Prunus spinosa Extract Loaded in Biomimetic Nanoparticles Evokes In Vitro Anti-Inflammatory and Wound Healing Activities.

Mattia Tiboni,Michele Guescini,Giancarlo Verardo,Andrea Gorassini,Mariastella Colomba,Daniele Fraternale,Sofia Coppari,Roberto Molinaro,Barbara Di Giacomo,Michele Mari,Seeram Ramakrishna,Luca Casettari,Loretta Guidi,Maria Cristina Albertini

doi:10.3390/nano11010036

Abstract

Prunus spinosa fruits (PSF) contain different phenolic compounds showing antioxidant and anti-inflammatory activities. Innovative drug delivery systems such as biomimetic nanoparticles could improve the activity of PSF extract by promoting (i) the protection of payload into the lipidic bilayer, (ii) increased accumulation to the diseased tissue due to specific targeting properties, (iii) improved biocompatibility, (iv) low toxicity and increased bioavailability. Using membrane proteins extracted from human monocyte cell line THP-1 cells and a mixture of phospholipids, we formulated two types of PSF-extract-loaded biomimetic vesicles differing from each other for the presence of either 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) or 1,2-dioleoyl-sn-glycero-3-phospho-(1′-rac-glycerol) (DOPG). The biological activity of free extract (PSF), compared to both types of extract-loaded vesicles (PSF-DOPCs and PSF-DOPGs) and empty vesicles (DOPCs and DOPGs), was evaluated in vitro on HUVEC cells. PSF-DOPCs showed preferential incorporation of the extract. When enriched into the nanovesicles, the extract showed a significantly increased anti-inflammatory activity, and a pronounced wound-healing effect (with PSF-DOPCs more efficient than PSF-DOPGs) compared to free PSF. This innovative drug delivery system, combining nutraceutical active ingredients into a biomimetic formulation, represents a possible adjuvant therapy for the treatment of wound healing. This nanoplatform could be useful for the encapsulation/enrichment of other nutraceutical products with short stability and low bioavailability.

Highlights

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We undertook to characterize the contribution of two different lipid mixtures having the DPPC:DSPC:CHOL as lipid backbone by adding either DOPC or dioleoyl-sn-glycero-3phospho-(1 -rac-glycerol) (DOPG) to obtain an almost neutral (DOPCs) or negatively charged formulation (DOPGs)
−28 mV before and after Prunus spinosa fruits (PSF)-loading, respectively), while a very slight difference could be observed for the DOPCs (−13 vs. −11 mV before and after PSF-loading, respectively). These findings reveal a different effect of PSF incorporation in the two formulations, which was predictable considering both the heterogeneity of PSF composition and the net difference between DOPC and DOPG, which confer distinct physicochemical properties to the vesicles

Summary

Introduction

Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. When enriched into the nanovesicles, the extract showed a significantly increased anti-inflammatory activity, and a pronounced wound-healing effect (with PSF-DOPCs more efficient than PSF-DOPGs) compared to free PSF. This innovative drug delivery system, combining nutraceutical active ingredients into a biomimetic formulation, represents a possible adjuvant therapy for the treatment of wound healing. This nanoplatform could be useful for the encapsulation/enrichment of other nutraceutical products with short stability and low bioavailability.

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Results

Discussion

Conclusion