Preparation of pellets containing Pothomorphe umbellata extracts by extrusion-spheronization: improvement of 4-nerolidylcatechol photostability

Abstract

Pothomorphe umbellata (L.) Miq., Piperaceae, has been extensively used in Brazilian folk medicine and it is well known for its strong antioxidant properties. However, its main active constituent, 4-nerolydilcatechol (4-NC), is sensitive to ultraviolet and visible light, which can limit the use of intermediate and final herbal preparations of this species. In the present work, coated multiparticulate solid dosage forms of P. umbellata were obtained with the purpose of increasing the stability of 4-NC. P. umbellata extract was used as a wetting liquid for the preparation of pellets by extrusion-spheronization. Pellets were coated in a fluidized bed by three different polymers (hydroxypropylmethylcellulose (HPMC), polyvynilpirrolidone K-30 (PVP-K30), and polyvinyl alcohol-polyethylene glycol graft-copolymer (PVAPEG)). 4-NC photostability was evaluated by an accelerated photostability protocol. Pellets showed a narrow size distribution and low friability. 4-NC photodegradation followed a second order degradation kinetics with similar k values for the percolate, uncoated pellets and HPMC coated pellets. Photoprotection was higher in pellets coated with PVP-K30 and PVA-PEG. PVA-PEG coated pellets with 6 and 9% weight gain resulted in a final concentration of 4-NC approximately cinco times higher than uncoated pellets or liquid extracts, suggesting the potential of this formulation as a multiparticulate solid dosage form for P. umbellata extracts

Physical characterization of multiparticulate systems

“…Obtention of immediate-release systems, with a focus on masking drug flavor (Hamedelniel, Bajdik, Pintye-Hódi, 2010;Issa et al, 2012b;Patel, Patel, Patel, 2010);  Controlled-release (Abbaspour, Sadeghi, Garekani, 2008;Bialleck, Rein, 2011;Cantor, Hoag, Augsburger, 2009a;Cantor, Hoag, Augsburger, 2009b;Franc et al, 2015;Ghanam, Kleinebudde, 2011;Ghosh, Chakraborty, 2013;Han et al, 2013;Heckötter et al, 2011;Hung et al, 2015;Ríos, Ghaly, 2015;Roblegg et al, 2011;Szkutnik-Fiedler et al, 2014;Wang et al, 2015;Xu, Liew, Heng, 2015;You et al, 2014);  Improvement in dissolution of poorly soluble drugs (Abdalla, Mader, 2007;Abdalla, Klein, Mader, 2008;Chopra, Venkatesan, Betageri, 2013;Ibrahim, El-Badry, 2014;Lu et al, 2009;Patel et al, 2016);  Gastro-retentive systems/ floating systems (Amrutkar, Chaudhari, Patil, 2012;Li et al, 2014;Pagariya, Patil, 2013;Qi et al, 2015;Zhang et al, 2012);  Enteric release/gastro-resistant systems (Andreo-Filho et al, 2009;Ghanam, Kleinebudde, 2011;Pund et al, 2010);  Improvement of plant extract or active ingredient stability (Araújo-Junior et al, 2013;Beringhs et al, 2012;Bu...…”

Preparation of pellets containing a standardized Artemisia annua L. extract by extrusion-spheronization

“…Accordingly, the best approach seems to be the use of phytotherapic products prepared from standardized vegetable extracts which should present an appropriate content of the active ingredient, as well as adequate flowability, density and hygroscopicity [10,11] . Industrial production of pellets is a promising strategy to improve the technological properties of vegetable extracts [11][12][13][14] . Additionally, pellets can ensure a proper drug dissolution rate with less irritation of the gastrointestinal tract [15] .…”

“…Lastly, pellets are especially advantageous when the active component is in great amounts in the formulation, because of its high density [16] . Among the technologies available for pelletization, the extrusion-spheronization technique is one of the most commonly used and has been successfully applied to herbal products [11][12][13] .…”

Microemulsion based on Pterodon emarginatus oil and its anti-inflammatory potential

“…The technological development of research on pharmaceutical forms containing herbal materials has expanded over recent decades and contributed to innovation in the pharmaceutical sector (Bassani, González, Petrovick, 2005;Calixto, 2005;Rocha et al, 2008;Araújo-Júnior et al, 2013;Beringhs et al, 2013;Couto et al, 2013;Klein et al, 2013;Quintão et al, 2013).…”