Rinse-off Composition with Oil Phase for Hydrophobic API Delivery
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Solution Overview
Problem
Current rinse-off compositions, particularly shampoos, face challenges in delivering hydrophobic and poorly soluble active pharmaceutical ingredients (APIs) effectively due to instability and poor solubility issues, especially for conditions like psoriasis, where APIs like clobetasol propionate require longer application times, which are inconvenient for users.
Innovation Solution
A rinse-off composition comprising an oil phase with hydrophobic APIs dissolved in non-polar, water-immiscible solvents dispersed in an aqueous surfactant matrix, allowing for efficient deposition and diffusion of APIs onto the skin and hair with reduced application time.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If hydrophobic APIs are dissolved in a hydroalcoholic surfactant matrix, then solubility is improved, but application time must be extended to 15 minutes which reduces ease of operation
Solution Approach 1:
The patent changes the solvent parameter from hydroalcoholic to water-immiscible oil phase, which fundamentally alters the solubility mechanism for hydrophobic APIs. This parameter change allows the API to remain soluble while enabling rapid deposition and penetration during normal rinse-off times without requiring extended 15-minute application periods.
Solution Approach 2:
The water-immiscible oil phase acts as an intermediary medium that facilitates the transfer of hydrophobic APIs from the rinse-off composition to the skin/hair surface. This intermediary oil phase enables efficient API delivery during standard rinse-off procedures by mediating between the aqueous composition and the hydrophobic API, eliminating the need for extended application times.
2Reliability
If hydrophobic APIs are used in rinse-off compositions, then therapeutic efficacy is achieved, but composition stability deteriorates due to poor solubility
Solution Approach 1:
The patent creates a composite composition system combining water-immiscible oil phase with hydrophobic API dissolved within it, dispersed in an aqueous rinse-off matrix. This composite structure maintains composition stability by providing a dedicated hydrophobic phase for API dissolution, preventing the instability and precipitation issues that would occur in purely aqueous or hydroalcoholic systems.
Solution Approach 2:
The composition is segmented into distinct phases: a water-immiscible oil phase containing the dissolved hydrophobic API, dispersed within an aqueous rinse-off composition. This segmentation allows each phase to perform its optimal function - the oil phase stabilizes the hydrophobic API while the aqueous phase provides rinse-off characteristics - thereby maintaining overall composition stability.
3Quantity of substance
If insoluble particulates of API are used, then deposition onto scalp occurs, but diffusion to pharmacological site is insufficient reducing productivity
Solution Approach 1:
The patent changes the physical state parameter of the API from insoluble particulate to dissolved state in water-immiscible oil phase. This parameter change enables the API to be delivered in solution form during rinse-off, allowing simultaneous deposition onto the scalp and subsequent diffusion to the pharmacological site of action, thereby improving therapeutic efficiency without sacrificing deposition.
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 composition achieves improved stability and increased deposition of active agents, allowing for effective treatment of conditions like psoriasis with a shorter application time compared to existing products, enhancing user convenience and therapeutic efficacy.
Implementation Method 1
one or more active agents dissolved in the oil phase
Implementation Method 2
the oil phase is dispersed in the aqueous surfactant matrix
Implementation Method 3
aqueous surfactant matrix wherein one or more active agents are dissolved in the oil phase
Data Source
AI summary
The present application relates to a rinse-off composition comprising an oil phase and an aqueous surfactant matrix, wherein one or more active agents are dissolved in one or more non-polar, water-immiscible solvents, and the oil phase is dispersed in the aqueous surfactant matrix. The present application also relates to methods of delivering the active agent(s) to a subject in need thereof topically, for example to the skin, the hair, and scalp. The present application also relates to use of the rinse-off compositions to treat and/or prevent topical conditions such as dermatitis and psoriasis. In some embodiments, the rinse-off compositions of the present application are shampoo compositions.