Drug Loading in Poly(butyl cyanoacrylate)-Based Polymeric Microbubbles

Molecular Pharmaceutics, vol. 17, pp. 2840–2848

Abstract

Microbubbles (MB) are routinely used ultrasound (US) contrast agents that have recently attracted increasing attention as stimuli-responsive drug delivery systems. To better understand MB-based drug delivery, we studied the role of drug hydrophobicity and molecular weight on MB loading, shelf-life stability, US properties, and drug release. Eight model drugs, varying in hydrophobicity and molecular weight, were loaded into the shell of poly(butyl cyanoacrylate) (PBCA) MB. In the case of drugs with progesterone as a common structural backbone (i.e., for corticosteroids), loading capacity and drug release correlated well with hydrophobicity and molecular weight. Conversely, when employing drugs with no structural similarity (i.e., four different fluorescent dyes), loading capacity and release did not correlate with hydrophobicity and molecular weight. All model drug-loaded MB formulations could be equally efficiently destroyed upon exposure to US. Together, these findings provide valuable insights on how the physicochemical properties of (model) drug molecules affect their loading and retention in and US-induced release from polymeric MB, thereby facilitating the development of drug-loaded MB formulations for US-triggered drug delivery.

Authors 7

1. Mengjiao Liu Aachen Institute for Experimental Molecular Imaging

   Universitätsklinikum Aachen · RWTH Aachen University

   Affiliation as printed

   Institute for Experimental Molecular Imaging, RWTH Aachen University Clinic, Aachen 52074, Germany

2. Anshuman Dasgupta Aachen Institute for Experimental Molecular Imaging

   Universitätsklinikum Aachen · RWTH Aachen University

   Affiliation as printed

   Institute for Experimental Molecular Imaging, RWTH Aachen University Clinic, Aachen 52074, Germany

3. Patrick Koczera Aachen Department of Intensive Care Medicine Medical Faculty Institute for Experimental Molecular Imaging

   Universitätsklinikum Aachen · RWTH Aachen University

   Affiliation as printed

   Department of Intensive Care Medicine, Medical Faculty, RWTH Aachen University Clinic, Aachen 52074, Germany

   Institute for Experimental Molecular Imaging, RWTH Aachen University Clinic, Aachen 52074, Germany

4. Dirk Rommel Aachen DWI - Leibniz Institute for Interactive Materials

   DWI – Leibniz Institute for Interactive Materials · RWTH Aachen University

   Affiliation as printed

   DWI—Leibniz Institute for Interactive Materials, RWTH Aachen University, Aachen 52074, Germany

5. Yang Mei Shi Aachen Institute for Experimental Molecular Imaging

   Universitätsklinikum Aachen · RWTH Aachen University

   Affiliation as printed

   Institute for Experimental Molecular Imaging, RWTH Aachen University Clinic, Aachen 52074, Germany

6. Fabian M. Kiessling Aachen Institute for Experimental Molecular Imaging

   Universitätsklinikum Aachen · RWTH Aachen University

   Affiliation as printed

   Institute for Experimental Molecular Imaging, RWTH Aachen University Clinic, Aachen 52074, Germany

7. Twan Lammers corresponding Aachen Institute for Experimental Molecular Imaging

   Universitätsklinikum Aachen · RWTH Aachen University

   Affiliation as printed

   Institute for Experimental Molecular Imaging, RWTH Aachen University Clinic, Aachen 52074, Germany