Detailed stability investigation of amorphous solid dispersions prepared by single-needle and high speed electrospinning

Démuth, Balázs; Farkas, Attila; Pataki, Hajnalka; Balogh, Attila; Szabó, Bence; Borbás, Enikő; Sóti, Péter Lajos; Vígh, Tamás; Kiserdei, Éva; Farkas, Balázs; Mensch, J.; Verreck, Geert; Assche, Ivo Van; Marosi, Gy.; Nagy, Zsombor Kristóf

doi:10.1016/j.ijpharm.2015.12.029

Cited by 57 publications

(47 citation statements)

References 49 publications

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“…Démuth et al have compared the ASDs prepared using single-fluid electrospinning and the film casting technology with itraconazole (ITR) as a model API and Kollidon® VA64 as the polymeric matrix. Both X-ray diffraction (XRD) and differential scanning calorimetry (DSC) results demonstrated that the electrospun SDs are totally amorphous while the cast products have some crystalline drug content owing to the slow drying process [65].…”

Section: Accepted Manuscriptmentioning

confidence: 99%

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

Williams

et al. 2018

Journal of Controlled Release

250

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

250

156

View full text Add to dashboard Cite

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“…Utilization of Raman spectroscopy also seems to be feasible for real-time monitoring of freeze-drying [40] and even real-time feedback control of continuous powder blending [41]. Furthermore, a PAT system can be particularly important and useful when tablets include ASDs since these metastable systems tend to crystallize during processing [42][43][44]. Raman and NIR spectroscopies can allow the detection of crystalline traces in the ASDs [45,46], thus these analytical methods can be of enormous significance for in-line process monitoring [47].…”

mentioning

confidence: 99%

Scaled-up preparation of drug-loaded electrospun polymer fibres and investigation of their continuous processing to tablet form

Szabó

Démuth

Nagy

et al. 2018

Express Polym. Lett.

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“…If the ratio of peaks at 666 and 639 cm À1 of ITR is over 1.05, it means that the examined sample is crystalline. 32 It is clearly visible in the figure that 666 cm À1 peak has larger intensity than the peak at 639 cm…”

Section: The Crystallization Phenomenonmentioning

confidence: 86%

Lubricant-Induced Crystallization of Itraconazole From Tablets Made of Electrospun Amorphous Solid Dispersion

Démuth

Farkas

Balogh

et al. 2016

Journal of Pharmaceutical Sciences

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Keywords:oral drug delivery amorphous solid dispersion dissolution crystallization nanotechnology tableting chemical stability Raman spectroscopy a b s t r a c t Investigation of downstream processing of nanofibrous amorphous solid dispersions to generate tablet formulation is in a quite early phase. Development of high speed electrospinning opened up the possibility to study tableting of electrospun solid dispersions (containing polyvinylpyrrolidone-vinyl acetate and itraconazole [ITR] in this case). This work was conducted to investigate the influence of excipients on dissolution properties and the feasibility of scaled-up rotary press tableting. The dissolution rates from tablets proved to be mainly composition dependent. Magnesium stearate acted as a nucleation promoting agent (providing an active hydrophobic environment for crystallization of ITR) hindering the total dissolution of ITR. This crystallization process proved to be temperature dependent as well. However, the extent of dissolution of more than 95% was realizable when a less hydrophobic lubricant, sodium stearyl fumarate (soluble in the medium), was applied. Magnesium stearate induced crystallization even if it was put in the dissolution medium next to proper tablets. After optimization of the composition, scaled-up tableting on a rotary press was carried out. Appropriate dissolution of ITR from tablets was maintained for 3 months at 25 C/60% relative humidity. HPLC measurements confirmed that ITR was chemically stable both in the course of downstream processing and storage.

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Detailed stability investigation of amorphous solid dispersions prepared by single-needle and high speed electrospinning

Cited by 57 publications

References 49 publications

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

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

Scaled-up preparation of drug-loaded electrospun polymer fibres and investigation of their continuous processing to tablet form

Lubricant-Induced Crystallization of Itraconazole From Tablets Made of Electrospun Amorphous Solid Dispersion

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