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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.

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), Article 145. 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.

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., Mantovani, G., & 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.

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.

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., Pritchard, D. I., & 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.