Intestinal and Skin Permeability Testing: Accelerate Drug Development with Validated Assays

Base Científica
Oct 18
7 min read

Validated Caco-2 and HaCaT Methods for Formulation Optimization and Strategic Decisions in Biotechnology

Drug development represents one of the greatest challenges facing the modern pharmaceutical industry. It requires millions of dollars in investment and years of research before a product reaches the market. In this scenario, intestinal and skin permeability tests emerge as fundamental strategic tools. They provide essential predictive data that allows biotechs, pharmaceutical companies, and laboratories to make informed decisions about the viability of their drug candidates.

These trials are not just another item on the list of preclinical studies. They represent a strategic investment that can determine the success or failure of a research and development project. By providing accurate data on how compounds cross critical biological barriers, these tests allow for early identification of bioavailability problems. If discovered only in advanced clinical stages, these problems can result in losses of millions of dollars.

Why are Permeability Tests Essential for your R&D?

The reality of pharmaceutical development is relentless. Only a small fraction of the compounds that enter preclinical development reach the market. Many failures occur due to absorption and bioavailability issues that could have been identified early through appropriate permeability testing.

Risk and Cost Reduction

The numbers speak for themselves. Phase I clinical trials can cost between R$5 million and R$15 million. Meanwhile, permeability tests represent a tiny fraction of this investment. More importantly, they can:

Eliminate unsuitable candidates before larger investments.
Guide structural modifications to improve absorption.
Optimize formulations based on solid scientific data.
Significantly reduce time-to-market.

Strategic Regulatory Support

Regulatory agencies don't just accept permeability data; they value it. These studies can allow waivers of in vivo bioequivalence studies for products with proven high permeability through validated cell models. This can represent substantial savings in time and resources, in addition to accelerating the approval process.

Validated Methodologies for Reliable Results

Choosing the right methodology is crucial to obtaining data that truly guides strategic decisions. Our approach is based on decades of scientific validation and global regulatory acceptance.

Intestinal Permeation: The Power of the Caco-2 Model

The Caco-2 model has revolutionized oral drug development. It offers a reliable alternative to animal studies. These cells, grown in Transwell plates, form a barrier that mimics the human small intestinal epithelium with impressive fidelity.

The greater than 85% correlation between the results obtained with Caco-2 cells and actual human absorption is no coincidence. It is the result of years of cross-validation involving hundreds of known compounds. We use TEER meters to continuously monitor the integrity of the cellular barrier. This ensures that each result accurately reflects the expected in vivo behavior.

Proven strategic advantages:

Accurate prediction of human oral absorption.
Identification of specific transport mechanisms.
Ability to assess drug interactions.
Results accepted by regulatory agencies.

Skin Permeation: Innovation with HaCaT Cells

The development of topical drugs and transdermal systems presents unique challenges. The HaCaT model (immortalized human keratinocyte lineage) elegantly addresses these challenges. These cells form a barrier that replicates the essential characteristics of human skin, enabling accurate assessments of skin penetration.

For R&D companies focused on drug delivery, this model offers valuable insights into how to optimize formulations. This maximizes delivery of the active ingredient to the desired location. The quantification methods employed, including HPLC and LC-MS/MS, ensure the analytical precision required for confident strategic decisions.

Results that Transform Development Strategies

The data generated by permeability tests goes far beyond simple numbers in a report. They provide strategic intelligence that can completely redirect a development program.

Evidence-Based Decision Making

Imagine having data that shows exactly why your promising compound isn't being absorbed properly. Or discovering that a simple formulation modification can increase bioavailability by up to 300%. These insights are real-world examples of how our trials have impacted client projects.

The quantitative parameters obtained include permeability coefficients, efflux ratios, and transport profiles. Interpreted by our specialized team, these data translate into clear strategic recommendations. Whether the decision is to move forward with a candidate, modify a formulation, or explore alternative drug delivery systems, our data provide the necessary solid scientific foundation.

Data for Informed Decisions

Laboratories that systematically incorporate permeability testing into their development pipelines gain a significant competitive advantage. This occurs through more informed decision-making. Early identification of absorption issues allows for adjustments in development while costs are still manageable. This is different from late discoveries in advanced clinical stages.

Strategic Applications by Segment

Biotechs

We serve companies ranging from proof-of-concept startups to pre-IPO companies with robust pipelines. We offer protocols tailored to specific development stages and fundraising documentation needs.

Pharmaceutical Industry

We support complex generic drug projects, strategic reformulations, and new product development. Our timelines and documentation are tailored to regulatory requirements.

CROs and Laboratories

We provide specialized services that complement existing portfolios. This allows for capacity expansion without investing in proprietary infrastructure.

Infrastructure and Expertise that Make a Difference

Performing reliable permeability tests requires much more than adequate equipment. It demands accumulated expertise, refined protocols, and the ability to interpret results within the strategic context of each project.

Our infrastructure combines cutting-edge technology with in-depth expertise. Our cell culture systems ensure reproducibility. Our array of quantification methods ensures analytical accuracy. But the real differentiator lies in our team's ability to translate technical data into actionable strategic insights.

Experienced professionals in:

Regulatory interpretation of permeation data.
In vitro-in vivo correlation for prediction of clinical performance.
Product validation according to technical standards.

Cutting-Edge Technology for Accurate Results

Our laboratory infrastructure includes state-of-the-art cell culture equipment, with cell authentication. This combination ensures not only impeccable technical execution of the assays but also the ability to adapt protocols to the specific needs of each project.

Strict quality control permeates every stage, from cell cultivation to final data analysis. Each experiment is meticulously documented, ensuring complete traceability and compliance with the most demanding regulatory standards.

Regulatory Compliance and Quality Assurance

In an increasingly stringent regulatory environment, compliance is crucial to the success of any pharmaceutical development project. Our protocols strictly follow Good Laboratory Practices (GLP) and guidelines established by regulatory agencies. This ensures that the data generated meets the highest technical and regulatory standards.

The comprehensive documentation we provide goes beyond simple technical reports. Each study includes complete data traceability, robust statistical analysis, and, crucially, interpretation of results within the relevant regulatory context. This approach has proven crucial for clients navigating complex approval processes.

Our quality management systems are structured to meet regulatory requirements. This ensures that the data generated is suitable for official submissions and provides strategic flexibility for our clients.

Competitive Advantages that Drive Results

Proven Experience in Project Diversity

Our track record includes challenging projects ranging from orphan drugs for emerging biotechs to strategic reformulations for multinational pharmaceutical companies. This diverse experience translates into a unique ability to adapt protocols and interpret results considering the specificities of each commercial and regulatory context.

Flexibility that Meets Commercial Realities

We recognize that development schedules rarely follow ideal plans. Our operational structure allows us to quickly adapt to changing priorities, scale as needed, and provide continuous support throughout the development cycle. This flexibility has been crucial for clients facing competitive pressures or limited windows of opportunity.

The added value our insights provide goes beyond technical execution. Clients consistently report that our studies generate data that inform critical strategic decisions. This includes everything from structural modifications to complete redirections of development programs.

Continuous Innovation: Preparing for the Future

Scientific research into cell permeability is evolving rapidly. We maintain continuous investment in technological and methodological updates. We closely monitor developments in 3D models, organ-on-chip technologies, and the application of artificial intelligence to permeability prediction.

This proactive approach ensures that our clients always have access to the most advanced and scientifically robust methodologies. This maintains a competitive advantage in increasingly demanding markets. Our team regularly participates in scientific conferences and collaborates with leading research centers. This ensures that we are always at the forefront of methodological developments.

Adapting to Future Demands

The regulatory landscape and expectations of the pharmaceutical industry are constantly evolving. Our ability to anticipate and adapt to these changes represents strategic value for long-term partnerships. This allows our clients to always stay ahead of market demands.

Success Stories and Impact

Our experience spans a wide range of successful projects across different segments of the pharmaceutical industry. From biotechs in early stages of development to established pharmaceutical companies seeking to optimize existing products, our trials have consistently contributed to informed strategic decisions and positive outcomes.

The diversity of cases we handle demonstrates our ability to adapt methodologies and interpret results, taking into account the specificities of each project, regulatory context, and commercial objectives. This versatility translates into tangible value for clients with distinct needs and varying timelines.

Accelerate Your Project with Our Expertise

Successful pharmaceutical development requires partners who combine technical excellence with deep strategic understanding. Whether you're developing a new drug, optimizing an existing formulation, or seeking competitive differentiation through innovative drug delivery , our intestinal and skin permeability testing can be the catalyst your project needs.

Our team of experts doesn't just perform assays. We develop customized solutions that meet the specific realities of your project, timeline, and strategic objectives. Each protocol is carefully tailored to generate the most relevant data for your research and development decisions.

Request a personalized proposal and discover how our expertise can accelerate your research development and product validation. This reduces risk, optimizes investments, and maximizes your chances of market success.

Request a Proposal

Bibliography

Artursson, P., et al. (2001). Caco-2 monolayers in experimental and theoretical predictions of drug transport. Advanced Drug Delivery Reviews , 46(1-3), 27-43.
Hubatsch, I., et al. (2007). Determination of drug permeability and prediction of drug absorption in Caco-2 monolayers. Nature Protocols , 2(9), 2111-2119.
FDA Guidance for Industry. (2017). Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System.
Lennernäs, H. (2007). Intestinal permeability and its relevance for absorption and elimination. Xenobiotica , 37(10-11), 1015-1051.
EMA Committee for Medicinal Products for Human Use. (2010). Guideline on the Investigation of Drug Interactions.