Dextrin-Based Nanohydrogels for Rokitamycin Prolonged Topical Delivery

Macrolides are widely used antibiotics with a broad spectrum of activity. The development of drug carriers to deliver this type of antibiotics has attracted much research. The present study aims at developing new swellable dextrin-based nanohydrogels for the topical delivery of rokitamycin, as model...

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Main Authors: Maria Tannous, Silvia Lucia Appleton, Gjylije Hoti, Fabrizio Caldera, Monica Argenziano, Yousef Khazaei Monfared, Adrián Matencio, Francesco Trotta, Roberta Cavalli
Format: Article
Language:English
Published: MDPI AG 2022-08-01
Series:Gels
Subjects:
Online Access:https://www.mdpi.com/2310-2861/8/8/490
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author Maria Tannous
Silvia Lucia Appleton
Gjylije Hoti
Fabrizio Caldera
Monica Argenziano
Yousef Khazaei Monfared
Adrián Matencio
Francesco Trotta
Roberta Cavalli
author_facet Maria Tannous
Silvia Lucia Appleton
Gjylije Hoti
Fabrizio Caldera
Monica Argenziano
Yousef Khazaei Monfared
Adrián Matencio
Francesco Trotta
Roberta Cavalli
author_sort Maria Tannous
collection DOAJ
description Macrolides are widely used antibiotics with a broad spectrum of activity. The development of drug carriers to deliver this type of antibiotics has attracted much research. The present study aims at developing new swellable dextrin-based nanohydrogels for the topical delivery of rokitamycin, as model macrolide. Rokitamycin is a synthetic analogous of macrolides with advantageous characteristics as far as bacterial uptake and post-antibiotic effect are concerned. It is also indicated for the treatment of severe infections caused by <i>Acanthamoeba</i> and for topical infections. The nanohydrogels have been prepared from two types of cross-linked polymers obtained by using β-cyclodextrin or Linecaps<sup>®</sup> was provided by the Roquette Italia SPA (Cassano Spinola, Al, Italy) as building blocks. The cross-linked polymers have been then formulated into aqueous nanosuspensions refined and tuned to achieve the incorporation of the drug. Cross-linked β-cyclodextrin (β-CD) and Linecaps<sup>®</sup> (LC) polymers formed dextrin-based nanohydrogels with high swelling degree and mucoadhesion capability. Rokitamycin was loaded into the nanohydrogels displaying an average size around 200 nm with negative surface charge. In vitro kinetic profiles of free and loaded drug in nanohydrogels were compared at two pH levels. Interestingly, a sustained and controlled release was obtained at skin pH level due to the high degree of swelling and a pH responsiveness possibly. The results collected suggest that these nanohydrogels are promising for the delivery of rokitamycin and may pave the way for the topical delivery of other macrolide antibiotics.
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spelling doaj.art-0e059e0ee4c149e5bb8d4135612c33792023-12-01T23:43:36ZengMDPI AGGels2310-28612022-08-018849010.3390/gels8080490Dextrin-Based Nanohydrogels for Rokitamycin Prolonged Topical DeliveryMaria Tannous0Silvia Lucia Appleton1Gjylije Hoti2Fabrizio Caldera3Monica Argenziano4Yousef Khazaei Monfared5Adrián Matencio6Francesco Trotta7Roberta Cavalli8Dipartimento di Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Turin, ItalyDipartimento di Chimica, Università di Torino, Via P. Giuria 7, 10125 Torino, ItalyDipartimento di Chimica, Università di Torino, Via P. Giuria 7, 10125 Torino, ItalyDipartimento di Chimica, Università di Torino, Via P. Giuria 7, 10125 Torino, ItalyDipartimento di Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Turin, ItalyDipartimento di Chimica, Università di Torino, Via P. Giuria 7, 10125 Torino, ItalyDipartimento di Chimica, Università di Torino, Via P. Giuria 7, 10125 Torino, ItalyDipartimento di Chimica, Università di Torino, Via P. Giuria 7, 10125 Torino, ItalyDipartimento di Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Turin, ItalyMacrolides are widely used antibiotics with a broad spectrum of activity. The development of drug carriers to deliver this type of antibiotics has attracted much research. The present study aims at developing new swellable dextrin-based nanohydrogels for the topical delivery of rokitamycin, as model macrolide. Rokitamycin is a synthetic analogous of macrolides with advantageous characteristics as far as bacterial uptake and post-antibiotic effect are concerned. It is also indicated for the treatment of severe infections caused by <i>Acanthamoeba</i> and for topical infections. The nanohydrogels have been prepared from two types of cross-linked polymers obtained by using β-cyclodextrin or Linecaps<sup>®</sup> was provided by the Roquette Italia SPA (Cassano Spinola, Al, Italy) as building blocks. The cross-linked polymers have been then formulated into aqueous nanosuspensions refined and tuned to achieve the incorporation of the drug. Cross-linked β-cyclodextrin (β-CD) and Linecaps<sup>®</sup> (LC) polymers formed dextrin-based nanohydrogels with high swelling degree and mucoadhesion capability. Rokitamycin was loaded into the nanohydrogels displaying an average size around 200 nm with negative surface charge. In vitro kinetic profiles of free and loaded drug in nanohydrogels were compared at two pH levels. Interestingly, a sustained and controlled release was obtained at skin pH level due to the high degree of swelling and a pH responsiveness possibly. The results collected suggest that these nanohydrogels are promising for the delivery of rokitamycin and may pave the way for the topical delivery of other macrolide antibiotics.https://www.mdpi.com/2310-2861/8/8/490rokitamycincyclodextrinlinecapsnanospongesformulationnanohydrogels
spellingShingle Maria Tannous
Silvia Lucia Appleton
Gjylije Hoti
Fabrizio Caldera
Monica Argenziano
Yousef Khazaei Monfared
Adrián Matencio
Francesco Trotta
Roberta Cavalli
Dextrin-Based Nanohydrogels for Rokitamycin Prolonged Topical Delivery
Gels
rokitamycin
cyclodextrin
linecaps
nanosponges
formulation
nanohydrogels
title Dextrin-Based Nanohydrogels for Rokitamycin Prolonged Topical Delivery
title_full Dextrin-Based Nanohydrogels for Rokitamycin Prolonged Topical Delivery
title_fullStr Dextrin-Based Nanohydrogels for Rokitamycin Prolonged Topical Delivery
title_full_unstemmed Dextrin-Based Nanohydrogels for Rokitamycin Prolonged Topical Delivery
title_short Dextrin-Based Nanohydrogels for Rokitamycin Prolonged Topical Delivery
title_sort dextrin based nanohydrogels for rokitamycin prolonged topical delivery
topic rokitamycin
cyclodextrin
linecaps
nanosponges
formulation
nanohydrogels
url https://www.mdpi.com/2310-2861/8/8/490
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