In vitro dissolution–permeation evaluation of an electrospun cyclodextrin-based formulation of aripiprazole using μFlux™

Borbás, Enikő; Balogh, Attila; Bocz, Katalin; Müller, Judit; Kiserdei, Éva; Vígh, Tamás; Sinkó, Bálint; Marosi, Attila Csaba; Halász, A; Dohányos, Zoltán; Szente, Lajos; Balogh, György Tibor

doi:10.1016/j.ijpharm.2015.06.019

Cited by 59 publications

(32 citation statements)

References 53 publications

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“…Thus, ex vivo permeation tests are vital to fully characterize their performance. Class II APIs tend to have some lipophilic properties, and their onset of action of can be enhanced with very rapid release because of the large concentration gradient which results [276]. The incorporation of a lipidic carrier into fibers can also be used to accelerate permeation [277].…”

Section: Accepted Manuscriptmentioning

confidence: 99%

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Williams

et al. 2018

Journal of Controlled Release

232

156

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The development of oral dosage forms for poorly water-soluble active pharmaceutical ingredients (APIs) is a persistent challenge. A range of methods has been explored to address this issue, and amorphous solid dispersions (ASDs) have received increasing attention. ASDs are typically prepared by starting with a liquid precursor (a solution or melt) and applying energy for solidification. Many techniques can be used, with the emergence of electrospinning as a potent option in recent years. This method uses electrical energy to induce changes from liquid to solid. Through the direct applications of electrical energy, electrospinning can generate nanofiber-based ASDs from drug-loaded solutions, melts and melt-solutions. The technique can also be combined with other approaches using the application of mechanical, thermal or other energy sources. Electrospinning has numerous advantages over other approaches to produce ASDs. These advantages include extremely rapid drying speeds, ease of implentation, compatibility with a wide range of active ingredients (including those which are thermally labile), and the generation of products with large surface areas and high porosity. Furthermore, this technique exhibits the potential to create so-called 'fifth-generation' ASDs with nanostructured architectures, such as core/shell or Janus systems and their combinations. These advanced systems can improve dissolution behaviour and provide programmable drug release profiles. Additionally, the fiber components and their spatial distributions can be precisely controlled. Electrospun fiber-based ASDs can maintain an incorporated active ingredient in the amorphous physical form for prolonged periods of time because of their homogeneous drug distribution within the polymer matrix (typically they comprise solid solutions), and ability to inhibit molecular motion. These ASDs can be utilised to generate oral dosage forms for poorly water-soluble drugs, resulting in linear or multiple-phase release of one or more APIs. Electrospun ASDs can also be exploited as templates for manipulating molecular self-assembly, offering a bridge between ASDs and other types of dosage forms. This review addresses the development, advantages and pharmaceutical applications of electrospinning for producing polymeric ASDs. Material preparation and analysis procedures are considered. The mechanisms through which performance has been improved are also discussed.

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Section: Accepted Manuscriptmentioning

confidence: 99%

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Williams

et al. 2018

Journal of Controlled Release

232

156

View full text Add to dashboard Cite

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“…Another strategy for reducing the droplet formation was to add high molecular weight polyethylene oxide (PEO) in low concentration to the PVA solution. PEO is a really good fiber forming polymer, thus it can help the fiber formation of various blends [36,37]. PEO can interact with the PVA molecules by competing with water molecules and combined with the larger molecule size results in an increase of the entanglement.…”

Section: Role Of Peomentioning

confidence: 99%

Electrospinning scale-up and formulation development of PVA nanofibers aiming oral delivery of biopharmaceuticals

Hirsch¹,

Vass²,

Démuth³

et al. 2019

Express Polym. Lett.

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The application of biopharmaceuticals for oral administration is a topic of great interest in the pharmaceutical industry due to the inherent advantages of oral delivery [1]. Biopharmaceutical formulations are more stable in the solid state than in liquid form; in addition, it has many advantages like storage at ambient temperature, longer shelf-life, easier product shipping and the possibility of controlled drug delivery [2]. Currently, the pharmaceutical industry is typically applying freeze drying and spray drying processes in order to obtain solid biopharmaceuticals, however, both technologies have disadvantages [3,4]. Freeze drying is a time-consuming batch technology, has high energy consumption, and the freezing can cause degradation of the biomolecules. On the contrary, spray drying can be operated continuously, is more economical, but can induce inactivation of heat-sensitive molecules, due to the high drying temperature. Electrospinning (ES), which is originally a fiber drawing technology, can be a promising alternative for continuous drying technologies, providing Abstract. Electrospinning is a promising drying technology providing a rapid and gentle drying at ambient temperature, thus electrospinning of polyvinyl alcohol aqueous solutions was investigated for the solid formulation of biopharmaceuticals. The commonly used single-needle electrospinning does not have adequate productivity to satisfy the industrial requirements, therefore our aim was to study the scale-up of the technology by using high-speed electrospinning. High molecular weight polyethylene oxide as a secondary polymer was applied to enhance the fiber formation of polyvinyl alcohol. While polyvinyl alcohol-polyethylene oxide formulations resulted in adequate fiber formation it was not possible to process them further as the friability of the fibers was too low. In order to increase the friability, the effect of adding various sugars (mannitol, glucose, lactose, saccharose, and trehalose) was investigated. The results showed that mannitol was the best friability enhancing excipient because of its crystallinity and low moisture content in the fibrous sample. In contrast, glucose, lactose, saccharose, and trehalose were amorphous with higher moisture content and fibers containing these were grindable only after post-drying.

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“…It has been reported a study that test an electrophilic formulation based on cyclodextrin of aripiprazole, with an apparatus (μFlux) which monitors the permeation along with the dissolution, and by this means a better in vitro-in vivo correlation. It has been demonstrated that an electrospinning formulation based on cyclodextrin-aripiprazole has the potential to ensure rapid delivery of drug through the oral mucosa due to the rapid dissolution of the drug in the formulation and the improved flow through the membranes, as shows by the result of the new in vitro dissolution and permeation test (79).…”

Section: Miscellaneousmentioning

confidence: 99%

Drugs Loaded into Electrospun Polymeric Nanofibers for Delivery

et al. 2019

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The electrospinning technique is a useful and versatile approach for conversion of polymeric solutions into continuous fibers, ranging from a few micrometers (10-100 μm) to the scale of nanometers (10-100 nm) in diameters. This technique can be used in a vast number of polymers, in some cases after modifying them to the required properties. The high surface-to-volume ratio of the fibers can improve some processes like cell binding and proliferation, drug loading, and mass transfer processes. One of the most important and studied areas of electrospinning is in the drug delivery field, for the controlled release of active substances ranging from antibiotics and anticancer agents, to macromolecules such as proteins and DNA. The advantage of this method is that a wide variety of low solubility drugs can be loaded into the fibers to improve their bioavailability or to attain controlled release. This review presents an overview of the reported drugs loaded into electrospun polymeric nanofibers to be used as drug delivery systems. These drugs are classified by their applications in pharmacy.

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In vitro dissolution–permeation evaluation of an electrospun cyclodextrin-based formulation of aripiprazole using μFlux™

Cited by 59 publications

References 53 publications

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Electrospinning scale-up and formulation development of PVA nanofibers aiming oral delivery of biopharmaceuticals

Drugs Loaded into Electrospun Polymeric Nanofibers for Delivery

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