Design of a Nasal Spray Based on Cardiospermum halicacabum Extract Loaded in Phospholipid Vesicles Enriched with Gelatin or Chondroitin Sulfate

The extract of Cardiospermum halicacabum L. (C. halicacabum) obtained from flower, leaf and vine was loaded into modified phospholipid vesicles aiming at obtaining sprayable, biocompatible and effective nasal spray formulations for the treatment of nasopharyngea...

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Autores principales:	Eleonora Casula, Maria Manconi, José Antonio Vázquez, Tania Belen Lopez-Mendez, José Luis Pedraz, Esteban Calvo, Antonio Lozano, Marco Zaru, Andreia Ascenso, Maria Letizia Manca
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	<i>Cardiospermum halicacabum</i> epithelial cells droplet size distribution plume angle antioxidant activity keratinocytes Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/78f15f39eaac4f78ba3f10503c1f4d71
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spelling	oai:doaj.org-article:78f15f39eaac4f78ba3f10503c1f4d712021-11-11T18:37:54ZDesign of a Nasal Spray Based on <i>Cardiospermum halicacabum</i> Extract Loaded in Phospholipid Vesicles Enriched with Gelatin or Chondroitin Sulfate10.3390/molecules262166701420-3049https://doaj.org/article/78f15f39eaac4f78ba3f10503c1f4d712021-11-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6670https://doaj.org/toc/1420-3049The extract of <i>Cardiospermum halicacabum</i> L. (<i>C. halicacabum</i>) obtained from flower, leaf and vine was loaded into modified phospholipid vesicles aiming at obtaining sprayable, biocompatible and effective nasal spray formulations for the treatment of nasopharyngeal diseases. Penetration enhancer-containing vesicles (PEVs) and hyalurosomes were formulated, and stabilized by adding a commercial gelatin from fish (20 mg/mL) or chondroitin sulfate from catshark cartilages (<i>Scyliorhinus canicula,</i> 20 mg/mL). Cryo-TEM images confirmed the formation of spherical vesicles, while photon correlation spectroscopy analysis disclosed the formation of small and negatively-charged vesicles. PEVs were the smaller vesicles (~100 nm) along with gelatin-hyalurosomes (~120 nm), while chondroitin-PEVs and chondroitin-hyalurosomes were larger (~160 nm). Dispersions prepared with chondroitin sulfate were more homogeneous, as the polydispersity index was ~0.15. The in vitro analysis of the droplet size distribution, average velocity module and spray cone angle suggested a good spray-ability and deposition of formulations in the nasal cavity, as the mean diameter of the droplets was in the range recommended by the Food and Drug Administration for nasal targets. The spray plume analysis confirmed the ability of PEVs, gelatin-PEVs, hyalurosomes and gelatin-hyalurosomes to be atomized in fine droplets homogenously distributed in a full cone plume, with an angle ranging from 25 to 30°. Moreover, vesicles were highly biocompatible and capable of protecting the epithelial cells against oxidative damage, thus preventing the inflammatory state.Eleonora CasulaMaria ManconiJosé Antonio VázquezTania Belen Lopez-MendezJosé Luis PedrazEsteban CalvoAntonio LozanoMarco ZaruAndreia AscensoMaria Letizia MancaMDPI AGarticle<i>Cardiospermum halicacabum</i>epithelial cellsdroplet size distributionplume angleantioxidant activitykeratinocytesOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6670, p 6670 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	<i>Cardiospermum halicacabum</i> epithelial cells droplet size distribution plume angle antioxidant activity keratinocytes Organic chemistry QD241-441
spellingShingle	<i>Cardiospermum halicacabum</i> epithelial cells droplet size distribution plume angle antioxidant activity keratinocytes Organic chemistry QD241-441 Eleonora Casula Maria Manconi José Antonio Vázquez Tania Belen Lopez-Mendez José Luis Pedraz Esteban Calvo Antonio Lozano Marco Zaru Andreia Ascenso Maria Letizia Manca Design of a Nasal Spray Based on <i>Cardiospermum halicacabum</i> Extract Loaded in Phospholipid Vesicles Enriched with Gelatin or Chondroitin Sulfate
description	The extract of <i>Cardiospermum halicacabum</i> L. (<i>C. halicacabum</i>) obtained from flower, leaf and vine was loaded into modified phospholipid vesicles aiming at obtaining sprayable, biocompatible and effective nasal spray formulations for the treatment of nasopharyngeal diseases. Penetration enhancer-containing vesicles (PEVs) and hyalurosomes were formulated, and stabilized by adding a commercial gelatin from fish (20 mg/mL) or chondroitin sulfate from catshark cartilages (<i>Scyliorhinus canicula,</i> 20 mg/mL). Cryo-TEM images confirmed the formation of spherical vesicles, while photon correlation spectroscopy analysis disclosed the formation of small and negatively-charged vesicles. PEVs were the smaller vesicles (~100 nm) along with gelatin-hyalurosomes (~120 nm), while chondroitin-PEVs and chondroitin-hyalurosomes were larger (~160 nm). Dispersions prepared with chondroitin sulfate were more homogeneous, as the polydispersity index was ~0.15. The in vitro analysis of the droplet size distribution, average velocity module and spray cone angle suggested a good spray-ability and deposition of formulations in the nasal cavity, as the mean diameter of the droplets was in the range recommended by the Food and Drug Administration for nasal targets. The spray plume analysis confirmed the ability of PEVs, gelatin-PEVs, hyalurosomes and gelatin-hyalurosomes to be atomized in fine droplets homogenously distributed in a full cone plume, with an angle ranging from 25 to 30°. Moreover, vesicles were highly biocompatible and capable of protecting the epithelial cells against oxidative damage, thus preventing the inflammatory state.
format	article
author	Eleonora Casula Maria Manconi José Antonio Vázquez Tania Belen Lopez-Mendez José Luis Pedraz Esteban Calvo Antonio Lozano Marco Zaru Andreia Ascenso Maria Letizia Manca
author_facet	Eleonora Casula Maria Manconi José Antonio Vázquez Tania Belen Lopez-Mendez José Luis Pedraz Esteban Calvo Antonio Lozano Marco Zaru Andreia Ascenso Maria Letizia Manca
author_sort	Eleonora Casula
title	Design of a Nasal Spray Based on <i>Cardiospermum halicacabum</i> Extract Loaded in Phospholipid Vesicles Enriched with Gelatin or Chondroitin Sulfate
title_short	Design of a Nasal Spray Based on <i>Cardiospermum halicacabum</i> Extract Loaded in Phospholipid Vesicles Enriched with Gelatin or Chondroitin Sulfate
title_full	Design of a Nasal Spray Based on <i>Cardiospermum halicacabum</i> Extract Loaded in Phospholipid Vesicles Enriched with Gelatin or Chondroitin Sulfate
title_fullStr	Design of a Nasal Spray Based on <i>Cardiospermum halicacabum</i> Extract Loaded in Phospholipid Vesicles Enriched with Gelatin or Chondroitin Sulfate
title_full_unstemmed	Design of a Nasal Spray Based on <i>Cardiospermum halicacabum</i> Extract Loaded in Phospholipid Vesicles Enriched with Gelatin or Chondroitin Sulfate
title_sort	design of a nasal spray based on <i>cardiospermum halicacabum</i> extract loaded in phospholipid vesicles enriched with gelatin or chondroitin sulfate
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/78f15f39eaac4f78ba3f10503c1f4d71
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Design of a Nasal Spray Based on <i>Cardiospermum halicacabum</i> Extract Loaded in Phospholipid Vesicles Enriched with Gelatin or Chondroitin Sulfate

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