated with 1,1-cyclobutanedicarboxylic acid through hydrogen bonds. This composite structure maintains the low toxicity profile of carboplatin while the additional cyclobutanedicarboxylic acid component provides enhanced aqueous stability and solubility, counteracting the inherent instability of modified platinum compounds.
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 carboplatin complex, or carboplatin 4.0, achieves improved stability, reduced toxicity, and broader clinical indications, including platinum-resistant tumors, with enhanced bioavailability and targeted drug delivery.
Implementation Method 1
1,1-cyclobutanedicarboxylic acid molecules are introduced into a carboplatin molecule through bonding of hydrogen bonds
Implementation Method 2
the self-assembly of carboplatin and 1,1-cyclobutanedicarboxylic acid is achieved, thereby preparing the target product with a purity or content as high as possible
Data Source
AI summary
Provided are a carboplatin complex and a pharmaceutical preparation thereof. The carboplatin complex is a complex formed by combining carboplatin and 1,1-cyclobutanedicarboxylic acid through two hydrogen bonds, each of the two hydrogen bonds is formed between a carbonyl oxygen of a carboplatin molecule and a carboxyl hydrogen of a 1,1-cyclobutanedicarboxylic acid molecule. The present invention further provides use of the carboplatin complex in manufacture of an antitumor drug, an antibacterial drug, an antifungal drug, or an antiviral drug, and a quality control method for the carboplatin complex.