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d-Xylose oxetane copolymers as bioderived and tuneable polyesters for amorphous solid dispersions (2024)
Journal Article
F. Clark, E., Howard, A., D. Morales Feliu, S., F. McCabe, J., C. Burley, J., Taresco, V., & Buchard, A. (2024). d-Xylose oxetane copolymers as bioderived and tuneable polyesters for amorphous solid dispersions. RSC Applied Polymers, 2(6), 1104-1112. https://doi.org/10.1039/D4LP00203B

The ring-opening copolymerisation of cyclic anhydrides with an oxetane derived from natural monosaccharide D-xylose has been used to synthesise fully biobased water soluble polyesters, which are able to stabilise the amorphous phases of nifedipine an... Read More about d-Xylose oxetane copolymers as bioderived and tuneable polyesters for amorphous solid dispersions.

Evaluating the effects of processing parameters on budesonide nanocrystals prepared by nanomilling (2022)
Journal Article
Olubi, R., Small, W., Burley, J., & Bosquillon, C. (2022). Evaluating the effects of processing parameters on budesonide nanocrystals prepared by nanomilling. British Journal of Pharmacy, 7(2), S1-S2. https://doi.org/10.5920/bjpharm.1140

The aim of this study was to optimise processing parameters in the preparation ofbudesonide nanocrystals by a miniature media milling process performed at labscale. Using Polysorbate 80 as the surfactant choice of stabilizer, the effectof milling bea... Read More about Evaluating the effects of processing parameters on budesonide nanocrystals prepared by nanomilling.

Effect of Excipients on Salt Disproportionation during Dissolution: A Novel Application of In Situ Raman Imaging (2021)
Journal Article
Abouselo, A., Rance, G. A., Tres, F., Taylor, L. S., Kwokal, A., Renou, L., …Aylott, J. W. (2021). Effect of Excipients on Salt Disproportionation during Dissolution: A Novel Application of In Situ Raman Imaging. Molecular Pharmaceutics, 18(9), 3247-3259. https://doi.org/10.1021/acs.molpharmaceut.1c00119

We have employed a bespoke setup combining confocal Raman microscopy and an ultraviolet–visible (UV–Vis) spectroscopy flow cell to investigate the effect of excipients on the disproportionation kinetics of Pioglitazone HCl (PioHCl) in tablets during... Read More about Effect of Excipients on Salt Disproportionation during Dissolution: A Novel Application of In Situ Raman Imaging.

Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine (2018)
Journal Article
Ali, J., Zgair, A., Hameed, G. S., Garnett, M. C., Roberts, C. J., Burley, J. C., & Gershkovich, P. (2019). Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine. International Journal of Pharmaceutics, 555, 228-236. https://doi.org/10.1016/j.ijpharm.2018.11.051

The oral cavity is of great importance to the performance of orally retained formulations, including: orally disintegrating tablets, taste-masked formulations, and buccal/sublingual delivery systems. With regards to in vitro dissolution assessment of... Read More about Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine.

In Silico Screening for Solid Dispersions: The Trouble with Solubility Parameters and χFH (2018)
Journal Article
Turpin, E. R., Taresco, V., Al-Hachami, W. A., Booth, J., Treacher, K., Tomasi, S., …Garnett, M. C. (2018). In Silico Screening for Solid Dispersions: The Trouble with Solubility Parameters and χFH. Molecular Pharmaceutics, 15(10), 4654-4667. https://doi.org/10.1021/acs.molpharmaceut.8b00637

© Copyright 2018 American Chemical Society. The problem of predicting small molecule-polymer compatibility is relevant to many areas of chemistry and pharmaceutical science but particularly drug delivery. Computational methods based on Hildebrand and... Read More about In Silico Screening for Solid Dispersions: The Trouble with Solubility Parameters and χFH.

High-Throughput Miniaturized Screening of Nanoparticle Formation via Inkjet Printing (2018)
Journal Article
Styliari, I. D., Conte, C., Pearce, A. K., Hüsler, A., Cavanagh, R. J., Limo, M. J., Gordhan, D., Nieto-Orellana, A., Suksiriworapong, J., Couturaud, B., Williams, P., Hook, A. L., Alexander, M. R., Garnett, M. C., Alexander, C., Burley, J. C., & Taresco, V. (2018). High-Throughput Miniaturized Screening of Nanoparticle Formation via Inkjet Printing. Macromolecular Materials and Engineering, 303(8), 1-9. https://doi.org/10.1002/mame.201800146

The self‐assembly of specific polymers into well‐defined nanoparticles (NPs) is of great interest to the pharmaceutical industry as the resultant materials can act as drug delivery vehicles. In this work, a high‐throughput method to screen the abilit... Read More about High-Throughput Miniaturized Screening of Nanoparticle Formation via Inkjet Printing.

Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays (2018)
Journal Article
Sanna, M., Sicilia, G., Alazzo, A., Singh, N., Musumeci, F., Schenone, S., …Alexander, C. (in press). Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays. ACS Medicinal Chemistry Letters, 9(3), https://doi.org/10.1021/acsmedchemlett.7b00456

A miniaturized assay was optimized to evaluate the enhanced apparent water solubility of pyrazolo[3,4-d]pyrimidine derivatives used extensively as anticancer drug scaffolds. The applied amount of drugs used in the reported strategy ranged from 5-10 μ... Read More about Water solubility enhancement of pyrazolo[3,4-d]pyrimidine derivatives via miniaturized polymer-drug microarrays.

Rapid nano-gram scale screening method of micro-arrays to evaluate drug-polymer blends using high-throughput printing technology (2017)
Journal Article
Taresco, V., Louzao, I., Scurr, D. J., Turpin, E. R., Laughton, C. A., Alexander, C., …Garnett, M. (in press). Rapid nano-gram scale screening method of micro-arrays to evaluate drug-polymer blends using high-throughput printing technology. Molecular Pharmaceutics, 14(6), https://doi.org/10.1021/acs.molpharmaceut.7b00182

A miniaturized, high-throughput assay was optimized to screen polymer-drug solid dispersions using a 2-D Ink-jet printer. By simply printing nanoliter amounts of polymer and drug solutions onto an inert surface, drug:polymer micro-dots of tunable com... Read More about Rapid nano-gram scale screening method of micro-arrays to evaluate drug-polymer blends using high-throughput printing technology.

New N-acyl amino acid-functionalized biodegradable polyesters for pharmaceutical and biomedical applications (2016)
Journal Article
Taresco, V., Suksiriworapong, J., Styliari, I. D., Argent, R. H., Swainson, S. M., Booth, J., …Garnett, M. C. (in press). New N-acyl amino acid-functionalized biodegradable polyesters for pharmaceutical and biomedical applications. RSC Advances, 6(111), 109401-109405. https://doi.org/10.1039/C6RA21464A

A novel class of biodegradable polyesters has been generated by coupling poly(glycerol adipate) with N-acyl aromatic amino acids. This new set of polymers from this highly versatile polymeric platform may offer unprecedented new opportunities to prod... Read More about New N-acyl amino acid-functionalized biodegradable polyesters for pharmaceutical and biomedical applications.

Properties of acyl modified poly(glycerol-adipate) comb-like polymers and their self-assembly into nanoparticles (2016)
Journal Article
Taresco, V., Suksiriworapong, J., Creasey, R., Burley, J. C., Mantovani, G., Alexander, C., & Garnett, M. (2016). Properties of acyl modified poly(glycerol-adipate) comb-like polymers and their self-assembly into nanoparticles. Journal of Polymer Science Part A: Polymer Chemistry, 54(20), 3267-3278. https://doi.org/10.1002/pola.28215

There is an increasing need to develop bio-compatible polymers with an increased range of different physicochemical properties. Poly(glycerol-adipate) (PGA) is a biocompatible, biodegradable amphiphilic polyester routinely produced from divinyl adipa... Read More about Properties of acyl modified poly(glycerol-adipate) comb-like polymers and their self-assembly into nanoparticles.

Indomethacin-Kollidon VA64 Extrudates: A Mechanistic Study of pH-Dependent Controlled Release (2016)
Journal Article
Wren, S. A. C., Aylott, J. W., Tres, F., Treacher, K., Booth, J., Hughes, L. P., …Burley, J. C. (2016). Indomethacin-Kollidon VA64 Extrudates: A Mechanistic Study of pH-Dependent Controlled Release. Molecular Pharmaceutics, 13(3), 1166-1175. https://doi.org/10.1021/acs.molpharmaceut.5b00979

© 2016 American Chemical Society. Because of its weakly acidic nature (pKa of 4.5), indomethacin presents an aqueous solubility that significantly increases when changing from acidic to neutral/alkaline pH (1.5 μg/mL at pH 1.2 and 105.2 μg/mL at pH 7... Read More about Indomethacin-Kollidon VA64 Extrudates: A Mechanistic Study of pH-Dependent Controlled Release.

Variation in structure and properties of poly(glycerol adipate) via control of chain branching during enzymatic synthesis (2016)
Journal Article
Taresco, V., Creasey, R., Kennon, J., Mantovani, G., Alexander, C., Burley, J. C., & Garnett, M. C. (2016). Variation in structure and properties of poly(glycerol adipate) via control of chain branching during enzymatic synthesis. Polymer, 89, https://doi.org/10.1016/j.polymer.2016.02.036

Poly (glycerol adipate) (PGA) can be produced from divinyl adipate and unprotected glycerol by an enzymatic route to generate a polymer with relatively low molar mass (12 kDa). PGA bears a pendant hydroxyl group which imparts a hydrophilic character... Read More about Variation in structure and properties of poly(glycerol adipate) via control of chain branching during enzymatic synthesis.

3D printing of five-in-one dose combination polypill with defined immediate and sustained release profiles (2015)
Journal Article
Khaled, S. A., Burley, J. C., Alexander, M. R., Yang, J., & Roberts, C. J. (in press). 3D printing of five-in-one dose combination polypill with defined immediate and sustained release profiles. Journal of Controlled Release, 217, https://doi.org/10.1016/j.jconrel.2015.09.028

We have used three dimensional (3D) extrusion printing to manufacture a multi-active solid dosage form or so called polypill. This contains five compartmentalised drugs with two independently controlled and well-defined release profiles. This polypil... Read More about 3D printing of five-in-one dose combination polypill with defined immediate and sustained release profiles.

Insights into the influence of the cooling profile on the reconstitution times of amorphous lyophilized protein formulations (2015)
Journal Article
Beech, K. E., Biddlecombe, J. G., van der Walle, C. F., Stevens, L. A., Rigby, S. P., Burley, J. C., Allen, S., Burley, J. C., & Allena, S. (2015). Insights into the influence of the cooling profile on the reconstitution times of amorphous lyophilized protein formulations. European Journal of Pharmaceutics and Biopharmaceutics, 96, 247-254. https://doi.org/10.1016/j.ejpb.2015.07.029

Lyophilized protein formulations must be reconstituted back into solution prior to patient administration and in this regard long reconstitution times are not ideal. The factors that govern reconstitution time remain poorly understood. The aim of thi... Read More about Insights into the influence of the cooling profile on the reconstitution times of amorphous lyophilized protein formulations.

Monitoring the Dissolution Mechanisms of Amorphous Bicalutamide Solid Dispersions via Real-Time Raman Mapping (2015)
Journal Article

Real-time in situ Raman mapping has been employed to monitor, during dissolution, the crystallization transitions of amorphous bicalutamide formulated as a molecular dispersion in a copovidone VA64 matrix. The dissolution performance was also investi... Read More about Monitoring the Dissolution Mechanisms of Amorphous Bicalutamide Solid Dispersions via Real-Time Raman Mapping.

Real time Raman imaging to understand dissolution performance of amorphous solid dispersions (2014)
Journal Article
Tres, F., Treacher, K., Booth, J., Hughes, L. P., Wren, S. A., Aylott, J. W., & Burley, J. C. (2014). Real time Raman imaging to understand dissolution performance of amorphous solid dispersions. Journal of Controlled Release, 188, https://doi.org/10.1016/j.jconrel.2014.05.061

We have employed for the first time Raman spectroscopic imaging along with multi-variate curve resolution (MCR) analysis to investigate in real time and in-situ the dissolution mechanisms that underpin amorphous solid dispersions, with data being col... Read More about Real time Raman imaging to understand dissolution performance of amorphous solid dispersions.