Lipids and polymers in pharmaceutical technology: lifelong companions

Juergen Siepmann (1, 2, 3) , Amina Faham (4) , Sophie-Dorothée Clas (5) , Ben Boyd (6) , Vincent Jannin (7) , Andreas Bernkop-Schnürch (8) , Hang Zhao (9, 10) , Sébastien Lecommandoux (9, 10) , James Evans (11) , Christine Allen (11) , Olivia Merkel (12) , Gabriella Costabile (12) , Morgan Alexander (13) , Ricky Wildman (13) , Clive Roberts (13) , Jean-Christophe Leroux (14)

1 INSERM - Institut National de la Santé et de la Recherche Médicale
2 CHRU Lille - Centre Hospitalier Régional Universitaire [CHU Lille]
3 MBLC - ADDS - Médicaments et biomatériaux à libération contrôlée: mécanismes et optimisation - Advanced Drug Delivery Systems - U 1008
4 DuPont Health & Nutrition
5 PharmaSolv Consulting
6 Monash Institute of Pharmaceutical Science
7 Gattefossé SAS
8 Leopold Franzens Universität Innsbruck - University of Innsbruck
9 LCPO - Laboratoire de Chimie des Polymères Organiques
10 Team 3 LCPO : Polymer Self-Assembly & Life Sciences
11 Department of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, Canada; 9Department of Biochemistry, Faculty of Medicine, University of Toronto
12 LMU - Ludwig Maximilian University [Munich] = Ludwig Maximilians Universität München
13 UON - University of Nottingham, UK
14 ETH Zürich - Eidgenössische Technische Hochschule - Swiss Federal Institute of Technology [Zürich]

In pharmaceutical technology, lipids and polymers are considered pillar excipients for the fabrication of most dosage forms, irrespective of the administration route. They play various roles ranging from support vehicles to release rate modifiers, stabilizers, solubilizers, permeation enhancers and transfection agents. Focusing on selected applications, which were discussed at the Annual Scientific Meeting of the Gattefossé Foundation 2018, this manuscript recapitulates the fundamental roles of these two important classes of excipients, either employed alone or in combination, and provides insight on their functional properties in various types of drug formulations. Emphasis is placed on oral formulations for the administration of active pharmaceutical ingredients with low aqueous solubilities or poor permeation properties. Additionally, this review article covers the use of lipids and polymers in the design of colloidal injectable delivery systems, and as substrates in additive manufacturing technologies for the production of tailor-made dosage forms.

Mots clés: peptides; gene delivery; polymersomes; liposomes; solid dispersions; self-emulsifying drug delivery systems; sustained release; 3D printing

Domaines: Polymères; Matériaux; Matière Molle [cond-mat.soft]; Sciences pharmaceutiques

Juergen Siepmann, Amina Faham, Sophie-Dorothée Clas, Ben Boyd, Vincent Jannin, et al.. Lipids and polymers in pharmaceutical technology: lifelong companions. International Journal of Pharmaceutics, 2019, 558, pp.128-142. ⟨10.1016/j.ijpharm.2018.12.080⟩. ⟨hal-01978128⟩