Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol

Vanna Sanna,1 Anna Maria Roggio,1 Silvia Siliani,1 Massimo Piccinini,1 Salvatore Marceddu,2 Alberto Mariani,3 Mario Sechi31Porto Conte Ricerche, Alghero, Italy; 2Istituto di Scienze delle Produzioni Alimentari (ISPA), Consiglio Nazionale delle Ricerche (CNR), Sezione di Sassari, Italy; 3Department o...

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Main Authors: Sanna V, Roggio AM, Siliani S, Piccinini M, Marceddu S, Mariani A, Sechi M
Format: Article
Language:English
Published: Dove Medical Press 2012-10-01
Series:International Journal of Nanomedicine
Online Access:http://www.dovepress.com/development-of-novel-cationic-chitosan--and-anionic-alginatendashcoate-a11284
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author Sanna V
Roggio AM
Siliani S
Piccinini M
Marceddu S
Mariani A
Sechi M
author_facet Sanna V
Roggio AM
Siliani S
Piccinini M
Marceddu S
Mariani A
Sechi M
author_sort Sanna V
collection DOAJ
description Vanna Sanna,1 Anna Maria Roggio,1 Silvia Siliani,1 Massimo Piccinini,1 Salvatore Marceddu,2 Alberto Mariani,3 Mario Sechi31Porto Conte Ricerche, Alghero, Italy; 2Istituto di Scienze delle Produzioni Alimentari (ISPA), Consiglio Nazionale delle Ricerche (CNR), Sezione di Sassari, Italy; 3Department of Chemistry and Pharmacy, University of Sassari, Sassari, ItalyBackground: Resveratrol, like other natural polyphenols, is an extremely photosensitive compound with low chemical stability, which limits the therapeutic application of its beneficial effects. The development of innovative formulation strategies, able to overcome physicochemical and pharmacokinetic limitations of this compound, may be achieved via suitable carriers able to associate controlled release and protection. In this context, nanotechnology is proving to be a powerful strategy. In this study, we developed novel cationic chitosan (CS)- and anionic alginate (Alg)-coated poly(d,l-lactide-co-glycolide) nanoparticles (NPs) loaded with the bioactive polyphenolic trans-(E)-resveratrol (RSV) for biomedical applications.Methods: NPs were prepared by the nanoprecipitation method and characterized in terms of morphology, size and zeta potential, encapsulation efficiency, Raman spectroscopy, swelling properties, differential scanning calorimetry, and in vitro release studies. The protective effect of the nanosystems under the light-stressed RSV and long-term stability were investigated.Results: NPs turned out to be spherical in shape, with size ranging from 135 to about 580 nm, depending on the composition and the amount of polyelectrolytes, while the encapsulation efficiencies increased from 8% of uncoated poly(d,l-lactide-co-glycolide) (PLGA) to 23% and 32% of Alg- and CS-coated PLGA NPs, respectively. All nanocarriers are characterized by a biphasic release pattern, and more effective controlled release rates are obtained for NPs formulated with higher polyelectrolyte concentrations. Stability studies revealed that encapsulation provides significant protection against light-exposure degradation, by reducing the trans–cis photoisomerization reaction. Moreover, the nanosystems are able to prevent the degradation of trans isoform and the leakage of RSV from the carrier for a period of 6 months.Conclusion: Our findings indicated that the newly developed CS- and Alg-coated PLGA NPs are suitable to be used for the delivery of bioactive RSV. The encapsulation of RSV into optimized polymeric NPs provides improved drug loading, effective controlled release, and protection against light-exposure degradation, thus opening new perspectives for the delivery of bioactive related phytochemicals to be used for (nano)chemoprevention/chemotherapy.Keywords: resveratrol, nanochemoprevention, PLGA, chitosan, alginate, nanoparticles
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spelling doaj.art-0b5ddbe6eabd4f688952480c603aba432022-12-21T19:19:34ZengDove Medical PressInternational Journal of Nanomedicine1176-91141178-20132012-10-012012default55015516Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrolSanna VRoggio AMSiliani SPiccinini MMarceddu SMariani ASechi MVanna Sanna,1 Anna Maria Roggio,1 Silvia Siliani,1 Massimo Piccinini,1 Salvatore Marceddu,2 Alberto Mariani,3 Mario Sechi31Porto Conte Ricerche, Alghero, Italy; 2Istituto di Scienze delle Produzioni Alimentari (ISPA), Consiglio Nazionale delle Ricerche (CNR), Sezione di Sassari, Italy; 3Department of Chemistry and Pharmacy, University of Sassari, Sassari, ItalyBackground: Resveratrol, like other natural polyphenols, is an extremely photosensitive compound with low chemical stability, which limits the therapeutic application of its beneficial effects. The development of innovative formulation strategies, able to overcome physicochemical and pharmacokinetic limitations of this compound, may be achieved via suitable carriers able to associate controlled release and protection. In this context, nanotechnology is proving to be a powerful strategy. In this study, we developed novel cationic chitosan (CS)- and anionic alginate (Alg)-coated poly(d,l-lactide-co-glycolide) nanoparticles (NPs) loaded with the bioactive polyphenolic trans-(E)-resveratrol (RSV) for biomedical applications.Methods: NPs were prepared by the nanoprecipitation method and characterized in terms of morphology, size and zeta potential, encapsulation efficiency, Raman spectroscopy, swelling properties, differential scanning calorimetry, and in vitro release studies. The protective effect of the nanosystems under the light-stressed RSV and long-term stability were investigated.Results: NPs turned out to be spherical in shape, with size ranging from 135 to about 580 nm, depending on the composition and the amount of polyelectrolytes, while the encapsulation efficiencies increased from 8% of uncoated poly(d,l-lactide-co-glycolide) (PLGA) to 23% and 32% of Alg- and CS-coated PLGA NPs, respectively. All nanocarriers are characterized by a biphasic release pattern, and more effective controlled release rates are obtained for NPs formulated with higher polyelectrolyte concentrations. Stability studies revealed that encapsulation provides significant protection against light-exposure degradation, by reducing the trans–cis photoisomerization reaction. Moreover, the nanosystems are able to prevent the degradation of trans isoform and the leakage of RSV from the carrier for a period of 6 months.Conclusion: Our findings indicated that the newly developed CS- and Alg-coated PLGA NPs are suitable to be used for the delivery of bioactive RSV. The encapsulation of RSV into optimized polymeric NPs provides improved drug loading, effective controlled release, and protection against light-exposure degradation, thus opening new perspectives for the delivery of bioactive related phytochemicals to be used for (nano)chemoprevention/chemotherapy.Keywords: resveratrol, nanochemoprevention, PLGA, chitosan, alginate, nanoparticleshttp://www.dovepress.com/development-of-novel-cationic-chitosan--and-anionic-alginatendashcoate-a11284
spellingShingle Sanna V
Roggio AM
Siliani S
Piccinini M
Marceddu S
Mariani A
Sechi M
Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol
International Journal of Nanomedicine
title Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol
title_full Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol
title_fullStr Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol
title_full_unstemmed Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol
title_short Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol
title_sort development of novel cationic chitosan and anionic alginate amp ndash coated poly d l lactide co glycolide nanoparticles for controlled release and light protection of resveratrol
url http://www.dovepress.com/development-of-novel-cationic-chitosan--and-anionic-alginatendashcoate-a11284
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