Amorphous solid dispersion technique for improved drug delivery: basics to clinical applications

Mishra, Dinesh Kumar; Dhote, Vinod; Bhargava, Arpit; Jain, Dinesh Kumar; Mishra, Pradyumna Kumar

doi:10.1007/s13346-015-0256-9

Cited by 51 publications

(20 citation statements)

References 82 publications

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“…In the broad sense of being systems with "drug dispersed in a solid matrix" [283], all drug-loaded electrospun nanofibers can be considered SDs. Nearly all electrospun fibers are also amorphous SDs, in which the drug molecules are dispersed into the polymer matrix with little phase separation.…”

Section: Drug Dissolution Profiles From Different Types Of Electrospumentioning

confidence: 99%

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

Williams

et al. 2018

Journal of Controlled Release

252

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: Drug Dissolution Profiles From Different Types Of Electrospumentioning

confidence: 99%

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

Williams

et al. 2018

Journal of Controlled Release

252

156

View full text Add to dashboard Cite

show abstract

“…There are four production methods for solid dispersions: solvent-removing, melting, precipitation and electro-spinning [34,35,37,41,44,[51][52][53]. In the solvent-removal method, drug and excipient are dissolved in an organic solvent and the solution is then evaporated or sublimated.…”

Section: Production Methodsmentioning

confidence: 99%

Inventory of oral anticancer agents: Pharmaceutical formulation aspects with focus on the solid dispersion technique

Sawicki

Schellens

Beijnen

et al. 2016

Cancer Treatment Reviews

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Dissolution from the pharmaceutical formulation is a prerequisite for complete and consistent absorption of any orally administered drug, including anticancer agents (oncolytics). Poor dissolution of an oncolytic can result in low oral bioavailability, high variability in blood concentrations and with that suboptimal or even failing therapy. This review discusses pharmaceutical formulation aspects and absorption pharmacokinetics of currently licensed orally administered oncolytics. In nearly half of orally dosed oncolytics poor dissolution is likely to play a major role in low and unpredictable absorption. Dissolution-limited drug absorption can be improved with a solid dispersion which is a formulation method that induces super-saturated drug dissolution and with that it enhances in vivo absorption. This review discusses formulation principles with focus on the solid dispersion technology and how it works to enhance drug absorption. There are currently three licensed orally dosed oncolytics formulated as a solid dispersion (everolimus, vemurafenib and regorafenib) and these formulations result in remarkably improved dissolution and absorption compared to what can be achieved with conventional formulations of the respective oncolytics. Because of the successful implementation of these three solid dispersion formulations, we encourage the application of this formulation method for poorly soluble oral oncolytics.

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“…The term solid dispersion describes a wide range of different, but related formulations which are designed to maintain drug in an amorphous or phase‐separated crystalline state . By reducing the drug particle size to the molecular level rapid dissolution can be facilitated, and production of an amorphous form will improve the apparent solubility, while solid dispersion can also confer improved wettability, increased porosity and, ultimately, improved biopharmaceutical performance . Solid dispersions are being used increasingly often as bio‐enabling formulations for PWSD to enhance oral bioavailability and numerous commercial preparations exist .…”

Section: Strategies To Overcome Food Effect Bioavailability In Drug Dmentioning

confidence: 99%

Food for thought: formulating away the food effect – a PEARRL review

O’Shea

Holm

O’Driscoll

et al. 2019

Journal of Pharmacy and Pharmacology

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There are clinical and commercial advantages to predicting the presence of food effects early in the drug development process, in order to mitigate this risk of variable food effect bioavailability. Formulation approaches aimed at reducing variable food-dependent bioavailability, through the use of bio-enabling formulations, are an essential tool in addressing this challenge and the latest state of the art in this field are summarised here.

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Amorphous solid dispersion technique for improved drug delivery: basics to clinical applications

Cited by 51 publications

References 82 publications

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

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

Inventory of oral anticancer agents: Pharmaceutical formulation aspects with focus on the solid dispersion technique

Food for thought: formulating away the food effect – a PEARRL review

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