Schlosser, Corinna S;
Morris, Christopher J;
Brocchini, Steve;
Williams, Gareth R;
(2024)
Hydrophobic ion pairing as a novel approach to co-axial electrospraying of peptide-PLGA particles.
International Journal of Pharmaceutics
, Article 124885. 10.1016/j.ijpharm.2024.124885.
(In press).
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Abstract
Electrospraying is a processing technique that has gained much interest to prepare polymeric particles. The technique operates at ambient temperature, thereby avoiding heat induced degradation of labile therapeutics (e.g. peptides and proteins). Exposure to organic solvents can be minimised by co-axial electrospraying through separation of core (aqueous) and shell (organic) solvents. However, aqueous solutions are often difficult to electrospray due to high surface tension. Immiscibility between the core–shell solvents creates a further process challenge. Herein, we describe for the first time the use of hydrophobic ion pairing (HIP) to encapsulate a polypeptide into polymeric particles prepared by co-axial electrospraying. Peptide ion pairs were prepared to incorporate a model peptide – teriparatide – into an organic solvent, permitting facile electrospraying while also protecting the peptide from denaturation. Teriparatide loaded PLGA particles were generated by electrospraying from aqueous or ethanolic peptide solutions (core). A PLGA solution in chloroform (with and without co-solvents) was employed as the shell solution. The aqueous core solution led to a teriparatide encapsulation efficiency of 79.2 ± 19.8 %, which was not significantly different from the ethanolic core (57.1 ± 14.5 %). When aqueous solutions were used the process lacked reproducibility, resulting in low process yields (61.3 ± 4.0 %). In contrast, when an organic core was used a dry powder bed was achieved with a yield of 102.2 ± 8.8 %. The peptide’s integrity and biological functionality were retained after electrospraying as ion pairs, as evidenced in a cell-based PTH1R receptor binding assay.
| Type: | Article |
|---|---|
| Title: | Hydrophobic ion pairing as a novel approach to co-axial electrospraying of peptide-PLGA particles |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1016/j.ijpharm.2024.124885 |
| Publisher version: | https://doi.org/10.1016/j.ijpharm.2024.124885 |
| Language: | English |
| Additional information: | © The Author(s), 2024. This is an Open Access article distributed under the terms of the Creative Commons Attribution Licence (CC BY 4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. https://creativecommons.org/licenses/by/4.0/ |
| Keywords: | Teriparatide, Peptide, Hydrophobic-ion-pairing, Electrospraying, PLGA, Controlled release, PTH1R |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics |
| URI: | https://discovery.ucl.ac.uk/id/eprint/10199998 |
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