Milk Protein Set to Deliver HIV/AIDS Drugs to Infants

With an estimated 3.4 million children living with HIV/AIDS, the World Health Organization reports that 9 out of 10 of these children live in countries with very limited resources. In these sub-Saharan countries, effective antiretroviral treatements still are not easily accessible.

The complicating matter surrounding these treatments is that most antitroviral drugs are poorly received by young children. Ritonavir, the most commonly prescribed drug for treatment and prevention, has undesirable side effects and oral-delivery problems that make it difficult to administer to infants.

Federico Harte, associate professor of food science at Penn State University, had this to say about the drug, "Ritonavir has a high hydrophobicity and low solubility in water, which lead to a low dissolution rate in the gastrointestinal fluid and, hence, to insufficient bioavailability. The liquid formulation used to treat infants over one month of age contains 43 percent ethanol and has an awful flavor that has been described as bitter-metallic, medicinal, astringent, sour and burning. Moreover, when coming into contact with the stomach mucosa, Ritonavir causes nausea, vomiting and diarrhea. Therefore, we need to develop alternative pediatric formulations of Ritonavir and overcome its poor water solubility to improve its oral administration to infants and children."

Harte solved this problem by looking towards a group of casein proteins in cow's milk - these proteins naturally deliver amino acids and calcium from mother to young. 

In a statement, Harte said, "I have been working with bovine casein micelles for a few years now, and we have investigated the structure and functionality of these proteins. What we found is these micelles are able to carry molecules that have very little solubility in water, that have low molecular weight and that are very hydrophobic -- such as Ritonavir."

By homogenizing the milk at an extremely high pressure (500 megapascals versus the normal 15 megapascals), the casein protein's quality to attach the drug molecules greatly improved.

"As a result of this enhanced binding of molecules, we believe a milk powder containing Ritonavir can be used as baby formula, providing a transport system for a drug that is not very soluble in water." Harte said, "Right now we are running tests, and we are in the final stages of an experiment in which we gave three different formulations to piglets,".

Harte and his team are working with the National Institutes of Health and St. Jude Children's Research Hospital in order to move the experiments into clinical trials.

Full Report via Penn State

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