For many cancer patients, the most effective chemotherapy drugs are those that are given intravenously. However, this method of administering the drug is not always convenient or accessible to patients, and can cause complications of its own
US doctors have developed a technology that makes exclusively intravenous drugs suitable for administration in pill form.
Recent medical research has shown that the desired therapeutic effect can sometimes be achieved in an unusual way. For example, blocking one of the proteins helped stop age-related vision deterioration, and activating a specific DNA molecule helped heal an inflamed wound faster.
Experts from Stanford University in the US have found a way to turn intravenous chemotherapy drugs into oral ones and make them effective at lower doses. This was made possible by a special molecular “tag” that can be added to the molecules of almost any drug. A study describing the new technology was published in the scientific journal Nature Communications.
In order for a medicine to do its job, a pill must go through several stages. When a person swallows it, it dissolves in the stomach and releases molecules of the active substance, which are then absorbed into the walls of the stomach or intestines and enter the bloodstream. The blood transports the drug molecules to the organs it is intended to treat, the medicine penetrates the membranes into the cells and only then begins to act.
The greater the percentage of the ingested drug that enters the bloodstream, the more pronounced the effect and the more bioavailable the drug is considered. Bioavailability rarely exceeds 20%, since it requires the drug to be soluble in both water (to release the active substance in the stomach) and oil (to pass through cell membranes).
Water and oil do not mix, so some drugs that are poorly soluble in water are injected directly into the blood to achieve the desired effect and avoid high dosages.
The authors of the new article have developed a molecular “tag” that can attach to any drug and make it highly soluble in water, and then be removed after absorption in the walls of the stomach or intestine. Thus, a water-soluble prodrug, entering the blood, turns into a fat-soluble drug.
It’s a stunningly simple solution to an old problem. With this new strategy, we can speed up the introduction of vast numbers of drugs into clinics. Millions of patients around the world who are undergoing chemotherapy will be able to receive care at home, without having to take steroids or undergo long infusions (a method of slowly introducing a solution of a substance into the blood).
The “tag” was tested on two popular chemotherapy drugs. The effectiveness of one of them soared from almost 0% to 100% when taken in pill form, but only mice were involved in the experiment. In the future, if the technology passes clinical trials on humans, it could increase the effectiveness of many drugs and reduce the cost of treating serious diseases.
This story was adapted by rnn.org.ng from here.
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