Enhancing the bioavailability of active ingredients is a key challenge for formulators, particularly with regards to molecules such as capsaicinoids from red chili peppers
A recently published study in the Journal of Functional Foods has demonstrated the capability of Akay’s Fenumat platform delivery technology to produce a bioavailable powder form of capsaicinoids for nutraceutical applications.
Enhancing the bioavailability of active ingredients is a key challenge for formulators, particularly with regards to molecules such as capsaicinoids from red chili peppers, which exhibit unfavourable organoleptic properties like pungency and bitterness and can cause heart burn or vomiting.
Some attempts have been made to solve this issue using through self-emulsifying drug delivery (SMEDDS), however this is only suitable for topical applications like pain balms, owing to the liquid state, lack of pungency masking, and usage of pharma grade synthetic emulsifiers. It’s therefore necessary to produce powder forms suitable for oral delivery formulations, ideally in a natural, food-grade and clean label format for functional food and nutraceutical applications.
We applied our Fenumat technology to pungent red chili extracts with a view to develop pungency-masked food-grade micro-beadlets
Akay’s Fenumat is a platform delivery technology for the delivery of lipophilic phytonutrients like curcumin and boswellic acids, either alone or as a co-delivery single powder form with enhanced bioavailability for each molecule (Journal of Functional Foods, 2021 and 2016).“We applied our Fenumat technology to pungent red chili extracts with a view to develop pungency-masked food-grade micro-beadlets (Capsifen) for the sustained-intestinal delivery with enhanced bioavailability,” said, Dr Krishnakumar, Chief Research Officer at Akay.
In the study, the authors received uniform microbeads (250-400 µm) containing no less than 2% capsaicinoid content manufactured at Akay’s GMP-facility using a proprietary gel-phase homogenisation technique followed by marmurisation and fluid bed coating. Through a series characterisation techniques, the study showed the beadlets to be stable, amorphous, directly compressible, and free flowing microbeads with a tap density of > 0.65 g/mL.
Swelling studies, in vitro release kinetics and particle size analysis indicated the microbeads’ sustained-intestinal delivery of soluble capsaicinoids enabled high absorption without discomfort. Further pharmacokinetic studies on Wistar rats reportedly revealed enhanced bioavailability (19-fold) of Capsifen compared with that of unformulated capsaicinoids. The product was also determined safe via gastric mucosa irritation test and demonstrated significant anti-obesity effect in high fat diet-induced hypercholesteremic rats.
“Capsifen opens up a new arena to the formulators and Nutraceutical manufacturers to make utilise the remarkable benefits of red chili capsaicinoids, with 100% natural and vegan claims,” said Mr Emmanuel, CMO at Akay.
A Joseph et al. Journal of Functional Foods 85 (2021); A green approach for the sustained intestinal delivery of red chili (capsicum annum L) extracted capsaicinoids with enhanced bioavailability