Nanoparticle Drying with Polymer-Surfactant Redispersion Control
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Solution Overview
Problem
Existing methods for producing pharmaceutical formulations from nanosuspensions result in irreversible aggregation of nanoparticles during drying, leading to poorer dissolution rates and larger particle sizes post-redispersion, often requiring matrix-forming agents that are not necessary.
Innovation Solution
A process involving suspending a pharmaceutical active substance in an aqueous solution of a water-soluble polymer, followed by drying, with the addition of an ionic surfactant to maintain particle size distribution and prevent aggregation, eliminating the need for matrix-forming agents.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If nanosuspensions are dried to produce solid dosage forms, then the active substance is converted into a solid form suitable for dosing, but irreversible aggregation of nanoparticles occurs leading to poorer dissolution rates
Solution Approach 1:
A polymer intermediary is introduced that adsorbs onto the nanoparticle surface during drying, forming a protective layer that prevents irreversible aggregation. The polymer acts as a mediator between the nanoparticle and the drying environment, maintaining particle stability while enabling solid dosage form production.
Solution Approach 2:
The patent modifies the chemical parameters of the suspension by adding specific polymers and surfactants that change the surface properties of nanoparticles. This parameter change prevents aggregation during drying while maintaining dissolution rate, resolving the contradiction between solid form production and dissolution performance.
2Device complexity
If conventional drying methods are used without additional stabilizers, then the process is simpler, but matrix-forming agents are required which increase formulation complexity
Solution Approach 1:
The patent extracts and eliminates the need for matrix-forming agents by using a specialized polymer-surfactant system that provides stabilization without requiring additional matrix components. This takes out the unnecessary complexity while maintaining manufacturing simplicity.
Solution Approach 2:
The polymer system performs multiple functions simultaneously: it stabilizes nanoparticles during drying, prevents aggregation, and eliminates the need for separate matrix-forming agents. This multi-functionality reduces formulation complexity while maintaining process simplicity.
3Stability of the object's composition
If ionic surfactants are added to maintain particle size distribution, then nanoparticle stability is improved, but the formulation requires additional components
Solution Approach 1:
The patent merges the functions of multiple components into a coordinated polymer-surfactant system where the ionic surfactant works synergistically with the polymer. This combination provides enhanced stability while the polymer framework eliminates the need for separate matrix-forming agents, balancing component quantity with stability requirements.
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 process ensures nearly complete redispersibility of nanoparticles with minimal particle size increase, maintaining the original particle size distribution and stability during drying and redispersion, without the use of additional stabilizing agents.
Implementation Method 1
the importance of charged surfactants in respect of the stability of particles during drying
Implementation Method 2
before step B) the pharmaceutical active substance is further contacted with an ionic surfactant
Implementation Method 3
a pharmaceutical active substance coated with an at least partially water-soluble polymer
Implementation Method 4
B) drying the mixture obtained in step A)
Implementation Method 5
Drying processes are often freeze-drying and spray-drying
Data Source
AI summary
A process for producing a pharmaceutical formulation comprises the steps of:A) suspending a pharmaceutical active substance in an aqueous solution of a polymer;B) drying the mixture obtained in step A);wherein in step A) the pharmaceutical active substance is present in the form of particles having a d90 value in the particle size distribution of ≤1 μm and before step B) the pharmaceutical active substance is further contacted with an ionic surfactant.