Issue 23, 2020

Optimisation and feature selection of poly-beta-amino-ester as a drug delivery system for cartilage

Abstract

Drug localisation is still one of the main challenges in treating pathologies affecting cartilage; poly-beta-amino-esters (PBAEs) drug conjugates are a possible solution; however, their efficacy highly depends on the polymer structure hence the full potential of this delivery system is still unknown. For the purpose of optimising the delivery system design, a large library of PBAEs was synthesised and dexamethasone (DEX) uptake in cartilage was determined. All three components of PBAE (amine, acrylate and end-capping) impacted the outcome. The most effective PBAE identified enhanced DEX uptake by 8 folds compared to an equivalent dose of the commercial formulation and also prevented, through delivery of DEX, the cartilage degradation caused by IL-1α (interleukine1α). A chemometrics based predictive model was constructed and PBAEs properties most affecting the performance of the drug delivery systems were identified. This model will allow further computer based PBAEs optimisation and fast track the bench to market process for this delivery system.

Graphical abstract: Optimisation and feature selection of poly-beta-amino-ester as a drug delivery system for cartilage

Supplementary files

Article information

Article type
Paper
Submitted
08 dek 2019
Accepted
14 apr 2020
First published
15 may 2020
This article is Open Access
Creative Commons BY license

J. Mater. Chem. B, 2020,8, 5096-5108

Optimisation and feature selection of poly-beta-amino-ester as a drug delivery system for cartilage

S. Perni and P. Prokopovich, J. Mater. Chem. B, 2020, 8, 5096 DOI: 10.1039/C9TB02778E

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