ThioMatrix offers a comprehensive range of in vitro/ex vivo studies to support your formulations development or reformulation strategy at any stage of your product development:
Discovery stage
Proof-of-concept studies
Method development
Early phase
Formulation development
Permeation & Mucoadhesion studies
Late phase
Formulation optimization
Compatibility studies
Commercial phase
Life-cycle-reformulation
Fast-track analytics
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In vitro and ex vivo analyses are the foundational steps in developing optimized drug delivery systems. Key parameters such as drug solubility, log P/log D values, stability, and membrane permeability provide the critical data needed to make early strategic decisions—such as determining the optimal route of administration (e.g., oral vs. subcutaneous injection) and selecting the most suitable delivery system. These data also support initial bioavailability estimations.
ThioMatrix brings extensive expertise in formulating poorly soluble APIs. To address solubility challenges, we have developed a rational screening platform that delivers rapid, cost-effective solutions. After conducting solubility screenings and crystallinity assessments, we can enhance API solubility through:
Solid-state modifications (e.g., salt formation, particle size reduction, stabilization of the amorphous state)
Use of co-solvents
Development of lipid-based systems such as microemulsions
Formation of complexes (e.g., cyclodextrins)
Achieving sufficient solubility is a prerequisite for downstream analyses such as permeation studies and the development of effective drug delivery systems.
Permeation studies are conducted using Ussing-type chambers with mucosal membranes (intestinal, nasal, buccal, vaginal) from various species, or using cell monolayers such as Caco-2. These studies provide detailed insights into:
Apparent permeability coefficient (P app )
Route of uptake (transcellular vs. paracellular; active vs. passive transport)
Degree of presystemic metabolism
Membrane toxicity
Impact of permeation enhancers
These findings serve as the basis for:
Initial bioavailability estimations
Molecular optimization (e.g., prodrug strategies, salt form selection)
Route-of-administration decisions
Design of advanced delivery systems
In vitro/ex vivo permeation studies help reduce the need for time-consuming and costly in vivo experiments. ThioMatrix can screen multiple drug candidates within weeks, offering customized service packages that include full data interpretation.
Mucoadhesive drug delivery systems (e.g., ocular inserts, bioadhesive gels) can significantly enhance bioavailability and prolong therapeutic effects. ThioMatrix conducts mucoadhesion studies using methods such as tensile strength testing and the rotating cylinder technique to determine:
Adhesion properties of formulations across different mucosal tissues
Impact of specific excipients on overall mucoadhesion
Expected retention time on target mucosal surfaces in vivo
ThioMatrix performs cytotoxicity assessments to evaluate the safety profile of formulations and excipients. Our testing portfolio includes:
Ciliary beat frequency analysis
LDH leakage assay
Resazurin test
MTT assay
BrdU incorporation test
Red blood cell lysis test
Release of proinflammatory cytokines from various tissues
Protein denaturation tests
Chemical Stability
Understanding the intrinsic chemical stability and identifying degradation products is vital for selecting the appropriate drug candidate and dosage form. ThioMatrix specializes in stress testing and rapid screening to assess chemical stability under various conditions.
Enzymatic Stability
We conduct enzymatic degradation studies using relevant enzymes (e.g., plasma enzymes, mucosal membrane-bound enzymes, intestinal secretions) to assess stability of small molecules, peptides, proteins, and nucleotides. These data supports:
Bioavailability predictions
Rational molecule modification (e.g., amino acid substitution for peptides)
Selection of enzyme inhibitors as excipients
Design of enzyme-protective delivery systems
Storage Stability
ThioMatrix offers ICH-compliant long-term, intermediate, and accelerated stability testing for newly developed dosage forms in their final packaging. Our testing includes physical, chemical, biological, and microbiological evaluations. Available test conditions:
−20 °C
5 °C
25 °C / 60% RH
30 °C / 60% RH
30 °C / 65% RH
40 °C / 75% RH
Photostability
Our climatic chambers are fully calibrated and monitored 24/7 via an automated alert system. Backup systems including emergency generators and additional chambers ensure uninterrupted testing. We provide expert guidance on:
Selection of validated analytical methods
Chemical, physical, and microbiological considerations
Interpretation of test results
Influence of formulation and packaging on stability
Compliance with global regulatory requirements