Improving pharmaceutical and biomedical applications through metal-organic frameworks (MOFs)

Starting with the first publication about metal-organic frameworks (MOFs) in 1999, MOFs have seen a rapid growth in the last years and have proven to be of great interest to the pharmaceutical industry. MOFs can improve drug delivery, stabilize enzymes or improve osseointegration of implants. Discover the opportunities MOFs offer for pharmaceutical applications.

As the name suggests, metal-organic frameworks feature highly-structured frameworks of metal ions/clusters connected with organic linkers. Like a sponge, metal-organic frameworks can take-up, hold and release molecules from their pores. The application of MOFs are seemingly endless, as the building blocks – metal ions and organic linkers – can be chosen almost without limitations. From combinations of single metal and single organic linker to multiple metals and multiple linkers. Furthermore, the framework itself can be either rigid or flexible, depending on the base materials. This tunability makes the so versatile – from harvesting water from dry air to improved gas storage.

These characteristics make MOFs perfect for pharmaceutical applications, in which ingredients have to be delivered to a specific target area in the body or be release over a specific period of time. Moreover, specific applications such as enzyme encapsulation and biomedical sensing and imaging can be performed using MOFs.

This article will give you a short overview of current and potential pharmaceutical applications based on the unique properties of metal-organic frameworks.

Drug Delivery

The delivery of drugs is usually characterized by a sharp peak of these ingredients directly after the ingestion. The market has thus longed for controllable drug release while at the same time reducing side effects and increasing efficacy of the drug. To do so, the active ingredients are bond to nanocarriers such as silica or MOFs and then released in a controllable manner within the body. MOFs have shown superior properties compared to other nanocarriers such as silica.

Metal-organic frameworks can be created to match the requirements of drug carriers:

• Have large loading capacity
• Be small enough to allow intravenous injection
• Be non-toxic
• Be biodegradable
• Offer a controllable release of the active ingredients

The active ingredients can be carried in different ways; by encapsulating them in the framework, attaching them to the linkers or by using them as linkers of the framework. More on drug delivery

MOFs in Implants

Following the idea of MOFs as intravenous drug carriers, implants can be coated with drug releasing MOFs too. Such coatings release active ingredients in a controlled manner while improving antibacterial activity and osseointegration.

MOFs as Gasotransmitter for NO and CO

The adsorbing and desorbing capabilities of metal-organic frameworks can be applied to gasotransmitters. MOFs are therefore tuned to securely bind molecules (such as CO and NO) and release them on a specific stimulus such as light or pressure. These could be applied in the human body, where CO is an important cell signaling mediator.

Nitric oxide is crucially involved in various functions within the body and the targeted delivery of NO is thus attractive for different applications. Futhermore, commonly used medical equipment used to deliver NO (e.g. stents) can be the reason for life-threatening complications. Polymers and zeolites have been found to also have harmful side products, that are carcinogen or inflammatory.

Metal-organic frameworks on the other hand, have a high adsorption properties that offer controllable release of the NO upon specific conditions. Different MOFs including HKUST-1 and CPO-27 have been tested for their gas storage capabilities and have been found very promising for future applications.

Enzyme encapsulation

While enzymes on their own are highly efficient and selective catalysts, they are also unstable in organic media, are hard to recycle and depend on coenzymes. Strategies to make enzymes more stable and thus usable in various applications include CLEA (cross-linked enzyme aggregates), silica gels and nanoparticles. Compared to these materials, metal-organic frameworks show great properties. Their uniform structure enables an equally uniform application of the enzymes, while their pores can be tuned to prevent leaching, denaturation and deactivation of the specific enzymes.

In short, MOFs keep the activity of enzymes unchanged while increasing their stability.