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Synthesis and Characterization of a Novel Degradabable Dendrimer and Preparation of Its Anti-tumor Prodrug

Author: FuJun
Tutor: ZhangXueFei
School: Xiangtan University
Course: Polymer Chemistry and Physics
Keywords: For controlled drug delivery system Dendrimer Oligomers Anticancer prodrugs Micelle
CLC: R914
Type: Master's thesis
Year: 2009
Downloads: 120
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Abstract

Controlled release of the drug and targeting administration in the human body is a hot today in the field of chemistry, medicine and pharmacy. How to make the drug to reach the lesion site quickly and accurately and to make a long-term release of drugs in the safety efficacy within is an important issue in today's drug delivery technologies. Macromolecular prodrug is a macromolecular compound as the carrier of a new drug delivery system. Its structure mainly include: active drug of the macromolecular carrier, small molecule, a linking group and a positioning base. The biodegradable polymer, they can degrade in the body, degradation products can be absorbed by the body or metabolized, the material of choice there is no accumulation of dangerous in the body, and therefore become the carrier of drug delivery systems. As a drug carrier material should include the following advantages: good biocompatibility and structural controlled accurately, narrow molecular weight distribution, a low toxicity and immunogenicity, biodegradability and efficient drug loading capacity. Dendrimer high degree of branching, spherical outer shape, surface functionalization and size accurately controllable as a drug carrier, etc. for its unique conditions. Dendrimer is a new class of efficient non-biological carrier, has a very broad application prospects in the field of medicine, with precise structure and morphology of dendritic macromolecules by chemical synthesis, can significantly improve the drug-loaded single molecule drug carrier the amount of the administration process to be achieved at the nanoscale. However, the dendrimers as drug carriers, there is poor biocompatibility, toxicity, non-degradable, limiting its application. We have designed a dendritic macromolecule composed of a glycerol and glycolic acid oligomers and other material of low biological toxicity, because the connection between which an ester bond, and has a good biodegradability. After to the dendrimer key connected to the PEG having a good biological describe and water soluble, may be formed with a good biocompatibility, low biological toxicity, and molecular weight distribution than the slaughter and having a biodegradable pharmaceutical carrier. Synthesis of different lengths glycolic acid oligomer, can control the the pharmacokinetic behavior expectations as an excellent drug carrier. Glycerol and glycolic acid oligomer template of dumbbell-shaped dendrimers, and polyethylene glycol - dendrimer as a carrier polymer micelle delivery system designed and prepared. The papers of dendritic macromolecules, the amphiphilic dendrimer polymer synthesis, characterization, as well as the drug-loaded micelles form size etc.. The specific contents are summarized as follows: a protected group was successfully synthesized accurate and controllable structure of the glycolic acid oligomer, wherein the carboxyl protecting group as tert-butyl. Glycerol and glycolic acid oligomer as a template the convergent synthesis algebra dendrimer. Finally, sebacic acid nuclear convergent synthesis of three generations of the dumbbell-shaped dendrimer structures were characterized using proton nuclear magnetic resonance (1H NMR). 2, MPEG end of a hydroxyl group with succinic anhydride under the reaction of the 4,4 '- dimethyl amino pyridine, there was obtained a terminal carboxyl group of MPEG. Dicyclohexyl carbodiimide (DCC) as a condensing agent, 4,4 '- dimethyl amino pyridine (DMAP) as catalyst, prepared end group is a carboxyl group of the polyethylene glycol monomethyl ether - three generations dendrimer molecular block copolymer. Further block polymer connected to paclitaxel, prepared the precise structure antitumor prodrug. And proton nuclear magnetic resonance (1H NMR) and gel permeation chromatography (GPC) its characterization. 3, the fluorescent probe Determination of polymer prodrug critical micelle concentration (CMC), investigated the micellization behavior.

Synthesis and Characterization of a Novel Degradabable Dendrimer and Preparation of Its Anti-tumor Prodrug

Abstract

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