Montelukast Topical Formulation via Cyclodextrin Inclusion
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Solution Overview
Problem
Atopic dermatitis treatment faces challenges due to the instability and photo-sensitivity of montelukast, requiring special handling and the formation of impurities, which complicates its formulation, especially in semi-solid forms, and there is a need for effective topical delivery that addresses the inflammatory mechanisms common with asthma and allergic rhinitis.
Innovation Solution
A topical formulation comprising montelukast or its pharmaceutically acceptable salt combined with a gelling agent and water, or a waterless formulation with an oil, designed to enhance penetration through the skin, utilizing penetration enhancers and specific excipients to stabilize the drug and improve delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If montelukast is formulated in semi-solid forms for topical treatment, then therapeutic efficacy for atopic dermatitis is improved, but formulation complexity increases due to drug instability and photo-sensitivity
Solution Approach 1:
The patent uses cyclodextrins as intermediary molecules to form inclusion complexes with montelukast. The cyclodextrin cavity encapsulates the montelukast molecule, protecting it from light and oxidation while improving formulation stability. This mediator approach allows the unstable drug to be formulated in semi-solid forms without requiring excessive protective measures.
Solution Approach 2:
The patent changes the physical and chemical parameters of montelukast by forming inclusion complexes with cyclodextrins. This transformation alters the drug's solubility, stability, and photosensitivity characteristics, enabling formulation in semi-solid forms while maintaining stability during storage and application.
2Ease of manufacture
If montelukast is exposed to light during handling and storage, then formulation and handling procedures become simpler, but drug stability deteriorates leading to impurity formation
Solution Approach 1:
Cyclodextrins serve as protective intermediaries that encapsulate montelukast molecules, shielding them from light exposure. This inclusion complex formation allows the drug to be handled and stored under normal conditions without requiring special light-protective measures, while maintaining stability.
Solution Approach 2:
The cyclodextrin inclusion complexes provide beforehand protection against light-induced degradation. By pre-encapsulating the montelukast molecules in stable cyclodextrin cavities before exposure to light, the formulation gains inherent stability that prevents impurity formation during storage and handling.
3Reliability
If topical formulation uses penetration enhancers to improve skin penetration, then drug delivery efficacy is improved, but formulation stability may be compromised
Solution Approach 1:
The cyclodextrin inclusion complexes act as stable intermediaries that can be combined with penetration enhancers. The cyclodextrin protects montelukast from degradation while allowing controlled release and penetration enhancement, balancing both stability and efficacy requirements in the topical formulation.
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 formulation effectively penetrates the epidermis, providing significant inhibition of clinical scores and cytokine levels associated with atopic dermatitis, demonstrating improved stability and efficacy compared to placebo and standard treatments like betamethasone valerate.
Implementation Method 1
designed to enhance penetration through the skin, utilizing penetration enhancers and specific excipients to stabilize the drug and improve delivery
Implementation Method 2
Montelukast or a pharmaceutically acceptable salt thereof, in the form of inclusion complexes with cyclodextrins
Data Source
AI summary
A topical formulation comprising Montelukast or a pharmaceutically acceptable salt thereof, a gelling agent and water for the treatment of atopic dermatitis.