Vitamin D Transdermal Patch Formulation for Low-Irritation Permeation
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Solution Overview
Problem
Existing chemical enhancers for transdermal drug delivery, particularly for fat-soluble compounds like vitamin D, often cause skin irritation and sensitization, and are not highly effective in increasing permeation rates without adverse effects.
Innovation Solution
A transdermal patch formulation comprising a backing layer, an adhesive drug reservoir layer with vitamin D, a polymeric adhesive, an organic solvent, and a permeation enhancer, such as transcutol, which enhances skin permeability without causing irritation or sensitization.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If high levels of chemical penetration enhancers are used to increase drug permeation rate, then the permeability of stratum corneum is enhanced, but skin irritation and sensitization problems occur
Solution Approach 1:
The patent changes the chemical parameters of the penetration enhancer by using lower concentrations (1-15 wt%) of safer chemicals like transcutol, isopropyl myristate, or ethyl oleate instead of high concentrations of traditional enhancers. This parameter change maintains effective drug delivery while reducing skin irritation and sensitization risks
Solution Approach 2:
The patent employs composite formulation strategies by combining multiple ingredients including polymeric adhesives (polyisobutylene, silicone, or acrylate), organic solvents (ethanol, isosorbide dimethyl ether, isopropyl laurate, or methyl laurate), and permeation enhancers in specific ratios. This composite approach achieves effective vitamin D transdermal delivery without requiring high levels of单一 penetration enhancers, thereby reducing skin damage while maintaining productivity
2Productivity
If traditional transdermal delivery methods are used for fat-soluble compounds like vitamin D, then the delivery system is simple, but the permeation rate through skin is extremely low
Solution Approach 1:
The patent uses composite material formulation combining polymeric adhesive, organic solvent, and permeation enhancer in specific ratios to achieve effective transdermal delivery of fat-soluble vitamin D. This composite approach overcomes the low permeation rate barrier while maintaining manageable formulation complexity through systematic ingredient selection
Solution Approach 2:
The patent changes the formulation parameters by incorporating specific organic solvents and permeation enhancers that are compatible with fat-soluble vitamin D, thereby dramatically increasing the permeation rate through skin while keeping the formulation structure relatively simple and manufacturable
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 patch effectively delivers vitamin D through intact skin with high permeation rates, increasing serum levels efficiently and safely, suitable for subjects with vitamin D malabsorption conditions like cystic fibrosis or after bariatric surgery.
Implementation Method 1
compounds that are administered along with the drug (or in some cases the skin may be pretreated with a chemical enhancer) in order to increase the permeability of the stratum corneum, and thereby provide for enhanced penetration of the drug through the skin
Implementation Method 2
The permeability of many therapeutic agents with diverse physicochemical characteristics may be enhanced using these chemical enhancement means
Data Source
AI summary
Compositions and methods for delivering vitamin D to a subject. In one embodiment the invention provides a transdermal patch for the transdermal administration of vitamin D comprising: (a) a backing layer that serves as the outer surface of the patch during use; (b) an adhesive drug reservoir layer for affixing the patch to skin; and (c) a release liner, which upon removal exposes the adhesive drug reservoir layer. The adhesive drug reservoir layer can include vitamin D, a polymeric adhesive, an organic solvent, and a permeation enhancer.