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

Abstract

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.

Gallic Acid‐Loaded Zein Nanoparticles by Electrospraying Process

“…Although EHDA processes (including e‐jet printing, electrospraying, and electrospinning) are fast developing to the multiple‐fluids ones, such as coaxial (Hai et al., ; Yu et al., ), triaxial (Liu et al., ; Yang et al., ), their microformation mechanisms are still unclear (Yang, Zhang, Liu, Wang, & Yu, ; Yu, Li, Williams, & Zhao, ). Thus, on one hand, the single‐fluid electrospraying and electrospinning are still the mainstreams of these fabrication methods.…”

Electrospun Environment Remediation Nanofibers Using Unspinnable Liquids as the Sheath Fluids: A Review

“…Based on the previous publications before this time point, they concluded that the shell working fluids must be electrospinnable for successfully carrying out a coaxial process and for creating a core-shell nanostructure [24]. However, Yu, et al broke this concept to develop a modified coaxial electrospinning, in which the sheath working fluid could be a pure solvent [12]. The modified process was successfully conducted to generate fibers from a concentrated polymer solution, which was impossible for a single-fluid process owing to the frequent clogging of the spinneret's nozzle.…”

“…These advanced techniques should greatly expand the capability of electrospinning in generating a wide variety of complex nanostructures. However, among all the complex nanostructures, the core-shell should be the most fundamental and the most important one [12]. It is not only because that many other complicated nanostructures can be viewed as a derivative of core-shell structure, but also this fundamental nanostructure has been broadly demonstrated to be extremely useful in designing and developing a wide variety of functional nanomaterials for applications in almost all the scientific fields [13,14].…”

Improved solubility, dissolution rate, and oral bioavailability of main biflavonoids from Selaginella doederleinii extract by amorphous solid dispersion

“…Similar to general pharmaceutics, the development of solid dispersions relies on having access to suitable pharmaceutical technologies and carriers to prepare the formulation (Yu et al, 2018). Previously, we demonstrated that the solvent evaporation method using anhydrous ethanol as a solvent enabled the successful development of TBESD-ASD.…”