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Lipids-based liquid iron formulations - frontiers in anaemia management

Arun Kedia
Wednesday, August 24, 2022, 08:00 Hrs  [IST]

Among the most prevalent nutritional disorders in the world, especially in underdeveloped countries, is iron deficiency or anemia. Iron plays a vital role in metabolic processes like oxygen transfer, DNA replication and hormone synthesis. A prolonged low level of iron in the blood can lead to iron deficiency anaemia (IDA), a disorder most common among pregnant women and children in the age group of 5 to 14 years, especially in developing countries. According to the WHO statistics for developing countries, 48% of children between 5 to 14 years and 52% of pregnant women are victims of this disorder.

IDA can result from an iron-deficient diet, worm infestation, Vit C deficiency, iron absorption inhibiting factors, and gastrointestinal disorders. Hepcidin is a key iron regulator and any dysregulation in hepcidin expression can also result in iron deficiency. Dietary changes alone may not be sufficient for the management of IDA. Hence, iron supplementation becomes necessary. However, conventional strategies to counter this problem like iron bio-fortified crops and iron dietary supplements are not very effective. Oral iron therapy has its limitations due to dose dependent side effects, poor absorption, low compliance and limitations in various inflammatory conditions. Low absorption of iron by the blood, low disposal of iron, and lipid peroxidation are common problems with these strategies. All this can prove to be detrimental in the long run.

As a result, there is a growing need for new forms of iron therapy and iron supplementation which focus on increased bioavailability of iron to enable more bioabsorption by the cells in a shorter duration. Now lipid-based nanotechnology is opening new avenues for successful delivery and enhanced bioavailability of iron in the body. Liposomal iron is being seen as a technological breakthrough in this regard. It offers an innovative delivery system which ensures higher absorption, bioavailability, greater tolerability and less gastrointestinal side effects as compared to conventional oral iron preparations.

Lipid nanotech-based iron formulations - new Frontiers in drug delivery for IDA
Oral and parenteral iron supplementation for the treatment of IDA has been so far the most accessible  option.  However, in the case of parenteral iron preparations, wherein, iron carbohydrate complex formulations are used, the weakly bound iron molecule may get deposited in the endocrine system. This affects the heart and the liver during the phase of iron release by causing oxidative stress. In the case of oral iron preparations, up to 70% of patients report GI side effects. This may not be the best option for patients who suffer from continuous blood loss, inflammatory bowel disease, kidney dysfunction, and other complications.

Liposomal iron supplements
In the case of patients, who do not respond to conventional iron replacement therapy, liposomal iron is a blessing in the management of IDA. Liposomes are considered effective drug carrier systems due to their low toxicity, bioavailability, and biodegradability.

Liposomes are nanoparticles and their spherical-shell structures comprising a phospholipid bilayer enclosing a aqueous core help to stabilize the encapsulated materials. In a liposomal oral iron preparation, the ferric pyrophosphate is encapsulated within the phospholipid-lecithin bilayer of the liposome. The advanced technology makes use of the liposome as a carrier. The biomolecule formed thus has a structure of an outer bilayer membrane and an inner core containing the iron particles. Since the ferric pyrophosphate is encapsulated within the liposome, the iron does not come in contact with GI mucosa but instead is directly absorbed in the intestine. The ferric pyrophosphate particle size is reduced by a process known as micronisation, which helps to increase the surface area of the molecule and thus enhances dissolution.

By further encapsulating it into the phospholipid bilayer, the degradation of the iron by enzymes present in the mouth and the stomach is prevented and the iron is directly absorbed into the small intestine. This results in overall increase in bioavailability at lower dosage than oral supplements. Liposomal iron has been found to facilitate quicker absorption with significant improvement of serum iron and liver iron contents as compared to conventional oral iron preparations.

According to a study, patients treated with liposomal iron supplements also showed better tolerance with significant improvements in side effects shown by other patients who were treated with other iron supplements. The study also suggests that liposomal iron may help in minimizing the oxidative damage that is typically associated with conventional iron.

Liposomal iron is being seen as a nano-engineered technological marvel. By overcoming the limitations of conventional iron preparations, it appears to offer favourable clinical outcomes. Due to these reasons, liposomal iron seems promising as an effective and safe alternative to parenteral iron in chronic inflammatory conditions associated with IDA.

Solid lipid nanoparticles
Solid lipid nanoparticles (SLNs) are emerging as an alternative drug delivery system. This novel colloidal drug carrier system enables various application routes such as oral, topical, parenteral, ophthalmic, and rectal. More recently, SLNs (Solid Lipid Nanoparticles) have shown to possess a high melting lipid core matrix that can solubilize lipophilic molecules. These are stable nanoparticles with high solubility, easier manufacturing, biocompatibility and controlled release.

A study has revealed that Fe-SLNs can significantly change the pharmacokinetic profile and can increase the drug's bioavailability by more than four times in comparison with the conventional oral preparations. One of the reasons is that the aqueous solubility of iron as a drug is very low. However, it was observed that when it was prepared as a SLNs not only its solubility increased, but there was an increase in tissue permeability as well.

This colloidal drug delivery mechanism offers many advantages in terms of higher absorption of drugs in addition to controlled and sustained drug targeting. This coupled with the possibility of scale-up in manufacturing makes it a preferred option. Studies indicate that Fe-SLNs could be a promising carrier for iron with enhanced oral bioavailability.

Combating malnutrition and IDA with lipid-encapsulated fortified body oil
More than 80% of the Indian population is known to suffer from Vitamin D and iron deficiency.  Almost 59% of children in the under 5 age categories suffer from severe iron deficiency. Iron deficiency at the age of 6 to 24 months old leads to poor cognitive and motor development. It is a known fact that Folate and Vit B 12 are very important micronutrients for brain development. However, most supplementation programmes are not very successful due to the low absorption of these micronutrients and GI intolerability when they are administered orally.

To address this issue, a new non-invasive transdermal route for administering these micronutrients has been gaining a lot of attention. Very few molecules can cross the skin barrier, however, with recent advances in nanotech-based formulations, an innovative formulation of body massage oil has been developed. In this body oil, soya phosphatidylcholine and oleic acid-based liposomes are used to encapsulate iron, Vit B 12, and Vit D. This liposomal encapsulated fortified body oil can permeate the skin barrier and indicates 40 to 50% enhanced efficiency for iron and 90 to 95 % increased efficiency for Vit D.

In developing countries, like India, especially in the rural population where IDA is a matter of concern with infants, this therapy may prove to have widespread acceptance from a cultural perspective where almost 90% of households in these regions believe in the benefits of oil massage during infancy.  Although this method has not prevented anaemia completely, it has shown significant results in preventing Vit D deficiency and prevented a decline in haemoglobin level. Further research would be needed for the optimisation of oil composition and dosage increments.

Liposomal iron, either as an oral iron preparation or transdermal oil formulation, is a new generation technology engineered through a process of micronisation and microencapsulation. It holds a promising future in overcoming the limitation associated with conventional iron preparations in terms of drug toxicity, bioavailability and patient friendly options compared to invasive injections. However, further clinical evaluations regarding bioactivity and toxicity for this novel formula continue to be the need of the hour to provide researchers with substantial data in furthering this technology.

(Author is managing director of VAV Life Sciences)


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