Amphiphilic properties of drug molecules

Forskning inom Självaggregering av amfifila läkemedel

Research with a focus on various aspects of the self-assembly process of amphiphilic drugs in presence of relevant drug delivery components

Details

  • Funder: Vinnova

Amphiphilic properties of drug molecules

Many pharmacologically active compounds are made up of amphiphilic molecules and possess many similar properties to ordinary surface active agents. Amphiphilic drugs may be found within several classes of drugs including tranquilizers, analgesics, antibiotics, antidepressants, antihistamines, local anaesthetics, anti-inflammatory drugs and anticancer drugs. The amphiphilic nature of these molecules is expected to play a crucial role for their pharmacological activity as well as important properties related to toxicity and haemolysis. In drug formulations the amphiphilic properties of the active substance is decisively important for the molecular mechanisms of solubilisation and drug delivery.

In this research program, we study various aspects of the self-assembly process of amphiphilic drugs in presence of relevant drug delivery components such as phospholipid bilayers, surfactants, proteins and other biomacromolecules. The structural behaviour is mainly investigated using various scattering techniques such as static and dynamic light scattering, small-angle x-ray scattering (SAXS) and small-angle neutron scattering (SANS), but also complementary techniques such as cryo-TEM electron microscopy (Fig.2).

Fig.2 : Cryo-TEM image of mixed sodium dodecyl sulfate/adiphenine hydrochloride vesicles

Fig.2: Cryo-TEM image of mixed sodium dodecyl sulfate/adiphenine hydrochloride vesicles.

Amphiphilic properties of drug molecules and their self-assembly in presence of phospholipids

Molecular components such as phospholipids, surfactants, proteins and drug molecules consist of both hydrophilic and lipophilic parts and are involved in various drug delivery systems. As a result, these components are able to self-assemble and interact strongly with one another in ways that usually determine molecular release mechanisms in drug delivery systems.

The aim of this project is to study the interactions and self-assembly in mixtures of different amphiphilic drug molecules and phospholipids. The study includes structural characterization of the drug-phospholipid aggregates (micelles, liposomes, bilayer structures) as well as investigating the location and impact of drug molecules on phospholipid bilayers, by mainly using various small-angle scattering techniques.

Magnus Bergström, Universitetslektor
Institutionen för läkemedelskemi
Magnus.Bergstrom@ilk.uu.se

Vahid Forooqi Motlaq, Doktorand
Institutionen för läkemedelskemi
Vahid.Motlaq@ilk.uu.se

Project members

Project leader: Magnus Bergström
Co-investigators: Vahid Forooqi Motlaq

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