Preclinical Models for Drug Discovery

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Unlocking Innovation with Novel Drug Delivery Systems: A Preclinical Perspective

The Future of Formulation: Preclinical Models for Drug Discovery

Biotech innovation is increasingly reliant on the ability to enhance the delivery of therapies. Novel drug delivery systems (NDDS) extend drug lifecycles, enhance bioavailability, and improve patient adherence. But these advancements come with regulatory, pharmacokinetic, and safety challenges. The key to success lies in leveraging accurate preclinical models for drug discovery, including in vitro, ex vivo, and in vivo systems, to guide development from candidate selection through IND-enabling studies.

Why Novel Drug Delivery Systems Matter

NDDS offers clear advantages over traditional methods:

  • Improved bioavailability: More active drug reaches the target site
  • Enhanced safety profiles: Reduced off-target effects through site-specific delivery
  • Patient compliance: Oral, sublingual, or sustained-release options minimize dosing hurdles
  • Regulatory efficiency: Using the FDA’s 505(b)(2) pathway, NDDS can fast-track approval by referencing existing safety/efficacy data

Role of In Vitro and In Vivo Pharmacokinetics in NDDS

Understanding how a drug moves through and acts within the body is fundamental. In vitro and in vivo pharmacokinetics models offer key insights:

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In Vitro Models

  • Caco-2 monolayers: Simulate human intestinal absorption
  • Excised tissues (ex vivo): Retain physiological barriers for skin and ocular models

In Vivo Models

  • Animal models: Provide whole-organism insight, accounting for metabolism, circadian rhythm, and feeding state
  • Intestinal perfusion (in situ): Measures absorption in live animals without full systemic complexity

These models are essential for predicting human outcomes, informing formulation decisions, and fulfilling regulatory requirements.

Real-World Application: Case Study in Sublingual Delivery

Pharmaron partnered with a US biotech to evaluate a sublingual NDDS. Using porcine buccal tissue and in vivo dog models, they discovered that menthol-enhanced formulations improved absorption 30-fold and increased Cmax nearly four times. These insights supported a successful patent extension strategy.

Specialized Use Case: Ocular Delivery Systems

Drug delivery to the eye presents unique challenges. NDDS like:

  • Cyclodextran nanoparticles improve corneal retention and reduce inflammation
  • Intravitreal implants (e.g., Durasert™) allow slow release to the posterior eye segment

Pharmaron’s preclinical ocular models help evaluate the safety, efficacy, and distribution of drugs across common eye disorders, including AMD, glaucoma, and keratoconjunctivitis.

Integrating Preclinical Science with Strategic Formulation

Selecting the right preclinical models for drug discovery can make or break your NDDS strategy. Pharmaron’s integrated approach—combining advanced pharmacokinetic modeling with disease-relevant in vivo testing—reduces risk, improves timelines, and supports regulatory clarity.

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Gain expert insights into how NDDS and preclinical modeling work together to accelerate your drug development timeline. Start making smarter formulation decisions today.