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 (Author), Laura di Muzio (Author), Jordan Trilli (Author), Chiara Brandelli (Author), Patrizia Paolicelli (Author), Stefania Petralito (Author), Maria Antonietta Casadei (Author)
Format: Book
Published: MDPI AG, 2020-08-01T00:00:00Z.
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Summary: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.
Item Description:10.3390/pharmaceutics12090819
1999-4923