Active Targeting
Actively targeted nanomedicines are drug delivery systems based on nanocarriers loaded with a therapeutic and/or imaging agent in which a targeting moiety has been attached onto their surface, with the aim of targeting and interacting with a specific rece
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Active Targeting Dolores Remedios Serrano Lopez and Aikaterini Lalatsa
Abstract Actively targeted nanomedicines are drug delivery systems based on nanocarriers loaded with a therapeutic and/or imaging agent in which a targeting moiety has been attached onto their surface, with the aim of targeting and interacting with a specific receptor, in order to elicit their effect. Three major components should be carefully considered in order to design an optimal nanomedicine including: the nanocarrier (e.g. liposomes, particles, dendrimers, micelles), the targeting moiety (e.g. proteins, peptides, oligonucleotides, carbohydrates), and the therapeutic and/or imaging agent. Nowadays, promising approaches have been developed, especially in the field of cancer and central nervous system diseases. However, very few active targeted nanomedicines have progressed from the proof-of-concept to clinical trials.
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Active Targeting of Nanomedicines Principles of Active Targeting of Nanomedicines
Actively targeted nanomedicines are drug delivery systems engineered using nanocarriers loaded with therapeutic and/or imaging agents possessing on their surface a targeting moiety. This targeting moiety can be an antibody or other protein, a carbohydrate, or a nucleic acid sequence in order to allow the nanoparticles to interact specifically with cells possessing the respective receptor. It is important to
D.R. Serrano Lopez Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, Complutense University of Madrid, Madrid, Spain A. Lalatsa (*) School of Pharmacy & Biomedical Sciences, University of Portsmouth, St. Michael Building, Portsmouth PO1 2DT, UK e-mail: [email protected] I.F. Uchegbu et al. (eds.), Fundamentals of Pharmaceutical Nanoscience, DOI 10.1007/978-1-4614-9164-4_13, © Springer Science+Business Media New York 2013
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D.R. Serrano Lopez and A. Lalatsa
Fig. 13.1 Active and passive targeting of nanomedicines. Nanomedicines can reach tumours selectively using biological mechanisms such as the EPR effect which results from the disorganised pathology of angiogenic tumour vasculature with its discontinuous endothelium, leading to hypermeability to circulating nanoparticles, and the lack of effective tumour lymphatic drainage, which leads to subsequent nanoparticle accumulation. On the other hand, active targeted nanomedicines accumulate in cells (in this case cancer cells) based on the interaction between the targeting moieties grafted at the surface of the nanoparticle that can bind specifically to receptors over-expressed by the cells
distinguish the term “targeted drug delivery” from “targeted therapy” which is commonly used in drug discovery referring to specific interactions between a drug and its receptor at the molecular level (Gerber 2008; Bae and Park 2011). Four key requirements are usually necessary for an effective actively targeted nanomedicine: (a) evasion from opsonisation and clearance by the liver and kidneys allowing sufficient circulation in the organism; (b) reten
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