and Drug Targeting
Rijksuniversiteit Groningen: WBFA060-05, June 2024
Do not plagiarize the posters
, Learning outcomes
1. Describe different strategies for drug targeting, personalized medicine and theranostics as well as innovative
experimental approaches for the development of targeted drugs (monoclonal-based therapies and protein-based
drug targeting strategies)
2. analyze the properties of the currently approved nanomedicines and major types of drug carriers and their
characteristics, as well as describe novel targeting and therapeutic strategies based on stimuli-responsive drug
carriers
3. Explain the different physiological barriers to drug delivery and (immune) cell-based clearance mechanisms, as we
as describe the cellular uptake and intracellular distribution of nanomedicines and targeted drugs and their
consequences
Content
Block 1 Introduction to drug delivery and drug targeting strategies 5
Block 2 Overview of main nanomedicine types, uptake & intracellular targeting 22
Block 3 Other targeting strategies with stimuli-responsive materials 31
*no book reading → research papers
Assignments
● 3 infographics based on main lectures (not research lectures)
○ A3 size
○ Original figures and text
○ To summarize main content
● During tutorials, 10 minute presentations for feedback (1 total per group)
○ No grade
Exam
● 30 multiple choice
● 3 open questions
● 60 points total
● 10 MC, 1 OC per block
● Minimum 6
, Introduction
Barriers for drugs
● Intestinal enzymes
● Mucus
● Tight junctions
● Epithelial cells
● Sub epithelium
Barriers in blood
● Immune system
● Opsonization
○ Binding of opsonin proteins
○ Signal for removal
Pathways across the blood-brain barrier
a. Paracellular aqueous pathway
b. Transcellular lipophilic pathway
c. Transport proteins
d. Receptor-medaited transcytosis
e. Adsorptive transcytosis
Intracellular barriers
● Barriers from drug targeting within cells
● To avoid lysosomal degradation
○ Avoid endosome entrapment
Importance of drug targeting
● Maxmizing drug efficacy
● Limiting side effects
● Limting off-target accumulation
Protein treatments
● Massive potential
● Needs uptake
● No uptake into cell and degradation without uptake mechanism
How to improve drug arrival at site of action
● Nanomedicine
○ Loading the drug in a drug carrier
● Drug targeting
○ Modifying the drug (carrier) to control where it goes or activate drug release
● Targeting strategies with stimuli-responsive materials
○ Control release of drug by exposing drug to stimuli once it is at target site