Iron casein succinylate-chitosan coacervate for the liquid oral delivery of iron with bioavailability and stability enhancement

• Published in: Archives of pharmacal research Vol. 39; no. 1; pp. 94 - 102
• Main Authors: Min, Kyoung Ah, Cho, Jung-Hye, Song, Yun-Kyoung, Kim, Chong-Kook
• Format: Journal Article
• Language: English
• Published: Seoul Pharmaceutical Society of Korea 01.01.2016; 대한약학회
• Subjects: Administration, Oral; bioavailability; Biological Availability; Caco-2 Cells; casein; Caseins - administration & dosage; Caseins - chemistry; Caseins - metabolism; Cell Membrane Permeability - drug effects; Cell Membrane Permeability - physiology; chitosan; Chitosan - administration & dosage; Chitosan - chemistry; Chitosan - metabolism; Drug Delivery Systems - methods; Drug Stability; human cell lines; Humans; iron; Iron - administration & dosage; Iron - chemistry; Iron - metabolism; Medicine; nanoparticles; nutrient deficiencies; Particle Size; patients; permeability; Pharmacology/Toxicology; Pharmacy; polyethylene glycol; Research Article; storage time; taste; zeta potential; 약학; Coacervation; Chitosan; Bioavailability; Nanoparticle; Iron casein succinylate
• ISSN: 0253-6269; 1976-3786
• DOI: 10.1007/s12272-015-0684-6

Iron casein succinylate (ICS) liquid oral preparation as iron supplement has uncomfortable taste after a long period of storage because of its stability, and poor bioavailability of iron compared to any other iron preparations. To improve the chemical stability of ICS and enhance the bioavailability of iron, chitosan-ICS nanoparticles (NPs) were prepared by complex coacervation method and stabilized with polyethylene glycol (PEG) 400. NPs were spherical (mean diameter of 830–1070 nm) with positive charge (+30–60 mV) depending on the composition of NPs. Addition of PEG400 (2 w/v %) increased the zeta potential (26–50 %) and physical stability of chitosan-ICS NPs suspension. Also, NPs decreased iron release compared to ICS after 7-weeks of storage at 4 °C. NPs markedly increased the permeability of iron in Caco-2 cell up to 32–38-fold compared to ICS, while physical mixture of chitosan and ICS increased the iron permeability only 2.5-fold. In summary, NPs improved the physicochemical stability and enhanced the transport of iron compared to other iron preparations in Caco-2 cell model. Thus, chitosan-ICS coacervate might be a promising candidate as a liquid oral iron delivery system for iron deficiency patients with stability and bioavailability enhancement.