Twin-screw extruded phospholipid implants for controlled parenteral delivery

Prof. Dr. R. Bodmeier1) and Dr. M. Kolbina1), FU Berlin/Germany

+ Show more

1.

Prof. Dr. Roland Bodmeier and Dr. Marina KolbinaCollege of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, Germany

People involved

Dr Marina Kolbina (Postdoc sponsored by the PRC) - FU Berlin, Germany (marina.kolbina@fu-berlin.de)

Abstract

Controlled parenteral drug delivery presents many advantages compared to conventional parenteral formulations. Along with biodegradable polymers, phospholipids have been widely applied in this field, resulting in several commercially available formulations primarily based on liposomes. Solid implants present several advantages compared to colloidal phospholipid formulations. Namely, the ease of manufacture, drug molecule stability during the manufacturing process (e.g. protein or drugs prone to hydrolysis), as well as stability during storage. Additionally, the use of lipid-based solid implants avoids such drawbacks as microenvironmental acidification and, potentially, interactions with incorporated proteins, which may lead to protein aggregation and incomplete release, compared to poly(lactide-co-glycolide) (PLGA).

The feasibility to prepare hydrogenated soybean phosphatidylcholine (HSPC) implants by hot melt extrusions has been described recently.1) The drug release rate from extrudates varied from several days to several months depending on drug solubility, drug loading, and implant dimensions, making this system interesting for parenteral controlled release application. The project is a follow-up study on phospholipids hot melt extrusion to define critical process and formulation parameters and to demonstrate the applicability of phospholipid-based implants for parenteral controlled delivery both for small molecule drugs and model proteins. The studies will additionally cover investigations on terminal sterilization option and the physicochemical stability of the dosage forms to support the applicability of the proposed formulation options.

Benefit for the community

The community could benefit from the replacement of synthetic excipients using a biodegradable excipient from natural sources.

Visit the supervisors lab

Contact

References:
1.
Kolbina M, Schulte A, van Hoogevest P, Körber M, Bodmeier R, 2019
Evaluation of Hydrogenated Soybean Phosphatidylcholine Matrices Prepared by Hot Melt Extrusion for Oral Controlled Delivery of Water-Soluble Drugs
AAPS PharmSciTech 20, 159