Oral Peptide Delivery Technology
Oral peptide formulation development is technically distinct from conventional small-molecule formulation. Peptides are susceptible to chemical degradation — including hydrolysis, oxidation, deamidation, and racemisation — under the conditions encountered during manufacturing, storage, and the gastrointestinal environment. These degradation pathways are molecule-specific and must be characterised early in the development program.
Physical stability presents a separate set of considerations. Solid-state properties, polymorphic form, and hygroscopicity influence how a formulation behaves over its shelf life. Moisture uptake can accelerate chemical degradation and alter the physical characteristics of the dosage form. Excipient selection must account for both functional role and compatibility with the active under the conditions of the intended dosage form.
Formulation compatibility — the interaction between the peptide and each excipient — is evaluated systematically through compatibility studies before prototype development begins. The formulation environment, including pH, ionic strength, and the presence of specific functional groups in excipients, can influence degradation rates and must be optimised for the specific molecule.
Dosage-form design integrates the outcomes of pre-formulation characterisation, excipient screening, and compatibility evaluation. The selection of tablet, capsule, or other solid oral format is subject to formulation feasibility for the specific peptide candidate. Not every peptide is suitable for every oral dosage form, and the development program is structured to identify the most technically appropriate path for each molecule.
Storage conditions — temperature, humidity, and light — are defined based on stability data and inform packaging specifications. Analytical verification using HPLC and LC-MS is integrated throughout the development workflow to monitor formulation integrity and batch consistency.
Oral Peptide Formulation Development
ShiLai™ Healthcare's oral formulation development follows a structured workflow from candidate evaluation through to manufacturing-ready documentation. Each stage builds on the outputs of the previous, ensuring that decisions are data-driven and technically justified.
Candidate Assessment
Evaluate the peptide or bioactive molecule for oral formulation feasibility. This includes physicochemical characterisation — molecular weight, solubility, charge, hydrophilicity — and an initial assessment of the program objectives and regulatory context.
Pre-Formulation
Characterise solubility profiles, hygroscopicity, thermal behaviour, and intrinsic stability. Pre-formulation data informs the formulation strategy and identifies potential degradation pathways before excipient selection begins.
Excipient Screening
Identify and evaluate excipients for functional role, compatibility with the active, and regulatory acceptability for the target dosage form. Compatibility studies are conducted under accelerated conditions to detect interactions early.
Dosage-Form Selection
Select the appropriate oral dosage form — tablet, capsule, or other solid oral format — based on pre-formulation data, program requirements, and manufacturing considerations. Selection is subject to formulation feasibility for the specific molecule.
Prototype Development
Prepare prototype formulations with defined composition and process parameters. Prototypes are evaluated for physical properties, content uniformity, and initial stability before progressing to formal stability studies.
Stability Evaluation
Conduct stability studies under defined temperature and humidity conditions. Chemical and physical stability, moisture uptake, and excipient compatibility are monitored analytically to support shelf-life development.
Analytical Verification
Apply HPLC, LC-MS, content assay, and purity testing throughout development to verify formulation integrity and batch consistency. Analytical methods are qualified for the specific molecule and dosage form.
Scale-Up
Transition from prototype to pilot-scale batches with process optimisation, in-process controls, and documentation. Scale-up data supports the manufacturing transfer and batch record development.
OEM Manufacturing
Commercial-scale OEM manufacturing with batch documentation, COA, and packaging support. Programs may be structured as ShiLai™ branded, OEM/private label, or custom formulation depending on partner requirements.
For more on ShiLai™ Healthcare's formulation development capabilities, see Peptide Formulation Development and Peptide CDMO. Peptide Formulation Development and Peptide CDMO.
Oral Dosage-Form Development
The selection of an appropriate oral dosage form depends on the peptide candidate, pre-formulation data, and the intended program context. Not every peptide is suitable for every oral dosage form — dosage-form selection is part of the pre-formulation evaluation and is subject to formulation feasibility for the specific molecule.
Tablets
Compressed solid oral dosage forms. Tablet development requires established compression parameters, excipient compatibility, and disintegration characteristics. Subject to formulation feasibility for the specific peptide candidate.
Capsules
Hard or soft capsule formats for powder, granule, or liquid-fill applications. Capsule selection depends on the formulation strategy, fill characteristics, and moisture sensitivity of the active. Subject to formulation feasibility.
Other Solid Oral Formats
Granules, pellets, and modified-release solid oral formats may be evaluated where the formulation strategy and program requirements support them. Applicability is assessed on a per-program basis.
Custom Oral Formulation Formats
For programs with specific technical requirements not addressed by standard dosage forms, custom formulation approaches are evaluated in collaboration with the B2B partner. Feasibility is assessed prior to development commitment.
Stability & Formulation Optimization
Stability evaluation is a core component of oral peptide formulation development. ShiLai™ Healthcare evaluates stability across multiple dimensions as part of the formulation development program, generating data that supports shelf-life assignment, storage specification development, and packaging selection.
Chemical Stability
Assessment of degradation pathways including hydrolysis, oxidation, deamidation, and racemisation under formulation and storage conditions. Degradation products are characterised by LC-MS.
Physical Stability
Evaluation of solid-state properties, polymorphic form, particle size, and physical changes over time in the dosage form under defined storage conditions.
Moisture Sensitivity
Characterisation of hygroscopicity and moisture uptake using dynamic vapour sorption. Results inform excipient selection, packaging specifications, and storage condition development.
Temperature Stability
Stability profiling under ICH-aligned temperature conditions (accelerated and real-time) to support storage specification development and shelf-life assignment.
Excipient Compatibility
Systematic evaluation of interactions between the active and each excipient under accelerated and real-time conditions, using HPLC and visual inspection.
Packaging Interaction
Assessment of primary packaging material compatibility with the formulation, including moisture vapour transmission, light transmission, and extractables considerations.
Shelf-Life Development
Compilation of stability data to support shelf-life assignment and storage condition specifications for the finished dosage form.
Stability data is compiled to support shelf-life assignment and storage condition specifications for the finished dosage form. Packaging selection is informed by moisture vapour transmission, light sensitivity, and extractables considerations specific to the formulation.
Analytical Verification for Oral Peptide Development
Analytical verification is integrated throughout the oral formulation development workflow. ShiLai™ Healthcare applies established analytical methods to verify formulation integrity, batch consistency, and stability at each stage of development. Methods are qualified for the specific molecule and dosage form.
HPLC
High-performance liquid chromatography for purity, content, and related substance analysis throughout development and manufacturing.
LC-MS
Liquid chromatography–mass spectrometry for identity confirmation, sequence verification, and degradation product characterisation.
Purity Testing
Assessment of related substances and impurity profiles in the formulated product against defined specification limits.
Content / Assay Testing
Quantitative determination of active content in the dosage form against specification, using validated analytical methods.
Stability Testing
Analytical monitoring of stability samples to track chemical and physical changes over time under defined storage conditions.
Batch Documentation
COA and batch records for each manufacturing batch, supporting B2B partner documentation and regulatory requirements.
For peptide-specific analytical testing resources, see Peptide Testing, Peptide HPLC Testing, and Peptide LC-MS Testing.
Oral Peptide OEM & Manufacturing
ShiLai™ Healthcare supports B2B partners through the full oral formulation development and manufacturing pathway. Engagements are structured around the partner's program objectives, regulatory context, and commercial requirements.
ShiLai™ Branded Programs
Formulation programs developed under the ShiLai™ Healthcare brand, with full development and manufacturing documentation.
OEM / Private Label
Custom formulation and manufacturing for B2B partners under their own brand. Packaging, labelling, and documentation support included.
Custom Formulation
Bespoke formulation development for molecules and programs not covered by existing ShiLai™ programs. Feasibility assessed prior to commitment.
Retail pricing is not displayed. All engagements are B2B only. For OEM and CDMO capabilities, see Peptide OEM and Peptide CDMO.
Oral Peptide Development Programs
The following programs are built on the ShiLai™ Oral Peptide Delivery Platform. Each program applies the formulation development, stability, analytical, and manufacturing capabilities described above to a specific molecule.
Oral Retatrutide
Oral dosage-form formulation development program for retatrutide. Pre-formulation, excipient screening, stability evaluation, and analytical verification.
OEM DEVELOPMENTOral NAD
Oral NAD formulation and OEM manufacturing development. Dosage-form engineering, stability evaluation, and analytical verification.
DEVELOPMENT PROGRAMOral Dihexa
Dihexa oral formulation development program. Research-stage B2B program covering pre-formulation, dosage-form development, and stability evaluation.
Can't Find Your Peptide?
The Oral Peptide Delivery Platform supports custom formulation development for molecules not listed above. Contact us to discuss your program requirements.
Discuss Custom Oral FormulationAlternative Peptide Delivery Platforms
The selection of a peptide delivery platform depends on the molecule, program objectives, and manufacturing context. The following comparison covers formulation considerations, dosage-form characteristics, stability, manufacturing complexity, packaging, and development workflow — not medical effectiveness.
| Consideration | Oral Delivery(this page) | Nasal Delivery | Cartridge-Based Delivery |
|---|---|---|---|
| Dosage Form / Device | Tablet, capsule, solid oral | Nasal spray solution or suspension | Lyophilized or liquid cartridge |
| Key Stability Factors | Moisture, temperature, excipient compatibility | pH, tonicity, microbial, container compatibility | Lyophilization cycle, reconstitution, container compatibility |
| Manufacturing | Solid-dose manufacturing; compression or fill-and-finish | Liquid formulation; spray-system integration; fill-and-finish | Lyophilization or liquid fill; cartridge integration; pen assembly |
| Packaging | Blister, bottle, sachet | Spray bottle, pump, cartridge | Cartridge, pen system, secondary packaging |
| Development Workflow | Pre-formulation → excipient screening → prototype → stability → scale-up | Formulation screening → spray-system evaluation → stability → scale-up | Formulation → lyophilization development → cartridge integration → scale-up |
Frequently Asked Questions
Discuss an Oral Peptide Project
ShiLai™ Healthcare works with B2B partners on oral peptide formulation development, stability evaluation, analytical verification, and OEM/CDMO manufacturing. Contact us to discuss your program requirements.
Discuss an Oral Peptide Project