Sucrosomial® Iron: A new generation of oral iron supplement with improved efficacy

Susanna Gomez-Ramirez1, Elisa Brilli3, Germano Tarantino3, and Manuel Muñoz4,*

1Department of Internal Medicine, Virgen de la Victoria University Hospital. Campus de Teatinos, 2010 Malaga, Spain; This email address is being protected from spambots. You need JavaScript enabled to view it.

2Scientific Department, Alesco S.r.l. Via delle Lenze, 216/B, 56122 Pisa, Italy; This email address is being protected from spambots. You need JavaScript enabled to view it.

3Scientific Department, Pharmanutra S.p.A. Via delle Lenze, 216/B, 56122 Pisa, Italy; This email address is being protected from spambots. You need JavaScript enabled to view it.

4Perioperative Transfusion Medicine, Department of Surgical Specialties, Biochemistry and Immunology, Medical School, Campus de Teatinos, 29071, Malaga, Spain

Abstract: Sucrosomal® Iron(SI) is an innovative oral iron preparation with unique structural, physicochemical and pharmacokinetic characteristics with high bioavailability and excellent tolerability. Data analysis confirms that SI is a reliable treatment for iron deficiency (DI), it is more effective and better tolerated than oral iron salts, and has similar efficacy with IV iron, but with fewer risks. Thus, SI is the drug of first choice for the prevention and treatment of GAD especially for patients with intolerance to iron salts or those for whom iron salts are ineffective and can be an alternative to intravenous iron for initial or maintenance treatment in different patient groups.

Data from 187 countries in 2010 showed that anemia affects approximately one-third of the world's population, although prevalence varies by region, with LD being responsible for almost 50% of anemia [1]. In a systematic analysis of the Global Burden of Disease Study 2016, WD was the fourth leading cause of disability, especially among women [2]. The main causes of JD are increased requirement, decreased absorption, or increased iron loss [3,4].

Treatment of anemia usually focuses on eliminating the causes of iron deficiency and restoring iron levels with oral or parenteral iron preparations and/or blood transfusions, depending on the patient's Hb level, tolerance, and comorbidities.

Oral iron supplements are usually the first-line treatment for uncomplicated iron deficiency because of their availability, ease of administration and relatively low cost [5,6]. They are prescribed in high doses (100-200 mg of elemental iron) with a frequency of administration 1-3 times per day. However, the bioavailability of divalent iron preparations (sulfate, gluconate, fumarate) is only 10% to 15% and lower for salts and complexes of trivalent iron (amino acids, polysaccharide, etc.). Concurrent intake with other medications (PPIs or antacids) or with food, as well as the presence of inflammatory processes can further complicate absorption of oral iron and reduce the effectiveness of therapy [7]. In addition, up to 50% of patients receiving oral iron report gastrointestinal side effects due to the direct toxicity of iron ion, which generally reduces treatment adherence [8,9].

As time passed, oral forms of iron were constantly being developed to improve tolerability [9]. Nevertheless, there was still a need for new carriers that would not only protect iron but also enhance its intestinal absorption, thereby reducing dosage and side effects [10].

Sucrosomal® Iron(SI), developed by Alesco srl (Pisa, Italy), is an innovative oral iron carrier in which iron pyrophosphate is protected by a phospholipid bilayer membrane (mainly from sunflower lecithin) and a sucrestor matrix. ). This proprietary technology provides maximum tolerability, gastroresistance (improved absorption), no negative taste or side effects normally associated with iron supplementation. In addition, absorption of the SI complex occurs without the usual intestinal absorption mechanisms. This allows for higher plasma concentrations than other oral iron compounds. Conventional iron preparations are absorbed via mediated transport proteins, instead of SI being completely absorbed by the intestinal mucosa as a vesicular structure.

Intestinal absorption of Sucrosomial Iron (SI) is provided by Payer's microfold cells (M-cells), where by endocytosis, with macrophages via lymphatic vessels, it enters unchanged into hepatocytes and other target organs. Since Sucrosomial® Iron (unlike divalent and trivalent iron in traditional preparations) does not interact with the enterocyte membrane and the transport enzymes in it (DMT proteins and ferroportin), its absorption does not depend on the inflammatory protein hepcidin, which in cases of concomitant inflammatory processes inhibits iron absorption in the intestine [10].

The most relevant evidence for the tolerability and efficacy of Sucrosomal® Iron in various preclinical and clinical settings was presented at the 3rd, 4th, 5th and 6th International Multidisciplinary Congresses on Iron Deficiency Anemia and other conferences: 10 studies in oncology ( 241 patients), 11 studies in nephrology for CCN (294 patients), 7 studies in gastroenterology (122 patients), 8 studies in cardiology (161 patients) and 10 studies in internal medicine, including gynecology and obstetrics (236 patients).

The CardioSideral Heart Surgery (NCT03560687), a prospective study of 1,000 consecutive patients undergoing cardiac surgery, is ongoing.

Multicenter studies have clearly demonstrated that sucrosomal iron has unique structural, physicochemical, and pharmacokinetic characteristics. The presence of sucrosomal iron confers gastroresistance to SI, protects its trivalent pyrophosphate iron from enzymatic reduction, and promotes absorption through the intestinal epithelium in a DMT-1 (divalent metal ion transporter) independent manner that is largely mediated by M cells. All this allows oral SI to have high bioavailability and low gastrointestinal toxicity.

Analysis of clinical data demonstrates Sucrosomal® Iron as a supplement with new features-a more convenient, effective form of iron (lower doses, greater Hb gains, and better iron replenishment) that has better tolerability than traditional oral iron salts and with fewer risks compared to parenteral iron.

Thus, Sucrosomal® Iron may be the drug of choice for the treatment of uncomplicated iron deficiency, especially for those who cannot tolerate iron salts or for whom iron salts are ineffective. Moreover, it should be considered as an alternative to intravenous iron for initial or maintenance treatment in different groups of patients.

Article provided in abbreviated form, access the full version: https://doi.org/10.3390/ph11040097

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