Abstract
The goal of this study was to develop floating microspheres that could be used as gastroretentive systems for the delivery of anthocyanins (ACNs). These compounds are absorbed in the stomach and small intestine, and insufficient residence time in these organs could result in limited absorption and contribute to degradation. The microparticles containing freeze‐dried haskap berry extract (321.96 ± 8.35 mg cyanidin 3‐glucoside equivalents per g) were prepared by ionotropic gelation of alginate (9%, w/w) with calcium ions (CaCl2 at 2%, w/v) in the gelation bath, with calcium carbonate as the gas‐generating compound (added at different ratios in the alginate/extract mixture). The effect of acetic acid concentration (2 and 10%, v/v) in the gelation medium was investigated. Increasing the carbonate : alginate weigh ratio from 0 to 3:4 resulted in different degrees of floatability, larger particles, higher encapsulation efficiency, and lower amount of ACN released. The power law equation fitted the experimental data well, indicating that release occurred mainly by diffusion. This is the first time floating microspheres are proposed as gastroretentive platforms for the delivery of ACNs.
Highlights
Gastroretentive systems (GRS) differ from conventional oral delivery platforms as they remain in the stomach is longer (Joseph, Lakshmi, & Jayakrishnan, 2002)
The objective of the present study was to develop floating microparticles for the oral delivery of ACNs extracted from haskap berries, using an ionotropic gelation method with sodium alginate, calcium chloride, and calcium carbonate (CaCO3) as the hydrocolloid, crosslinking ion, and gas-generating compound, respectively
All the samples exhibited a burst phase with high amounts of ACNs released into the acidic fluid, followed by a reduction in release rate. For both gelation media, increased concentrations of CaCO3 resulted in lower concentrations of ACNs released over time until a plateau was reached
Summary
Gastroretentive systems (GRS) differ from conventional oral delivery platforms as they remain in the stomach is longer (Joseph, Lakshmi, & Jayakrishnan, 2002). Ma et al (2008) showed that floating particles remained in the stomach of volunteers for over 5 hr compared to a residence time of 2.5 hr for nonfloating systems These systems can increase the residence time of bioactive compounds that are stable under acidic conditions and absorbed in the stomach, such as anthocyanins (ACNs), a group of hydrophilic pigments (Delgado- Vargas, Jiménez, & Paredes-López, 2000) with health-promoting properties (Cassidy et al, 2013; Wallace, 2011). Amongst the known sources of these compounds, haskap berries (Lonicera caerulea L.) exhibit a high concentration of ACNs in addition to other bioactive molecules (Celli, Ghanem, & Brooks, 2014), which makes them an interesting raw material for the development of value- added products. These berries are native to Siberia and north-eastern Asia (Bors et al, 2012), and have recently been introduced in the North American market
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