Bilayer mucoadhesive buccal films with prolonged release of ciclopirox olamine for the treatment of oral candidiasis: In vitro development, ex vivo permeation testing, pharmacokinetic and efficacy study in rabbits

Gajdošová, Markéta; Vetchý, David; Muselík, Jan; Gajdziok, Jan; Juřica, Jan; Vetchá, Martina; Hauptman, Karel; Jekl, Vladimír

doi:10.1016/j.ijpharm.2020.120086

Cited by 28 publications

(13 citation statements)

References 43 publications

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“…Buccal films have gained relevance as novel, convenient and patient-friendly formulations [8]. These formulations have been developed to release drugs locally for the treatment of fungal or bacterial infections [9][10][11][12]. Mucoadhesive films, in turn, provide intimate contact with buccal mucosa, which implies longer retention time and can therefore release drugs in a prolonged manner [13,14].…”

Section: Introductionmentioning

confidence: 99%

Polyelectrolyte Multilayer Films as a Potential Buccal Platform for Drug Delivery

2022

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The goal of this research was to study the potential of polyelectrolyte multilayers as buccal dosage forms for drug delivery and to investigate how the properties of the drugs impact the overall performance of the delivery system. Multilayer films based on the polyelectrolyte interaction between casein and chitosan were developed using benzydamine, tolfenamic acid and betahistine as model drugs. The samples were characterized for surface pH, moisture content and moisture absorption, swelling behavior and mucoadhesion. Additionally, surface morphology was investigated, as well as the drugs’ physical state after incorporation in the multilayer films. The samples proved to be non-irritant (pH was within the physiological range), physically stable (moisture content and moisture absorption below 5%) and mucoadhesive, adsorbing from 60 to 70% mucin. The release behavior corelated to the swelling index profiles of the samples and was strongly dependent on the drug solubility. The developed multilayer films appeared to be an optimum delivery system for sparingly soluble drugs due to the high drug loading achieved.

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Section: Introductionmentioning

confidence: 99%

Polyelectrolyte Multilayer Films as a Potential Buccal Platform for Drug Delivery

2022

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“…Over the last years, numerous scientific approaches dedicated to the development of buccal films as potential platforms for either local [10][11][12] or systemic [13][14][15] drugs have been undertaken. Apart from "traditional" monolayer films, systems with more complex structure have been designed as well, nevertheless, they are predominantly composed of layers of neutral or positive polymers dedicated for incorporation of different active substances or they are "equipped" with an additional layer of water-insoluble material ensuring unidirectional drug release at the application site [11,16]. Our attention is particularly drawn by multilayer systems composed of layers of oppositely charged polyelectrolytes separated by layers of interacting polymers chains creating PECs.…”

Section: Introductionmentioning

confidence: 99%

Multilayer Films Based on Chitosan/Pectin Polyelectrolyte Complexes as Novel Platforms for Buccal Administration of Clotrimazole

et al. 2021

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Buccal films are recognized as easily applicable, microbiologically stable drug dosage forms with good retentivity at the mucosa intended for the therapy of oromucosal conditions, especially infectious diseases. Multilayer films composed of layers of oppositely charged polymers separated by ionically interacting polymeric chains creating polyelectrolyte complexes represent very interesting and relatively poorly explored area. We aimed to develop the antifungal multilayer systems composed of cationic chitosan and anionic pectin as potential platforms for controlled delivery of clotrimazole. The systems were pharmaceutically characterized with regard to inter alia their release kinetics under different pH conditions, physicomechanical, or mucoadhesion properties with using an animal model of the buccal mucosa. The antifungal activity against selected Candida sp. and potential cytotoxicity with regard to human gingival fibroblasts were also evaluated. Interactions between polyions were characterized with Fourier transform infrared spectroscopy. Different clotrimazole distribution in the films layers highly affected their in vitro dissolution profile. The designed films were recognized as intelligent pH-responsive systems with strong antifungal effect and satisfactory safety profile. As addition of chitosan resulted in the improved antifungal behavior of the drug, the potential utilization of the films in resistant cases of oral candidiasis might be worth of further exploration.

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“…Other researchers have found prolonged release of the following active substances from emulgels: ibuprofen [ 20 ], ciclopirox olamine [ 30 ], and vancomycin [ 19 ]. This release profile is appropriate for antifungal formulations when the drug is used for a long time and the presence of the drug at the site of action must be ensured [ 35 ].…”

Section: Resultsmentioning

confidence: 99%

Assessment of Physical, Mechanical, Biopharmaceutical Properties of Emulgels and Bigel Containing Ciclopirox Olamine

et al. 2022

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Emulsions are thermodynamically unstable systems and it is difficult to produce biphasic formulations with large amounts of oil. The aim of our study was to prepare biphasic formulations containing 1% ciclopirox olamine and to determine the influence of the method of oil incorporation (without and with emulsifier and gelifier) on the physical (pH, particle size, rheological properties), mechanical, and biopharmaceutical properties of the formulations. It was found that the use of a poloxamer 407 gel as the hydrophase could result in a stable formulation when an oil with (EPG) or without an emulsifier (APG) or oleogel (OPG) was used as the oily phase. The results of the studies showed that the addition of an emulsifier (polysorbate 80) led to a decrease in the sol-gel temperature, a slower release of ciclopirox olamine, and a higher stability in the freeze–thaw test. However, regardless of the way the oil is incorporated, the particles are distributed in the same range and the antifungal activity against T. rubrum is the same. It is possible to create a biphasic formulation with a large amount of oil and poloxamer gel, but for greater stability, it is recommended to include an emulsifier in the composition.

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Bilayer mucoadhesive buccal films with prolonged release of ciclopirox olamine for the treatment of oral candidiasis: In vitro development, ex vivo permeation testing, pharmacokinetic and efficacy study in rabbits

Cited by 28 publications

References 43 publications

Polyelectrolyte Multilayer Films as a Potential Buccal Platform for Drug Delivery

Polyelectrolyte Multilayer Films as a Potential Buccal Platform for Drug Delivery

Multilayer Films Based on Chitosan/Pectin Polyelectrolyte Complexes as Novel Platforms for Buccal Administration of Clotrimazole

Assessment of Physical, Mechanical, Biopharmaceutical Properties of Emulgels and Bigel Containing Ciclopirox Olamine

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