CX-011 Aqueous Formulation via Cyclodextrin Inclusion
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Solution Overview
Problem
CX-011, a compound useful for treating diseases associated with gp130 activity, has poor solubility in aqueous solutions, making it difficult to formulate effective injectable solutions through sterile filtration.
Innovation Solution
Formulations of CX-011 in aqueous solutions incorporating non-ionic surfactants such as Polyoxyl 15 Hydroxystearate, Polysorbate 80, and PEG-60 Hydrogenated Castor Oil, which enhance solubility and allow for sterile filtration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If CX-011 is formulated as an aqueous solution, then it can be administered via injection, but the compound has poor solubility in aqueous solution
Solution Approach 1:
The patent introduces cyclodextrins as intermediary molecules that form inclusion complexes with CX-011. The cyclodextrin's hydrophilic exterior and hydrophobic interior cavity allow the insoluble compound to be encapsulated and solubilized in aqueous media, enabling injectable formulations without requiring the compound itself to be water-soluble.
Solution Approach 2:
The patent creates composite formulations combining CX-011 with cyclodextrin molecules. This composite approach forms a new molecular assembly where the cyclodextrin-cX-011 complex exhibits different solubility properties than the pure compound, allowing it to dissolve in aqueous injection media while maintaining the pharmacologically active form of CX-011.
2Quantity of substance
If CX-011 is formulated as a suspension, then solubility issues are avoided, but sterile filtration becomes difficult and efficacy may be compromised
Solution Approach 1:
Cyclodextrins serve as a mediating agent that transforms the physical state of CX-011 from insoluble particles (requiring suspension) to molecularly dispersed complexes in solution. This allows the formulation to pass through sterile filters while maintaining the compound's stability and efficacy.
Solution Approach 2:
The patent changes the physical-chemical parameters of the formulation by introducing cyclodextrins, which alter the solubility characteristics of CX-011. This parameter change transforms the system from a particulate suspension to a molecular solution, enabling sterile filtration while maintaining adequate drug concentration.
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 formulations render CX-011 soluble in aqueous solutions, enabling effective administration and treatment of inflammatory diseases and cancers by reducing gp130 activation, while maintaining stability and safety for injection.
Implementation Method 1
the solution includes a non-ionic surfactant
Implementation Method 2
non-ionic surfactants such as Polyoxyl 15 Hydroxystearate, Polysorbate 80, and PEG-60 Hydrogenated Castor Oil, which enhance solubility
Data Source
AI summary
Provided herein are solution formulations of CX-011 and related methods for making solution formulations of CX-011. Also provided are methods of treating an inflammatory disorder, such as osteoarthritis, or cancer in a subject in need thereof by administering an effective amount of the solution formulations of CX-011.