Enhanced Loading Efficiency and Mucoadhesion Properties of Gellan Gum Thin Films by Complexation with Hydroxypropyl-β-Cyclodextrin

Polymeric oral thin films (OTFs) were prepared by the casting method, combining gellan gum (GG), a water-soluble polysaccharide, and glycerol (Gly) as a plasticizing agent. GG-Gly films were investigated as potential systems for buccal drug delivery using fluconazole (Class I of the Biopharmaceutica...

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Main Authors: Alessandra Adrover, Laura di Muzio, Jordan Trilli, Chiara Brandelli, Patrizia Paolicelli, Stefania Petralito, Maria Antonietta Casadei
Format: Article
Language:English
Published: MDPI AG 2020-08-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/12/9/819
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author Alessandra Adrover
Laura di Muzio
Jordan Trilli
Chiara Brandelli
Patrizia Paolicelli
Stefania Petralito
Maria Antonietta Casadei
author_facet Alessandra Adrover
Laura di Muzio
Jordan Trilli
Chiara Brandelli
Patrizia Paolicelli
Stefania Petralito
Maria Antonietta Casadei
author_sort Alessandra Adrover
collection DOAJ
description Polymeric oral thin films (OTFs) were prepared by the casting method, combining gellan gum (GG), a water-soluble polysaccharide, and glycerol (Gly) as a plasticizing agent. GG-Gly films were investigated as potential systems for buccal drug delivery using fluconazole (Class I of the Biopharmaceutical Classification System) as a model drug. At a low concentration of Gly drug precipitation occurred while, for higher concentrations of Gly, a significant deterioration of mucoadhesive and mechanical properties was observed. One possible way to overcome all these problems could be the addition of hydroxypropyl-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-cyclodextrin (HP-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-CD) to the GG-Gly formulation as a drug-precipitation inhibitor. In this work the effect of cyclodextrin addition on the mechanical, mucoadhesive, swelling and release properties of GG-Gly films was investigated. In-vitro drug release studies were carried out using the paddle type dissolution apparatus (USP II) and the millifluidic flow-through device (MFTD). A moving-boundary model for swelling dynamics and release in USP II is proposed to estimate the effective diffusivity of the solvent, HP-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-CD, fluconazole and complex fluconazole/HP-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-CD in the swelling film. Experimental results, supported by theoretical modeling, confirmed that gellan gum-low glycerol thin films including HP-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-CD represent a suitable formulation for fluconazole drug delivery. A sustained release was observed when GG-Gly film is loaded with a preformed complex fluconazole/HP-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-CD.
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spelling doaj.art-271c5d2609d0490ba593c7a05385fe912023-11-20T11:42:47ZengMDPI AGPharmaceutics1999-49232020-08-0112981910.3390/pharmaceutics12090819Enhanced Loading Efficiency and Mucoadhesion Properties of Gellan Gum Thin Films by Complexation with Hydroxypropyl-β-CyclodextrinAlessandra Adrover0Laura di Muzio1Jordan Trilli2Chiara Brandelli3Patrizia Paolicelli4Stefania Petralito5Maria Antonietta Casadei6Dipartimento di Ingegneria Chimica, Materiali e Ambiente, Sapienza Universitá di Roma, Via Eudossiana 18, 00184 Rome, ItalyDipartimento di Chimica e Tecnologia del Farmaco, Sapienza Universitá di Roma, Piazzale Aldo Moro 5, 00185 Rome, ItalyDipartimento di Chimica e Tecnologia del Farmaco, Sapienza Universitá di Roma, Piazzale Aldo Moro 5, 00185 Rome, ItalyDipartimento di Chimica e Tecnologia del Farmaco, Sapienza Universitá di Roma, Piazzale Aldo Moro 5, 00185 Rome, ItalyDipartimento di Chimica e Tecnologia del Farmaco, Sapienza Universitá di Roma, Piazzale Aldo Moro 5, 00185 Rome, ItalyDipartimento di Chimica e Tecnologia del Farmaco, Sapienza Universitá di Roma, Piazzale Aldo Moro 5, 00185 Rome, ItalyDipartimento di Chimica e Tecnologia del Farmaco, Sapienza Universitá di Roma, Piazzale Aldo Moro 5, 00185 Rome, ItalyPolymeric oral thin films (OTFs) were prepared by the casting method, combining gellan gum (GG), a water-soluble polysaccharide, and glycerol (Gly) as a plasticizing agent. GG-Gly films were investigated as potential systems for buccal drug delivery using fluconazole (Class I of the Biopharmaceutical Classification System) as a model drug. At a low concentration of Gly drug precipitation occurred while, for higher concentrations of Gly, a significant deterioration of mucoadhesive and mechanical properties was observed. One possible way to overcome all these problems could be the addition of hydroxypropyl-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-cyclodextrin (HP-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-CD) to the GG-Gly formulation as a drug-precipitation inhibitor. In this work the effect of cyclodextrin addition on the mechanical, mucoadhesive, swelling and release properties of GG-Gly films was investigated. In-vitro drug release studies were carried out using the paddle type dissolution apparatus (USP II) and the millifluidic flow-through device (MFTD). A moving-boundary model for swelling dynamics and release in USP II is proposed to estimate the effective diffusivity of the solvent, HP-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-CD, fluconazole and complex fluconazole/HP-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-CD in the swelling film. Experimental results, supported by theoretical modeling, confirmed that gellan gum-low glycerol thin films including HP-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-CD represent a suitable formulation for fluconazole drug delivery. A sustained release was observed when GG-Gly film is loaded with a preformed complex fluconazole/HP-<inline-formula><math display="inline"><semantics><mi mathvariant="sans-serif">β</mi></semantics></math></inline-formula>-CD.https://www.mdpi.com/1999-4923/12/9/819thin filmsdrug deliverygellan gumcyclodextrinsUSP IImillifluidic flow-through device
spellingShingle Alessandra Adrover
Laura di Muzio
Jordan Trilli
Chiara Brandelli
Patrizia Paolicelli
Stefania Petralito
Maria Antonietta Casadei
Enhanced Loading Efficiency and Mucoadhesion Properties of Gellan Gum Thin Films by Complexation with Hydroxypropyl-β-Cyclodextrin
Pharmaceutics
thin films
drug delivery
gellan gum
cyclodextrins
USP II
millifluidic flow-through device
title Enhanced Loading Efficiency and Mucoadhesion Properties of Gellan Gum Thin Films by Complexation with Hydroxypropyl-β-Cyclodextrin
title_full Enhanced Loading Efficiency and Mucoadhesion Properties of Gellan Gum Thin Films by Complexation with Hydroxypropyl-β-Cyclodextrin
title_fullStr Enhanced Loading Efficiency and Mucoadhesion Properties of Gellan Gum Thin Films by Complexation with Hydroxypropyl-β-Cyclodextrin
title_full_unstemmed Enhanced Loading Efficiency and Mucoadhesion Properties of Gellan Gum Thin Films by Complexation with Hydroxypropyl-β-Cyclodextrin
title_short Enhanced Loading Efficiency and Mucoadhesion Properties of Gellan Gum Thin Films by Complexation with Hydroxypropyl-β-Cyclodextrin
title_sort enhanced loading efficiency and mucoadhesion properties of gellan gum thin films by complexation with hydroxypropyl β cyclodextrin
topic thin films
drug delivery
gellan gum
cyclodextrins
USP II
millifluidic flow-through device
url https://www.mdpi.com/1999-4923/12/9/819
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