Researchers Identified An Effective Way to Deliver HIV Drugs to Infants

Investigators from the College of Agricultural Sciences at Pennsylvania State University say they have identified a method to provide an antiretroviral medicine to infants and young kids via a baby formula – a way that could considerably enhance therapy for the around 3 million children globally residing with HIV.

Investigators say they have identified a method to modify the particles generated by the casein protein (pictured). Image credit: College of Agriculture, Penn State

The study team, which includes Frederico Harte, presented their results in the journal Pharmaceutical Research.

About 90% of kids with human immunodeficiency virus (HIV) reside in sub-Saharan Africa, where there is minimal accessibility to antiretroviral therapies. With respect to the World Health Organization (WHO), only 23% of these kids obtained antiretroviral drugs previous year.

But even when kids are capable to access these drugs, they may not react well to it. Harte notices that Ritonavir – one of the very generally used antiretroviral medicines to prevent and deal with HIV and AIDS – can lead to a number of side effects, like diarrhea, vomiting, stomach discomfort and weakness.

Harte states that it can also be challenging to provide the medicine to babies. “The fluid formulation utilized to treat babies above 1 month of age comprises of 43% ethanol and has an bad taste.

In addition, the medicine is not absorbed simply. “Ritonavir has a great hydrophobicity and minimal solubility in water,” claims Harte, “which cause to a lower dissolution rate in the gastrointestinal fluid and, therefore, to inadequate bioavailability.”

Therefore, Harte and co-workers set out to find a more efficient way to provide this drug to children, while providing it can be simply dissolved in the gut.

Binding Ritonavir to cow’s milk substances

For their research, the team researched a group of proteins known as caseins, which are identified in cow’s milk.

Casein proteins generate casein micelles – particles that are reason for milk’s white color. Casein micelles are accountable for providing calcium and amino acids in milk from a mother to their baby. This got the team considering: could casein micelles deliver Ritonavir substances, too?

“I have been operating with bovine casein micelles for a several years now, and we have examined the design and functionality of these proteins,” states Harte. “What we identified is these micelles are capable to bring molecules that have extremely little solubility in water, that have lower molecular weight and that are very hydrophobic in nature like as Ritonavir.”

What is more, the team identified that they could modify the casein micelles to increase their binding qualities, which means they could connect Ritonavir molecules to the micelles more successfully. They did this by homogenizing cow’s milk at 400-500 megapascals. For evaluation, Harte notices that milk is generally homogenized at 10-15 megapascals.

Describing what these results mean, Harte says:

“As an outcome of this increased binding of molecules, we consider a milk powder that contains Ritonavir can be applied as baby formula, offering a transport system for a medicine that is not extremely soluble in water.”

Promising outcomes in piglets

The scientists say they are presently in the procedure of testing this formula on 3 piglets, and blood samples are being obtained from the animals every 3 hours to evaluate its effectiveness.

“The wish is that – and we do not have the data yet – we discover that the Ritonavir is being effectively provided by the protein in milk,” says Harte. “So if that performs, I think we are fairly close to having a formulation that can be applied with hydrophobic drugs.”

He adds that he is optimistic their results will guide to a new drug delivery system to protect against and treat HIV and AIDS, but he notes that the formula needs to be tested in clinical trials to know for certain.