Bioavailability Enhancement for Insoluble Compounds & PROTAC & Oral Peptides

Advanced Drug Delivery Solutions

Crystal Pharmatech specializes in addressing the unique biopharmaceutical challenges of complex molecules, where nearly 70% of R&D candidates face poor water solubility. Our expertise in crystallization and advanced formulation technologies enables us to overcome these bottlenecks through data-driven strategies.

Solutions for Insoluble Compounds

Bioavailability Enhancement for Insoluble Compounds

Approximately 70% of small-molecule drugs under research are classified as BCS Class II or IV. For these poorly soluble drugs, we employ a variety of specialized solubilization methods to achieve therapeutic goals.

API Salt Form Screening

A cost-effective approach for organic weak acids or bases. Converting these into soluble salts can increase solubility by up to 100x and significantly improve oral bioavailability.

API Micronization

A fluid dynamics-driven process that reduces particle size to the micrometer range. This increases specific surface area, porosity, and surface energy, accelerating dissolution.

Amorphous Solid Dispersion (ASD)

The preferred formulation strategy for insoluble compounds. We utilize two primary platforms:

Spray Drying (SD): A particle engineering technique that handles temperature-sensitive molecules and provides consistent particle size control.
Hot-Melt Extrusion (HME): A continuous, solvent-free manufacturing process that allows for ASD formation.

Solutions for Protein Degraders (e.g. PROTAC)

Formulation Strategies for Protein Degraders (e.g. PROTAC)

PROTAC (Proteolysis Targeting Chimeras) present "BCS Class IV nightmares" due to high molecular weights (MW > 700), low permeability, and poor solubility. We utilize five core strategies to transform these molecules into viable oral delivery candidates:

Solubility & Supersaturation

Salt/Cocrystal Screening: Early screening of 20+ counterions to unlock solubility.
Amorphous Solid Dispersions: Using spray drying to trap the API in a high-energy state with polymers and surfactants to drive supersaturation far beyond physical mixtures and improve wettability.

Lipid Systems & Size Reduction

Lipid-Based Formulations: Utilizing SEDDS and SMEDDS to solubilize lipophilic PROTACs in GI fluids and bypass gut barriers.
Particle Size Reduction: Nano-milling to the sub-micron range to ensure faster dissolution and better systemic exposure.

Permeability Enhancement

Incorporating surfactants or absorption enhancers into the matrix to open tight junctions and move the large molecule across membranes.

Solutions for Oral Peptide Development

Oral Peptide Development

Oral delivery of peptides remains a significant challenge due to their size and susceptibility to degradation. Our enabling formulation platform addresses these hurdles through integrated technologies:

Permeability Enhancement

We utilize specialized matrix components to facilitate the transport of oral peptides and proteins across the intestinal epithelium.

SMEDDS Protection

Self-Microemulsifying Drug Delivery Systems (SMEDDS) are employed to protect the peptide and enhance its absorbability.