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Associating Drugs with Polymer Nanoparticles: A Challenge Christelle Zandanel and Christine Charrueau

Abstract Conditions to achieve drug association with polymer nanoparticles are examined in this chapter. The different types of interactions and modes of association were considered using examples taken among 12 drugs that were associated with different types of nanoparticles using different approaches. The drugs were selected to represent the various properties of active pharmaceutical ingredient (API) varying from their lipophilicity and hydrophilicity and their low-or high-molecular weights. Strategies developed to enhance performance of drug loading are discussed in relation with the different methods used to associate drugs with polymer nanoparticles.











Keywords Active pharmaceutical ingredient Adsorption Drug loading Association Covalent bonding Electrostatic interactions Entrapment Hydrophobic interactions Hydrophobic drugs Hydrophilic drugs Polymer nanoparticles Small molecules Macromolecules

























1 Introduction Developing strategies to administer drug using nanoparticles has been widely studied and reported in the literature for drugs that presented delivery problems. Delivery of active pharmaceutical ingredients (API) by nanoparticles offers many possibilities to enhance their therapeutic potential while the formulations are suitable to be administered by systemic routes or used in topical applications. Depending on the nature of drugs and their applications, nanoparticles can be used: C. Zandanel (&) Institut Galien Paris Sud, UMR CNRS 8612, Univ. Paris-Sud, Université Paris Saclay, 5 Rue J.B. Clément, 92296 Chatenay-Malabry Cedex, France e-mail: [email protected] C. Charrueau Faculté de Pharmacie de L’Université Paris Descartes, Unité de Technologies Chimiques et Biologiques Pour La Santé UTCBS, CNRS UMR8258 – Inserm U1022, Paris, France © Springer International Publishing Switzerland 2016 C. Vauthier and G. Ponchel (eds.), Polymer Nanoparticles for Nanomedicines, DOI 10.1007/978-3-319-41421-8_13

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C. Zandanel and C. Charrueau

• to improve the bioavailability of drugs that are poorly absorbed helping the drug to go across biological barriers or preventing premature degradation in biological environments. • to reduce severe side effects of anticancer, anti-inflammatory, antifungal, antiviral, or immunosuppressive drugs thanks to a better control of their biodistribution enhancing the delivery to target sites and diverting distribution from sites, where the API is highly toxic. Nanoparticles are “intentionally produced particles with dimension characteristic ranging from 1 to 100 nm and that have properties that are not shared by non-nanoscale size particles of the same composition” (Auffan et al. 2009). As underlined by the authors, the second part of the definition is more relevant to characterize nanoparticles from the bulk as the term of nanoparticles is often generalized to all nano-objects with a size in the range of 10–1000 nm. Following European