Spray-Dried Nanoparticle Compositions for Transmucosal Delivery
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Solution Overview
Problem
Current formulations for transmucosal administration of active agents like progesterone and mometasone are inconvenient, unstable, and limited in emergency situations, requiring special equipment and preparation, while intravenous administration is not suitable for rapid or direct delivery to the intended site of action.
Innovation Solution
Development of dry pharmaceutical compositions comprising spray-dried particles with active agent nanoparticles, a binder, and a pharmaceutically acceptable carrier, optimized for intranasal or intravaginal administration, ensuring controlled particle size distribution for enhanced absorption and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If intravenous administration is used for systemic effect, then the active agent can be delivered effectively, but it requires special medical equipment and trained health care providers, making it inconvenient
Solution Approach 1:
The patent changes the physical state of the formulation from liquid (intravenous) to dry powder (transmucosal), and modifies the particle size parameters to nanoscale (1-100 nm) to enable mucosal penetration and systemic absorption, thereby achieving effective delivery through a convenient non-invasive route
Solution Approach 2:
The patent introduces mucosal membranes (nasal or vaginal) as an intermediary delivery route between intravenous injection and oral administration, using spray-dried nanoparticle formulations that can penetrate the mucosa and enter the bloodstream, providing a convenient alternative that maintains delivery effectiveness
2Reliability
If intravenous formulations are prepared, then the active agent can be administered, but they are unstable and must be prepared shortly before use
Solution Approach 1:
The patent utilizes phase transition by converting the active agent into nanoparticle form and then into a dry powder formulation through spray-drying, which stabilizes the composition for long-term storage while maintaining the ability to deliver the active agent effectively when administered
Solution Approach 2:
The patent performs preliminary stabilization by formulating the active agent as spray-dried nanoparticles with controlled particle size and surface characteristics before storage, allowing the formulation to be prepared in advance and stored stably without requiring preparation shortly before use
3Adaptability or versatility
If transmucosal administration is used, then it offers an alternative to intravenous administration, but it requires careful formulation to promote absorption via nasal mucosae rather than pulmonary route
Solution Approach 1:
The patent applies local quality by optimizing specific properties of the formulation for nasal mucosal absorption, including particle size (1-100 nm), surface charge, and hydrophilicity, while controlling the spray-drying parameters to ensure particles are delivered to the nasal mucosa rather than the lungs
Solution Approach 2:
The patent changes multiple formulation parameters including particle size (1-100 nm), surface area to volume ratio, and hydrophilic-lipophilic balance to optimize transmucosal absorption while preventing pulmonary deposition, thereby achieving versatile administration with controlled formulation
4Reliability
If spray-dried particles are used with optimized particle size distribution, then absorption is enhanced, but the manufacturing process becomes more complex
Solution Approach 1:
The patent replaces complex mechanical size classification methods with spray-drying technology, where the particle size is controlled by adjusting spray-drying parameters (inlet temperature, outlet temperature, feed rate, nozzle type) rather than requiring multiple stages of milling and sieving, thereby simplifying the manufacturing process while achieving the desired particle size distribution
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 compositions achieve rapid and effective delivery of active agents with improved stability and bioavailability, allowing for convenient, ready-to-use formulations suitable for emergency situations without the need for specialized equipment.
Implementation Method 1
comprising spray-dried particles that comprise active agent nanoparticles, binder, and a pharmaceutically acceptable carrier
Data Source
AI summary
Provided herein are dry pharmaceutical compositions for transmucosal delivery, comprising spray-dried particles that include pharmaceutically active agent nanoparticles, a binder, and a pharmaceutically acceptable carrier, where the active agent nanoparticles have an average particle size diameter prior to spray-drying of less than about 1 μm, and wherein up to 10% of the spray-dried particles have a particle size of less than 10 μm; at least 50% of the spray-dried particles have a particle size of at least about 15 μm; and at least 90% of the spray-dried particles have a particle size of up to about 55 μm. Also provided are methods for making such pharmaceutical compositions and therapeutic methods comprising transmucosally aministering the compositions, such as intranasally or intravaginally.