Biomedical Engineering Reference
In-Depth Information
CHAPTER 9
Design of Complex Micelles for
Drug Delivery
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RUJIANG MA AND LINQI SHI*
Key Laboratory of Functional Polymer Materials, Ministry of Education, and
Institute of Polymer Chemistry, Nankai University, Tianjin 300071, P. R.
China
* E-mail: shilinqi@nankai.edu.cn
9.1 Introduction
Polymeric micelles have been extensively studied as controlled drug delivery
vehicles based on their inherent properties 1 such as tunable size in the nano
range, stability against agglomeration, and long circulation time due to the
protection by hydrophilic shells of poly(ethylene glycol) (PEG), enhancement
of solubility of insoluble drugs, and decrease of toxicity of drugs. More
importantly, polymeric micelles can be passively targeted to tumor issue by the
enhanced permeability and retention (EPR) effect or actively targeted to
cancer cells by conjugating with many ligands such as antibody fragments,
epidermal growth factors, folate, etc.
Typical polymeric micelles for drug delivery are generally composed of a
hydrophobically associated biodegradable core and a soluble PEG shell for
biocompatibility. Water-insoluble drugs such as doxorubicin (DOX) and
paclitaxel (PTX) can be loaded into the micelle core by hydrophobic
interaction. The hydrophilic PEG shell protects the drug-loaded micelle not
only from aggregation but also from nonspecific adsorption of proteins in the
blood circulation. However, a simple core-shell structure is vulnerable under
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