How to predict what happens to long-acting injectables?

We are very happy to announce that Ge Fiona Gao just got her second first-author paper accepted by the Journal of Controlled Release. Our investigation of the drug release from PLGA microspheres highlights the need for biorelevant conditions to simulate degradation effects and predict bioavailability. Our international team of authors from Germany, Singapore, and Japan established in vitro-in vivo correlations for two drug formulations of tacrolimus. The formulations were tested in biorelevant medium in presence of protein background using the DR technology. To establish the IVIVC, a drug recovery model and a membrane permeation model were used and the fraction released in the in-vitro system was calculated. Mechanistic understanding of the physiological processes was gained by means of an in-silico model reflecting the absorption mechanisms in the subcutaneous tissue. The interplay between release, drug diffusion, lymphatic transport, and degradation plays a key role in the performance of injectables that remain in the subcutaneous tissue for a longer time period. Once production is over, the manuscript will become available under:

Gao GF, Ashtikar M, Kojima R, Yoshida T, Kaihara M, Tajiri T, Shanehsazzadeh S, Modh H, Wacker MG (2020); Predicting drug release and degradation kinetics of long-acting microsphere formulations of tacrolimus for subcutaneous injection, J Control Release (Accepted for publication) 

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