Drug Delivery by Polymer Nanoparticles: The Challenge of Controlled Release and Evaluation
The controlled release of the drugs at the site of action is a key issue for nanoparticulate carriers. The purpose of this chapter is to review the current strategies used to control the release profiles of polymer nanoparticles. Based on 12 representativ
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Drug Delivery by Polymer Nanoparticles: The Challenge of Controlled Release and Evaluation Christine Charrueau and Christelle Zandanel
Abstract The controlled release of the drugs at the site of action is a key issue for nanoparticulate carriers. The purpose of this chapter is to review the current strategies used to control the release profiles of polymer nanoparticles. Based on 12 representative drugs with hydrophobic or hydrophilic properties, the mechanisms controlling the drug release are described, the different ways to tune the release profile are analyzed, and the methods for evaluating drug release from nanoparticles are discussed. In conclusion, based on the physicochemical properties of the drugs, the types and characteristics of nanoformulations, and the route of administration, promising tracks for tuning release profiles can be proposed. Suggestions for choosing the most appropriate methods for studying drug release are also presented.
Keywords Drug release Nanoparticles Hydrophobic drugs Hydrophilic drugs Dissolution Dialysis Diffusion Pharmacokinetics Release evaluation
1 Introduction The endpoint of nanomedicines and of approaches consisting in developing polymer nanoparticulate carriers of drugs is, first, to control the pharmacokinetics and biodistribution of the drugs to improve their delivery to target tissues and cells, and second, to control the release of the drugs at the site of action. While the first events are developed in other chapters, the present chapter deals with the challenge of drug release at the site of action. To achieve that goal, the association between the drug and its nanoparticulate C. Charrueau (&) Faculté de Pharmacie de l’Université Paris Descartes, Unité de Technologies Chimiques et Biologiques pour la Santé UTCBS, CNRS UMR8258 – Inserm U1022, 4 avenue de l’Observatoire, 75270 Paris Cedex 06, France e-mail: [email protected] C. Zandanel Institut Galien Paris Sud, UMR CNRS 8612, Univ. Paris Sud, Université Paris-Saclay, Châtenay-Malabry, France © Springer International Publishing Switzerland 2016 C. Vauthier and G. Ponchel (eds.), Polymer Nanoparticles for Nanomedicines, DOI 10.1007/978-3-319-41421-8_14
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polymer carrier needs to be stable during its distribution from the administration site to the target site. The encapsulation and retention of the drug into its carrier can be controlled by different formulation methods that are described in the Chap. 13 by Zandanel and Charrueau. Once the target is reached, the carrier must release the drug with the appropriate rate. Ideally, the release would be triggered by specific stimuli allowing for “on demand” release. One of the main problems to overcome is the phenomenon of uncontrolled burst release. This chapter aims at explaining the current strategies employed to control the drug release from polymer nanoparticles. This will be discussed from examples of 12 representative drugs which properties are described in this chapter. Main physicochem
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