Prodrugs/bioprecursors

Understanding the limitations associated with the administration of an active ingredient (solubility, bioavailability, etc.).

General description of the enzymatic systems involved in the biotransformation of nutrients and exogenous compounds.

Description of the main modes of membrane transport and transport systems for fundamental biomolecules (sugars, amino acids, nucleosides, etc.).

Examples of prodrug and bioprecursor designs.

Hourly Volumes*:

CM: 3:00 p.m.

TD: 5 H

Understand and be able to analyze the issues associated with the administration of an active ingredient

Be able to propose a prodrug and/or bioprecursor strategy for a biomolecule.

2-hour final written exam

• Authorized documents: No
• Non-graphical calculators allowed: yes
• Internet access allowed: No

Inductive (problem-based) and deductive teaching methods. Materials available on the digital learning platform (Moodle): Course materials, tutorial materials, past exam questions, and reference publications.

1. Introduction & General Concepts: (2 hours)

- Definitions and Basic Concepts (ADME)

- Limiting factors between the site of administration and the site of action of a biomolecule

- Main routes of administration (advantages & disadvantages)

1. Nutrient Absorption (2 H)

- Basic concepts of physiology: the digestive system,

- Enzymatic processes involved in the degradation of macromolecules,

- Description of epithelial tissue; functional aspects

- Blood and lymphatic systems

1. Biotransformation and conjugation: (2 H)

- Overview of Liver Metabolism

- Main Types of Reactions

- Impact on the efficacy of an active ingredient

- Examples.

1. Membrane Diffusion & Transport: (3 hours)

- Passive diffusion, Facilitated transport & Active transport,

- Systems for transporting biomolecules (sugars, dipeptides and tripeptides, amino acids, etc.)

- Assessment Models

5.: Prodrug Approaches (6 hours)

- Concepts & Definitions, Potential Applications

- Molecular vectorization

- Bioprecursors

- Examples

TD (5 hours): Individual work; exercises to be prepared before and during the session.

Case studies (interpretation of data from the literature).

Administrative contact(s):

Master's in Chemistry Office

https://master-chimie.edu.umontpellier.fr/