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

Abstract

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-β-cyclodextrin (HP-β-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-β-CD, fluconazole and complex fluconazole/HP-β-CD in the swelling film. Experimental results, supported by theoretical modeling, confirmed that gellan gum-low glycerol thin films including HP-β-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-β-CD.

Mucoadhesive Gelatin Buccal Films with Propranolol Hydrochloride: Evaluation of Mechanical, Mucoadhesive, and Biopharmaceutical Properties

“…Buccal mucosa is relatively permeable and has good vascularization [ 3 , 4 ]. This route offers many advantages compared to the oral route, such as avoiding gastrointestinal irritation and drug degradation and first-pass liver metabolism, which means it ensures better drug bioavailability [ 2 , 5 , 6 ]. Moreover, buccal mucosa is accessible, so that a dosage form can be easily administered, leading to better patient compliance compared to other drug dosing routes [ 5 , 6 ].…”

“…This route offers many advantages compared to the oral route, such as avoiding gastrointestinal irritation and drug degradation and first-pass liver metabolism, which means it ensures better drug bioavailability [ 2 , 5 , 6 ]. Moreover, buccal mucosa is accessible, so that a dosage form can be easily administered, leading to better patient compliance compared to other drug dosing routes [ 5 , 6 ]. Buccal administration is particularly suitable for the pediatric and geriatric population, as well as patients that have problems with swallowing [ 6 ].…”

“…Moreover, buccal mucosa is accessible, so that a dosage form can be easily administered, leading to better patient compliance compared to other drug dosing routes [ 5 , 6 ]. Buccal administration is particularly suitable for the pediatric and geriatric population, as well as patients that have problems with swallowing [ 6 ]. There are many different dosage forms for buccal administration, such as tablets, films, gels, patches, sprays, pastes [ 7 ].…”

3D Printed Buccal Films for Prolonged-Release of Propranolol Hydrochloride: Development, Characterization and Bioavailability Prediction

“…The oral mucosa has very good vascularization, and the API absorbed there directly enters systemic circulation [13,14]. This application route is convenient and accessible, and the buccal dosage form can be easily removed if needed [15]. In addition, patient compliance is improved, especially for the geriatric and pediatric population, as well as for patients with gastroesophageal disorders or patients having trouble swallowing [15].…”

Antimicrobial Polymer-Based Hydrogels for the Intravaginal Therapies—Engineering Considerations

“…Gellan gum, a natural polysaccharide, is also considered a mucoadhesive polymer due to the formation of hydrogen bonds between the carboxyl groups of glucuronic acid, the hydroxyl groups of the gellan gum, and the appropriate H-group donor/acceptor groups of the mucin [ 63 , 67 ]. Another natural polymer, i.e., gelatin, a protein derived from animal sources such as bovine, porcine, and fish, by collagen hydrolysis, displays mucoadhesion thanks to the presence of hydrophilic groups such as carboxyl, hydroxyl, and amine, which can participate in hydrogen bonding [ 68 ].…”