Protein free microcapsules obtained from plant spores as a model for drug delivery: ibuprofen encapsulation, release and taste masking

Abstract

Sporopollenin exine capsules (SEC) extracted from Lycopodium clavatum spores were shown to encapsulate ibuprofen as a drug model, with 97 AE 1% efficiency as measured by recovery of the loaded drug and absence of the drug on the SEC surface by scanning electron microscopy (SEM). The encapsulated ibuprofen was shown to be unchanged from its bulk crystalline form by solid state NMR, FTIR and XRD. Essential for drug delivery applications, SEC were shown to be non-toxic to human endothelial cells and free of allergenic protein epitopes by MALDI-TOF-MS and ESI-QqToF-MS. Potential application for targeted release into the intestinal region of the gastrointestinal tract (GIT) was demonstrated by 88 AE 1% of the drug being retained in simulated gastric fluid (SGF) after 45 minutes and 85 AE 2% being released after 5 min in buffer (PBS; pH 7.4). The SEC were shown to provide significant taste masking of encapsulated ibuprofen in a double blind trial with 10 human volunteers.

Lycopodium Spores: A Naturally Manufactured, Superrobust Biomaterial for Drug Delivery

“…Our results with natural spores support previous studies using exine capsules, which indicate the lack of a barrier to retard macromolecule release in SGF and SIF for a longer period of time. [ 7,16,18 ] Similar drug release profi les were reported with the use of processed sporopollenin microcapsules extracted from L. clavatum spores. [ 16,18 ] To explore the structural changes after FITC-conjugated BSA release in PBS, we performed CLSM after complete release and Adv.…”

“…[30][31][32] Most conventional techniques used for encapsulation such as emulsion solvent evaporation, spray drying, and chemical conjugation fail to reliably provide either size monodispersity or well-defi ned microstructures. [ 26,27,[30][31][32] Although several studies have reported the use of empty exine microcapsules for the encapsulation of drugs, vaccines, and magnetic resonance imaging (MRI) contrast agents, as well as for use in cosmetics and food supplements, [ 7,[16][17][18]22 ] the use of the natural "spores" as a microencapsulation material and delivery vehicle still remains unexplored. In this regard, we have directed our efforts toward exploring systems to produce macromoleculeloaded spores using three different microencapsulation techniques.…”

Hollow Pollen Shells to Enhance Drug Delivery

“…Any protein in the raw material is eradicated during the extraction to produce allergen free, non-toxic shells [20]. …”

Sporopollenin, The Least Known Yet Toughest Natural Biopolymer

“…After this process, the cells still remain viable within the chamber and the exines undamaged, which further illustrate the remarkable elasticity and physical robustness of the exines. The potential for sporopollenin exines to be used in food and pharmaceutical applications has been demonstrated by their having taste-masking properties to the tongue when encapsulated with, such as fish oil and ibuprofen (Diego-Taboada et al, 2013). Also, the exines were shown to encapsulate a commercial gadolinium(III) MRI contrast agent and allow slow release over 8 h in blood plasma (Lorch et al, 2009).…”

“…Also, the exines were shown to encapsulate a commercial gadolinium(III) MRI contrast agent and allow slow release over 8 h in blood plasma (Lorch et al, 2009). In vitro studies have shown exines to have the potential to act as an effective drug delivery vector in which release can be triggered by pH (Beckett et al, 2009;Diego-Taboada et al, 2013).…”