Amorphous solid dispersions and the contribution of nanoparticles to in vitro dissolution and in vivo testing: Niclosamide as a case study

MO Jara, ZN Warnken, RO Williams III - Pharmaceutics, 2021 - mdpi.com
We developed an amorphous solid dispersion (ASD) of the poorly water-soluble molecule
niclosamide that achieved a more than two-fold increase in bioavailability. Notably, this …

Oral delivery of niclosamide as an amorphous solid dispersion that generates amorphous nanoparticles during dissolution

MO Jara, ZN Warnken, S Sahakijpijarn, R Thakkar… - Pharmaceutics, 2022 - mdpi.com
Niclosamide is an FDA-approved anthelmintic that is being studied in clinical trials as a
chemotherapeutic and broad-spectrum antiviral. Additionally, several other applications are …

[HTML][HTML] Formulating a heat-and shear-labile drug in an amorphous solid dispersion: Balancing drug degradation and crystallinity

DA Davis Jr, DA Miller, S Santitewagun… - International Journal of …, 2021 - Elsevier
We seek to further addresss the questions posed by Moseson et al. regarding whether any
residual crystal level, size, or characteristic is acceptable in an amorphous solid dispersion …

Producing amorphous solid dispersions via co-precipitation and spray drying: impact to physicochemical and biopharmaceutical properties

AKP Mann, L Schenck, A Koynov… - Journal of …, 2018 - Elsevier
Many small-molecule active pharmaceutical ingredients (APIs) exhibit low aqueous
solubility and benefit from generation of amorphous dispersions of the API and polymer to …

[HTML][HTML] Combining drug salt formation with amorphous solid dispersions–a double edged sword

TN Hiew, LS Taylor - Journal of Controlled Release, 2022 - Elsevier
Glass transition temperature (T g) is important for amorphous compounds because it can
have implications on their physical and chemical stability. With drugs that possess ionizable …

In Vitro and In Vivo Behaviors of KinetiSol and Spray-Dried Amorphous Solid Dispersions of a Weakly Basic Drug and Ionic Polymer†

SV Jermain, MB Lowinger, DJ Ellenberger… - Molecular …, 2020 - ACS Publications
Oral delivery of poorly water-soluble, weakly basic drugs may be problematic based on the
drugs' intrinsic properties. Many drugs in this subset have overcome barriers to delivery …

The use of amorphous solid dispersions: A formulation strategy to overcome poor solubility and dissolution rate

G Van den Mooter - Drug Discovery Today: Technologies, 2012 - Elsevier
The use of amorphous solid dispersions is an interesting strategy to increase the
bioavailability of poorly soluble drugs by improving their rate and extent of dissolution. Lack …

Formulation and processing strategies which underpin susceptibility to matrix crystallization in amorphous solid dispersions

DE Moseson, TN Hiew, Y Su, LS Taylor - Journal of pharmaceutical …, 2023 - Elsevier
Through matrix crystallization, an amorphous solid may transform directly into its more stable
crystalline state, reducing the driving force for dissolution. Herein, the mechanism of matrix …

Solubility advantage of amorphous pharmaceuticals, part 3: is maximum solubility advantage experimentally attainable and sustainable?

SB Murdande, MJ Pikal, RM Shanker… - Journal of pharmaceutical …, 2011 - Elsevier
A method is described for screening compounds that inhibit crystallization in solution to
enable more accurate measurement of amorphous drug solubility. Three polymers …

Characterizing and exploring the differences in dissolution and stability between crystalline solid dispersion and amorphous solid dispersion

X Wang, L Zhang, D Ma, X Tang, Y Zhang, T Yin… - Aaps …, 2020 - Springer
Solid dispersion is one of the most effective ways to improve the dissolution of insoluble
drugs. When the carrier can highly disperse the drug, it will increase the wettability of the …