Eudragit® L100/chitosan composite thin bilayer films for intravaginal pH-responsive release of Tenofovir

Martín-Illana, Araceli; Cazorla-Luna, Raúl; Notario-Pérez, Fernando; Rubio, J.; Ruíz-Caro, Roberto; Tamayo, Aitana; Veiga, M.M.

doi:10.1016/j.ijpharm.2022.121554

Cited by 18 publications

(4 citation statements)

References 47 publications

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“…Increased adhesion would increase the effect of frictional force on the pH-responsive layer, facilitating earlier removal. Chitosan is a mucoadhesive biopolymer that has been used in pH-responsive drug delivery systems and has been shown not to affect the pH-responsiveness of underlying layers 22 , 24 , 25 .…”

Section: Discussionmentioning

confidence: 99%

Freestanding region-responsive bilayer for functional packaging of ingestible devices

et al. 2023

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Ingestible capsules have the potential to become an attractive alternative to traditional means of treating and detecting gastrointestinal (GI) disease. As device complexity increases, so too does the demand for more effective capsule packaging technologies to elegantly target specific GI locations. While pH-responsive coatings have been traditionally used for the passive targeting of specific GI regions, their application is limited due to the geometric restrictions imposed by standard coating methods. Dip, pan, and spray coating methods only enable the protection of microscale unsupported openings against the harsh GI environment. However, some emerging technologies have millimeter-scale components for performing functions such as sensing and drug delivery. To this end, we present the freestanding region-responsive bilayer (FRRB), a packaging technology for ingestible capsules that can be readily applied for various functional ingestible capsule components. The bilayer is composed of rigid polyethylene glycol (PEG) under a flexible pH-responsive Eudragit® FL 30 D 55, which protects the contents of the capsule until it arrives in the targeted intestinal environment. The FRRB can be fabricated in a multitude of shapes that facilitate various functional packaging mechanisms, some of which are demonstrated here. In this paper, we characterize and validate the use of this technology in a simulated intestinal environment, confirming that the FRRB can be tuned for small intestinal release. We also show a case example where the FRRB is used to protect and expose a thermomechanical actuator for targeted drug delivery.

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Section: Discussionmentioning

confidence: 99%

Freestanding region-responsive bilayer for functional packaging of ingestible devices

et al. 2023

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“…This is required for enhancing the outcomes of several medical procedures; e.g., buccal local anesthesia [11,12] Likewise, hydrophobic plasticizers can be used in the formulation of monolithic films intended to provide a sustained drug release profile for a long time span, such as in vaginal and ocular administration. Acetate esters such as glyceryl triacetate (triacetin), triethyl citrate, and acetyl triethyl citrate; phthalate esters (e.g., diethyl phthalate and dibutylphthalate); and acetylated monoglycerides are widely used for these purposes [29][30][31][32].…”

Section: Plasticizersmentioning

confidence: 99%

The Potential of Films as Transmucosal Drug Delivery Systems

de Carvalho,

Paiva,

Demonari

et al. 2023

Pharmaceutics

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Pharmaceutical films are polymeric formulations used as a delivery platform for administration of small and macromolecular drugs for local or systemic action. They can be produced by using synthetic, semi-synthetic, or natural polymers through solvent casting, electrospinning, hot-melt extrusion, and 3D printing methods, and depending on the components and the manufacturing methods used, the films allow the modulation of drug release. Moreover, they have advantages that have drawn interest in the development and evaluation of film application on the buccal, nasal, vaginal, and ocular mucosa. This review aims to provide an overview of and critically discuss the use of films as transmucosal drug delivery systems. For this, aspects such as the composition of these formulations, the theories of mucoadhesion, and the methods of production were deeply considered, and an analysis of the main transmucosal pathways for which there are examples of developed films was conducted. All of this allowed us to point out the most relevant characteristics and opportunities that deserve to be taken into account in the use of films as transmucosal drug delivery systems.

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“…CS, in combination with xanthan gum, karaya gum or pectin, was employed to develop multi-layered vaginal films for release of the antiviral tenofovir, exploiting the CS ability to interact with anionic polymers to form polyelectrolyte complexes (PECs) able to assure a controlled drug release [ 245 ]. Eudragit ® L100/CS composite bilayer vaginal films were also developed for a pH-responsive release of tenofovir, by combining the CS mucoadhesive properties with the Eudragit ® L100 ability to improve the film’s mechanical properties and to control the drug release into the vaginal medium [ 246 ].…”

Section: Chitosan-based Mucosal Drug Delivery Systemsmentioning

confidence: 99%

Multiple Roles of Chitosan in Mucosal Drug Delivery: An Updated Review

et al. 2022

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Chitosan (CS) is a linear polysaccharide obtained by the deacetylation of chitin, which, after cellulose, is the second biopolymer most abundant in nature, being the primary component of the exoskeleton of crustaceans and insects. Since joining the pharmaceutical field, in the early 1990s, CS attracted great interest, which has constantly increased over the years, due to its several beneficial and favorable features, including large availability, biocompatibility, biodegradability, non-toxicity, simplicity of chemical modifications, mucoadhesion and permeation enhancer power, joined to its capability of forming films, hydrogels and micro- and nanoparticles. Moreover, its cationic character, which renders it unique among biodegradable polymers, is responsible for the ability of CS to strongly interact with different types of molecules and for its intrinsic antimicrobial, anti-inflammatory and hemostatic activities. However, its pH-dependent solubility and susceptibility to ions presence may represent serious drawbacks and require suitable strategies to be overcome. Presently, CS and its derivatives are widely investigated for a great variety of pharmaceutical applications, particularly in drug delivery. Among the alternative routes to overcome the problems related to the classic oral drug administration, the mucosal route is becoming the favorite non-invasive delivery pathway. This review aims to provide an updated overview of the applications of CS and its derivatives in novel formulations intended for different methods of mucosal drug delivery.

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Eudragit® L100/chitosan composite thin bilayer films for intravaginal pH-responsive release of Tenofovir

Cited by 18 publications

References 47 publications

Freestanding region-responsive bilayer for functional packaging of ingestible devices

Freestanding region-responsive bilayer for functional packaging of ingestible devices

The Potential of Films as Transmucosal Drug Delivery Systems

Multiple Roles of Chitosan in Mucosal Drug Delivery: An Updated Review

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