Transdermal Silicone Gel Composition for Stable Drug Delivery
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current topical compositions for pain management have limitations such as low viscosity, temperature sensitivity, shear stress, gumming, and hardening, which affect their stability and efficacy, and fail to efficiently deliver a wide range of active compounds uniformly and cosmetically.
Innovation Solution
A transdermal silicone gel (silogel) composition is developed, utilizing a water-in-silicone emulsion system with polymeric surfactants and hydrocolloids, allowing for high water content, stable, and controlled release of pharmaceutical actives, with enhanced spreading and film-forming properties, and improved skin feel.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If traditional topical compositions are used for pain management, then they can deliver active compounds to the skin, but they exhibit low viscosity, temperature sensitivity, shear stress, gumming, and hardening which reduce stability and efficacy
Solution Approach 1:
The patent employs a composite gel composition integrating multiple components: a silicone base polymer providing stability and skin feel, a hydrocolloid component (carboxymethylcellulose sodium) enhancing viscosity and structural integrity, and a surfactant (polysorbate 80) ensuring uniform distribution of active compounds. This composite structure eliminates temperature sensitivity and shear stress issues while preventing gumming and hardening, achieving stable composition without harmful effects.
Solution Approach 2:
The patent optimizes specific parameter ranges to achieve stable composition: silicone base polymer at 5-50%, hydrocolloid at 1-20%, surfactant at 1-10%, and active compounds at 1-50%. By controlling these parameters within defined ranges, the formulation maintains optimal viscosity, prevents phase separation, and eliminates temperature sensitivity and shear stress problems while avoiding gumming and hardening.
2Ease of operation
If high water content is incorporated into the gel composition, then skin feel and spreading properties are improved, but viscosity control and stability become challenging
Solution Approach 1:
The hydrocolloid component (carboxymethylcellulose sodium) acts as an intermediary between water and the silicone base polymer. It increases water content for improved spreading and film-forming properties while simultaneously providing viscosity control and structural integrity. The surfactant (polysorbate 80) further mediates between hydrophilic and lipophilic components, ensuring uniform distribution and preventing phase separation, thus maintaining stability despite high water content.
3Manufacturing precision
If uniform delivery of diverse active compounds is achieved, then therapeutic efficacy is improved, but formulation complexity increases
Solution Approach 1:
The silicone base polymer serves as a universal vehicle capable of dissolving or suspending diverse active compounds including NSAIDs, opioids, adjuvants, and local anesthetics. The surfactant (polysorbate 80) provides multi-functionality by emulsifying both hydrophilic and lipophilic compounds, ensuring uniform distribution throughout the gel matrix. This universal approach enables delivery of diverse actives without requiring separate formulations, reducing overall complexity while achieving uniform delivery.
4Productivity
If transdermal penetration is enhanced, then drug delivery efficacy is improved, but risk of side effects increases
Solution Approach 1:
The gel formulation achieves local quality optimization by maintaining a balanced composition that enhances transdermal penetration of active compounds at the application site while minimizing systemic absorption. The silicone base polymer and hydrocolloid create a controlled release matrix that sustains local drug concentration, improving efficacy. The surfactant ensures uniform distribution, preventing localized hotspots that could increase side effects. This local quality control enables enhanced penetration with reduced side effect risk.
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 silogel composition achieves high viscosity without separation, is not temperature-sensitive, and provides sustained release of active ingredients, improving skin permeation and reducing side effects, with up to 71% of the applied dose penetrating the stratum corneum, compared to standard formulations.
Implementation Method 1
multifunctional polymeric emulsifiers can attach to an interface via several segments. The energy of adsorption is equal to the sum of the interactions of all segments, and can be considerably greater than the energy of individual monomeric surfactants. Hence these multifunctional polymeric emulsifiers can adsorb very strongly at an interface.
Implementation Method 2
Transdermal pharmaceutical delivery compositions, utilizing matrices of a silogel... providing sustained release of active ingredients, improving skin permeation
Data Source
AI summary
A silicone gel (“silogel”) composition used to deliver pharmaceutical products transdermally as well as a method for producing the silogel composition, which may contain up to 80% additive ingredients. Preferred embodiments of the invention may include silogel compositions which provide high viscosity/no separation due to API. They are not temperature-sensitive, have no shear stress from the ointment mill/EMP, have no gumming up/stickiness, and no hardening.