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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.

Design, Synthesis, and Evaluation of Lung-Retentive Prodrugs for Extending the Lung Tissue Retention of Inhaled Drugs (2022)
Journal Article
Ayre, J., Redmond, J. M., Vitulli, G., Tomlinson, L., Weaver, R., Comeo, E., …Stocks, M. J. (2022). Design, Synthesis, and Evaluation of Lung-Retentive Prodrugs for Extending the Lung Tissue Retention of Inhaled Drugs. Journal of Medicinal Chemistry, 65(14), 9802-9818. https://doi.org/10.1021/acs.jmedchem.2c00416

A major limitation of pulmonary delivery is that drugs can exhibit suboptimal pharmacokinetic profiles resulting from rapid elimination from the pulmonary tissue. This can lead to systemic side effects and a short duration of action. A series of diba... Read More about Design, Synthesis, and Evaluation of Lung-Retentive Prodrugs for Extending the Lung Tissue Retention of Inhaled Drugs.

PEGylation of recombinant human deoxyribonuclease I decreases its transport across lung epithelial cells and uptake by macrophages (2020)
Journal Article
Mahri, S., Hardy, E., Wilms, T., De Keersmaecker, H., Braeckmans, K., De Smedt, S., …Vanbever, R. (2021). PEGylation of recombinant human deoxyribonuclease I decreases its transport across lung epithelial cells and uptake by macrophages. International Journal of Pharmaceutics, 593, Article 120107. https://doi.org/10.1016/j.ijpharm.2020.120107

Conjugation to high molecular weight (MW ≥ 20 kDa) polyethylene glycol (PEG) was previously shown to largely prolong the lung residence time of recombinant human deoxyribonuclease I (rhDNase) and improve its therapeutic efficacy following pulmonary d... Read More about PEGylation of recombinant human deoxyribonuclease I decreases its transport across lung epithelial cells and uptake by macrophages.

Biodistribution and elimination pathways of PEGylated recombinant human deoxyribonuclease I after pulmonary delivery in mice (2020)
Journal Article
Mahri, S., Rondon, A., Wilms, T., Bosquillon, C., & Vanbever, R. (2021). Biodistribution and elimination pathways of PEGylated recombinant human deoxyribonuclease I after pulmonary delivery in mice. Journal of Controlled Release, 329, 1054-1065. https://doi.org/10.1016/j.jconrel.2020.10.034

Conjugation of recombinant human deoxyribonuclease I (rhDNase) to polyethylene glycol (PEG) of 20 to 40 kDa was previously shown to prolong the residence time of rhDNase in the lungs of mice after pulmonary delivery while preserving its full enzymati... Read More about Biodistribution and elimination pathways of PEGylated recombinant human deoxyribonuclease I after pulmonary delivery in mice.

Development of an in vitro system to study the interactions of aerosolized drugs with pulmonary mucus (2020)
Journal Article
Alqahtani, S., Roberts, C. J., Stolnik, S., & Bosquillon, C. (2020). Development of an in vitro system to study the interactions of aerosolized drugs with pulmonary mucus. Pharmaceutics, 12(2), https://doi.org/10.3390/pharmaceutics12020145

© 2020 by the authors. Licensee MDPI, Basel, Switzerland. Mucus is the first biological component inhaled drugs encounter on their journey towards their pharmacological target in the upper airways. Yet, how mucus may influence drug disposition and ef... Read More about Development of an in vitro system to study the interactions of aerosolized drugs with pulmonary mucus.

Targeted PEG-poly(glutamic acid) complexes for inhalation protein delivery to the lung (2019)
Journal Article
Nieto-Orellana, A., Li, H., Rosiere, R., Wauthoz, N., Williams, H., Monteiro, C., …Stolnik, S. (2019). Targeted PEG-poly(glutamic acid) complexes for inhalation protein delivery to the lung. Journal of Controlled Release, 316, 250-262. https://doi.org/10.1016/j.jconrel.2019.10.012

Pulmonary delivery is increasingly seen as an attractive, non-invasive route for the delivery of forthcoming protein therapeutics. In this context, here we describe protein complexes with a new ‘complexing excipient’ - vitamin B12-targeted poly(ethyl... Read More about Targeted PEG-poly(glutamic acid) complexes for inhalation protein delivery to the lung.

In vitro investigation on the impact of airway mucus on drug dissolution and absorption at the air-epithelium interface in the lungs (2019)
Journal Article
Cingolani, E., Alqahtani, S., Sadler, R. C., Prime, D., Stolnik, S., & Bosquillon, C. (2019). In vitro investigation on the impact of airway mucus on drug dissolution and absorption at the air-epithelium interface in the lungs. European Journal of Pharmaceutics and Biopharmaceutics, 141, 210-220. https://doi.org/10.1016/j.ejpb.2019.05.022

Although the mucus layer is the first biological barrier encountered by inhaled drugs upon their deposition in the upper airways, its potential impact on drug dissolution and absorption in the lung has hardly been investigated. Bio-relevant in vitro... Read More about In vitro investigation on the impact of airway mucus on drug dissolution and absorption at the air-epithelium interface in the lungs.

Contribution of the alkylquinolone quorum sensing system to the interaction of Pseudomonas aeruginosa with bronchial epithelial cells. (2018)
Journal Article
Liu, Y., Hussain, F., Negm, O., Pavia, A., Halliday, N., Frédéric Dubern, J., …Martínez-Pomares, L. (2018). Contribution of the alkylquinolone quorum sensing system to the interaction of Pseudomonas aeruginosa with bronchial epithelial cells. Frontiers in Microbiology, 9, Article 3018. https://doi.org/10.3389/fmicb.2018.03018

Pseudomonas aeruginosa causes infections in patients with compromised epithelial 32 barrier function. Multiple virulence factors produced by P. aeruginosa are controlled 33 by quorum sensing (QS) via 2-alkyl-4(1H)-quinolone (AQ) signal molecules. Her... Read More about Contribution of the alkylquinolone quorum sensing system to the interaction of Pseudomonas aeruginosa with bronchial epithelial cells..

Comparison of gene transfection and cytotoxicity mechanisms of linear poly(amidoamine) and branched poly(ethyleneimine) polyplexes (2018)
Journal Article
Almulathanon, A. A., Ranucci, E., Ferruti, P., Garnett, M. C., & Bosquillon, C. (2018). Comparison of gene transfection and cytotoxicity mechanisms of linear poly(amidoamine) and branched poly(ethyleneimine) polyplexes. Pharmaceutical Research, 35(4), Article 86. https://doi.org/10.1007/s11095-017-2328-7

Purpose: This study aimed to further explore the mechanisms behind the ability of certain linear polyamidoamines (PAAs) to transfect cells with minimal cytotoxicity. Methods: The transfection efficiency of DNA complexed with a PAA of a molecular we... Read More about Comparison of gene transfection and cytotoxicity mechanisms of linear poly(amidoamine) and branched poly(ethyleneimine) polyplexes.

Dry-powder formulations of non-covalent protein complexes with linear or miktoarm copolymers for pulmonary delivery (2018)
Journal Article
Nieto-Orellana, A., Coghlan, D., Rothery, M., Falcone, F. H., Bosquillon, C., Childerhouse, N., …Stolnik, S. (2018). Dry-powder formulations of non-covalent protein complexes with linear or miktoarm copolymers for pulmonary delivery. International Journal of Pharmaceutics, 540(1-2), https://doi.org/10.1016/j.ijpharm.2018.02.008

Pulmonary delivery of protein therapeutics has considerable clinical potential for treating both local and systemic diseases. However, poor protein conformational stability, immunogenicity and protein degradation by proteolytic enzymes in the lung ar... Read More about Dry-powder formulations of non-covalent protein complexes with linear or miktoarm copolymers for pulmonary delivery.

A comparison of drug transport in pulmonary absorption models: isolated perfused rat lungs, respiratory epithelial cell lines and primary cell culture (2017)
Journal Article
Bosquillon, C., Madlova, M., Patel, N., Clear, N., & Forbes, B. (in press). A comparison of drug transport in pulmonary absorption models: isolated perfused rat lungs, respiratory epithelial cell lines and primary cell culture. Pharmaceutical Research, 34(12), https://doi.org/10.1007/s11095-017-2251-y

Purpose To evaluate the ability of human airway epithelial cell layers and a simple rat isolated perfused lung (IPL) model to predict pulmonary drug absorption in rats in vivo. Method The permeability of seven compounds selected to possess a r... Read More about A comparison of drug transport in pulmonary absorption models: isolated perfused rat lungs, respiratory epithelial cell lines and primary cell culture.

Ipratropium is ‘luminally recycled’ by an inter-play between apical uptake and efflux transporters in Calu-3 bronchial epithelial cell layers (2017)
Journal Article
Panduga, V., Stocks, M. J., & Bosquillon, C. (2017). Ipratropium is ‘luminally recycled’ by an inter-play between apical uptake and efflux transporters in Calu-3 bronchial epithelial cell layers. International Journal of Pharmaceutics, 532(1), https://doi.org/10.1016/j.ijpharm.2017.08.112

The mechanism by which quaternized anticholinergic bronchodilators permeate the airway epithelium remains controversial to date. In order to elucidate the role of drug transporters, ipratropium bidirectional transport as well as accumulation and rele... Read More about Ipratropium is ‘luminally recycled’ by an inter-play between apical uptake and efflux transporters in Calu-3 bronchial epithelial cell layers.

Enhanced expression of Organic Cation Transporters in bronchial epithelial cell layers following insults associated with asthma – impact on salbutamol transport (2017)
Journal Article
Mukherjee, M., Cingolani, E., Pritchard, D., & Bosquillon, C. (2017). Enhanced expression of Organic Cation Transporters in bronchial epithelial cell layers following insults associated with asthma – impact on salbutamol transport. European Journal of Pharmaceutical Sciences, 106, https://doi.org/10.1016/j.ejps.2017.05.052

Increasing evidence suggests Organic Cation Transporters (OCT) might facilitate the absorption of inhaled bronchodilators, including salbutamol, across the lung epithelium. This is essentially scarred and inflamed in asthma. Accordingly, the impact o... Read More about Enhanced expression of Organic Cation Transporters in bronchial epithelial cell layers following insults associated with asthma – impact on salbutamol transport.

Effect of polymer topology on non-covalent polymer-protein complexation: miktoarm versus linear mPEG-poly(glutamic acid) copolymers (2017)
Journal Article
Nieto-Orellana, A., Di Antonio, M., Conte, C., Falcone, F. H., Bosquillon, C., Childerhouse, N., …Stolnik, S. (in press). Effect of polymer topology on non-covalent polymer-protein complexation: miktoarm versus linear mPEG-poly(glutamic acid) copolymers. Polymer Chemistry, 8(14), https://doi.org/10.1039/C7PY00169J

Non-covalent polymer-protein conjugation is emerging as a potential route to improve pharmacokinetics and pharmacodynamics of protein therapeutics. In this study, a family of structurally related block copolymers of mPEG2k - poly(glutamic acid) with... Read More about Effect of polymer topology on non-covalent polymer-protein complexation: miktoarm versus linear mPEG-poly(glutamic acid) copolymers.

PEGylation of paclitaxel largely improves its safety and anti-tumor efficacy following pulmonary delivery in a mouse model of lung carcinoma (2016)
Journal Article
Luo, T., Loira-Pastoriza, C., Patil, H. P., Ucakar, B., Muccioli, G. G., Bosquillon, C., & Vanbever, R. (in press). PEGylation of paclitaxel largely improves its safety and anti-tumor efficacy following pulmonary delivery in a mouse model of lung carcinoma. Journal of Controlled Release, 239, https://doi.org/10.1016/j.jconrel.2016.08.008

Pulmonary delivery offers an attractive route of administration for chemotherapeutic agents, with the advantages of high drug concentrations locally and low side effects systemically. However, fast clearance mechanisms result in short residence time... Read More about PEGylation of paclitaxel largely improves its safety and anti-tumor efficacy following pulmonary delivery in a mouse model of lung carcinoma.

Synthesis and in vitro evaluation of polyethylene glycol-paclitaxel conjugates for lung cancer therapy (2016)
Journal Article
Alexander, C., Luo, T., Magnusson, J., Bosquillon, C., Préat, V., Frédérick, R., & Vanbever, R. (2016). Synthesis and in vitro evaluation of polyethylene glycol-paclitaxel conjugates for lung cancer therapy. Pharmaceutical Research, 33(7), 1671-1681. https://doi.org/10.1007/s11095-016-1908-2

Purpose Pulmonary drug delivery is considered an attractive route of drug administration for lung cancer chemotherapy. However, fast clearance mechanisms result in short residence time of small molecule drugs in the lung. Therefore, achieving a sust... Read More about Synthesis and in vitro evaluation of polyethylene glycol-paclitaxel conjugates for lung cancer therapy.

Digoxin net secretory transport in bronchial epithelial cell layers is not exclusively mediated by P-glycoprotein/MDR1 (2013)
Journal Article
Hutter, V., Chau, D. Y., Hilgendorf, C., Brown, A., Cooper, A., Zann, V., …Bosquillon, C. (2014). Digoxin net secretory transport in bronchial epithelial cell layers is not exclusively mediated by P-glycoprotein/MDR1. European Journal of Pharmaceutics and Biopharmaceutics, 86(1), 74-82. https://doi.org/10.1016/j.ejpb.2013.06.010

The impact of P-glycoprotein (MDR1, ABCB1) on drug disposition in the lungs as well as its presence and activity in in vitro respiratory drug absorption models remain controversial to date. Hence, we characterised MDR1 expression and the bidirectiona... Read More about Digoxin net secretory transport in bronchial epithelial cell layers is not exclusively mediated by P-glycoprotein/MDR1.