Improved Remdesivir Solubility by Sonication

Remdesivir (GS-5734) is an anti-viral drug, which is under research for treating the Ebola virus disease and COVID-19, which is caused by the Sars-CoV-2 coronavirus. Remdesivir is pharmaceutical solution, which is administered intravenously. Whilst short ultrasonic dissolving alone enhances the solubility of remdesivir and improves its formulation, ultrasonic complexation of remdesivir within cyclodextrin complexes is a promising technique to overcome the dissolubility issues of remdesivir, which makes the drug more bioavailable.

Ultrasonic Complexation of Remdesivir into Cyclodextrin Drug Carriers

Pharmaceuticals in ampulesSulfobutyl-ether beta-cyclodextrin (SBE-β-CD) is used as an excipient or a formulating agent to increase the solubility of poorly soluble agents. Research suggests that the complexation of remdesivir into SBE-β-CD complexes will improve the solubility of remdesivir significantly improving thereby its absorption rate and bioavailability.

Formulations for “in vitro” research:

  1. H2O : 250 mg/mLrequires ultrasonication for solubilisation
  2. Dimethyl sulfoxide (DMSO) : 5.625 mg/mLrequires ultrasonication + heating for solubilisation

Formulations for “in vivo” research:

  1. Add each solvent one by one: 10% DMSO, 40% PEG300, 5% Tween 80, 45% saline + sonication
    Solubility: ≥ 2.17 mg/mL (3.60 mM); Clear solution
  2. Add each solvent one by one: 10% DMSO, 90% (20% Sulfobutyl-ether beta-cyclodextrin (SBE-β-CD) in saline) + sonication
    Solubility: ≥ 2.17 mg/mL (3.60 mM); Clear solution
  3. Add each solvent one by one: 10% DMSO, 90% corn oil + sonication
    Solubility: ≥ 2.17 mg/mL (3.60 mM); Clear solution

Ultrasonication promotes dispersing and dissolving remdesivir resulting in more effective formulations and higher bioavailability.

Advantages of Cyclodextrin Complexes

Cyclodextrins (CDs) are widely used to improve drug efficacy and potency, which means the drug can be administered in the lowest possible dose whilst achieving optimum therapeutic activity.
Drugs formulated into cyclodextrin complexes offer a significantly increased drug solubility, which lowers cytotoxicity by making the drug effective at lower doses. For instance, β-cyclodextrin complexation of ganciclovir improved the drug’s antiviral activity of on human cytomegalovirus clinical strains. Subsequently, the increased drug potency resulted in a reduced the drug toxicity. Overall, cyclodextrins show a very good absorption rate and reduce drug-induced irritancies. Cyclodextrin inclusion complexes lower the local concentration of the free drug, so that the concentration is below the irritancy threshold. Cyclodextrin inclusion improves drug stability and prevents against incompatibilities. Finally, CD complexes mask drug odour and off-flavours.

Ultrasonication is highly effective to encapsulate drugs such as remdesivir into cyclodextrin complexes.

UIP2000hdT ultrasonicator for pharmaceuticals in stainless-steel pharma batch reactor

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High Performance Ultrasonicators for Drug Encapsulation

Hielscher Ultrasonics is long-time experienced in the design, manufacturing, and distribution of high-performance ultrasonic homogenisers for the pharmaceutical, food, and cosmetic industry. Hielscher is proud to be not only hardware supplier, but offers sophisticated consulting and training for ultrasonic applications as well as the installation and operation of ultrasonic systems.
The preparation of high-quality cyclodextrin complexes and other nanostructured drug carriers auch as niosomes, liposomes, solid lipid nanoparticles, or polymeric nanoparticles are processes, in which Hielscher ultrasonic systems excel due to their high reliability, consistent power output, and precise controllability. Hielscher ultrasonicators allow for precise control over all process parameters, such as amplitude, temperature, pressure and sonication energy. The intelligent software automatically protocols all sonication parameters (time, date, amplitude, net energy, total energy, temperature, pressure) on the built-in SD-card.
The robustness of Hielscher’s ultrasonic equipment allows for 24/7 operation at heavy duty and in demanding environments.
Donja tablica daje vam naznaku približnog kapaciteta obrade naših ultrazvučnih uređaja:

Volumen serijeProtokPreporučeni uređaji
1 do 500 ml10 do 200 ml/minUP100H
10 do 2000 ml20 do 400 ml/minUP200Ht, UP400St
0.1 do 20L0.2 do 4L/minUIP2000hdT
10 do 100l2 do 10L/minUIP4000hdT
na10 do 100L/minUIP16000
navećiklaster od UIP16000

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Hielscher Ultrasonics manufactures high-performance ultrasonic homogenizers for dispersion, emulsification and cell extraction.

High-power ultrasonic homogenizers from lab to pilot i industrial scale.

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Remdesivir is drug, which has been developed by Gilead Science to treat viral infections such as Ebola virus disease and Marburg virus disease. As of state April 2020, it is in the phase of clinical trail studies in order to get possibly approved as treatment for the Ebola virus disease. In the 2020 COVID-19 pandemic, remdesivir’s antiviral effects on the SARS-CoV-2 coronavirus is investigates. As a nucleotide analogue, specifically an adenosine analogue, remdesivir inserts into the RNA chain of the virus, interfering with the virus’ replication mechanism.

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