Solid Shaped Masses for Oral Protein Delivery
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Solution Overview
Problem
Many proteins and peptides used in pharmaceuticals face challenges in being formulated into solid forms for oral or other delivery methods without losing their bioactivity, as fabrication processes like molding, compression, or encapsulation can disrupt their complex structures, leading to reduced biological efficacy.
Innovation Solution
The development of pharmaceutical compositions in the form of solid shaped masses, where proteins or polypeptides are combined with excipients like drug sequestering polymers and lubricants, allowing for compression or other shaping methods that minimize bioactivity loss, and utilizing water-swellable polymers to control release through pH changes or enzymatic degradation in the GI tract.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If proteins are subjected to conventional fabrication processes like molding or compression to form solid shapes, then the drug can be delivered in a stable solid form, but the biological activity of the protein is lost due to structural disruption
Solution Approach 1:
The patent combines proteins with excipients including hydrophilic polymers, lipids, and surfactants to create a composite material system. This composite structure provides mechanical stability for solid form while the excipients protect the protein structure from denaturation during fabrication processes, thus maintaining biological activity alongside structural stability
Solution Approach 2:
The patent employs controlled parameter changes during fabrication, including maintaining specific temperature ranges, pH levels, and moisture content. These controlled parameter changes allow the protein to undergo phase transitions or structural adjustments that result in stable solid forms while preserving the native conformation and biological activity of the protein
2Ease of manufacture
If compression forces are applied to form solid masses, then the drug can be delivered in a convenient solid dosage form, but the protein structure is disrupted leading to bioactivity loss
Solution Approach 1:
The patent applies preliminary actions by pre-forming the protein-excipient mixture into a molded shape before compression, and by selecting excipients that pre-protect the protein structure. This preliminary protection and shaping reduces the compression force needed and minimizes structural disruption during the compression step
Solution Approach 2:
The patent uses excipients as intermediary substances between the compression force and the protein. These excipients including polymers and lipids act as cushioning agents that distribute compression forces uniformly and prevent direct mechanical stress on the protein structure, thereby maintaining biological activity while enabling solid form fabrication
3Ease of operation
If proteins are formulated into solid forms for oral delivery, then the drug can be administered orally, but the protein is degraded by GI tract secretions
Solution Approach 1:
The patent applies beforehand cushioning by incorporating protective excipients such as enteric coatings, hydrophilic polymers, and lipids that form protective barriers around the protein before oral administration. These protective layers cushion the protein from harsh GI conditions including acid and enzymatic degradation, enabling successful oral delivery while preserving protein integrity
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
This approach preserves at least 70% of the biological activity of proteins or peptides post-formation and allows controlled release, effectively maintaining therapeutic efficacy while avoiding degradation by GI tract secretions, enabling oral delivery of sensitive therapeutic agents.
Implementation Method 1
utilizing water-swellable polymers to control release through pH changes or enzymatic degradation in the GI tract
Data Source
AI summary
Embodiments of the invention provide shaped masses (SM) comprising one or more drugs such as proteins or polypeptides and methods for forming and delivering such SM's. One embodiment provides a SM comprising a drug e.g., a protein or polypeptide having a biological activity in the body of a mammal. The SM is formed by compression of a precursor material (PM) comprising the drug wherein an amount of biologically active drug in the SM is a minimum level to that in the PM. Drugs which may be incorporated into the SM include insulin, incretins and immunoglobulins e.g., interleukin neutralizing antibodies or TNF-α-inhibiting antibodies. Embodiments of the invention are particularly useful for the oral delivery of drugs which would be degraded within the GI tract, wherein the SM containing the drug is formed as or incorporated into a tissue penetrating member which is inserted into the intestinal wall after oral ingestion.