Biomembrane models and drug-biomembrane interaction studies: Involvement in drug design and development

Abstract

Contact with many different biological membranes goes along the destiny of a drug after its systemic administration. From the circulating macrophage cells to the vessel endothelium, to more complex absorption barriers, the interaction of a biomolecule with these membranes largely affects its rate and time of biodistribution in the body and at the target sites. Therefore, investigating the phenomena occurring on the cell membranes, as well as their different interaction with drugs in the physiological or pathological conditions, is important to exploit the molecular basis of many diseases and to identify new potential therapeutic strategies. Of course, the complexity of the structure and functions of biological and cell membranes, has pushed researchers toward the proposition and validation of simpler two- and three-dimensional membrane models, whose utility and drawbacks will be discussed. This review also describes the analytical methods used to look at the interactions among bioactive compounds with biological membrane models, with a particular accent on the calorimetric techniques. These studies can be considered as a powerful tool for medicinal chemistry and pharmaceutical technology, in the steps of designing new drugs and optimizing the activity and safety profile of compounds already used in the therapy.

Experimental Modeling of Flavonoid–Biomembrane Interactions

“…The advantages of these systems arise from their reduced 19 complexity and improved experimental control compared to cell cultures. 9, 10 …”

Structural insights into anticancer activity of D‐ring modified estrone derivatives using their lipophilicity in estimation of SAR and molecular docking studies

“…Therefore, retention constants were used to represent molecular lipophilicity in correlation with calculated pharmacokinetic parameters which are important factors for possible future administration. (Table ) . These factors are logBB – logarithm of the blood–brain barrier (BBB) partition coefficient; HIA – human intestinal absorption in percent; DPB – plasma protein bound in percent; PE jejunum pH = 6.5 (cm/s); Vd – human volume of distribution (l/kg); and SP – skin permeability.…”

DSC applications: macromolecules

“…17 Another fast growing application of DSC is the characterization of interactions between drugs and/or drug carriers and membranes; these interactions are important for drug design. 18,19 For antibiotics or anti-cancer drugs, these studies often use model membranes as a preliminary screen of drug interactions. DSC not only addresses the interactions between the drug and the membrane, but also the release of drugs from their carrier.…”