Biologicals and the current obstacles
Biologicals are the future of Pharma. With their tremendous potential to address various unmet medical needs, they make up the major part of the pipelines of Pharma companies. However, there are some issues with which pharmaceutical companies developing biologicals continue to struggle.
They are difficult to make, and they are hard for patients to take. This article specifically deals with the last issue. Both patients and manufacturers prefer that drugs can be taken orally.
For the patients, the ease and convenience of oral administration are of great importance.
For manufacturers the production costs for oral dosage forms are often lower and they are also the easiest form for the further optimization of drug delivery.
Why are not all biologicals made as pills or syrups then? There are a few physical and chemical obstacles that the developers do not seem to overcome. These are the high molecular weight, hydrophilicity, and instability of large biomolecules.
First, the absorption across the gut seems to be a problem. Biologicals are often quite large molecules, making them difficult to diffuse across the epithelial layer. Moreover, they often do not have the physicochemical properties to be therapeutically active when orally administered. For example, the polar surface of peptides ensures that they are not lipophilic enough to be absorbed. Secondly, biologicals are often sensitive to enzymatic and chemical degradation in the gut. The acidity of the stomach as well as the enzymatic activity in the intestines is often a problem. The third challenge is the stability of the biologicals. Temperature, pH, and light can affect the molecules. This can be a problem especially for manufacturing and storage.
Fortunately, plenty of solutions are being developed, such as the following examples:
The oral delivery of biologic APIs is often called the “holy grail” of pharmaceutical drug delivery. It is exciting to see that more and more innovative companies emerge in the field of biotherapeutics. The stunning wide range of different product lifecycle strategies leads to a stimulating and dynamic area of research and investment for the coming years.