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Research on Curcumin-Loaded PLGA-PEG-PLGA Micelles

Author: SongZhiMei
Tutor: DiGuangXi
School: Shandong University
Course: Pharmacy
Keywords: Curcumin PLGA - PEG - PLGA micelle In vitro release Pharmacokinetic Tissue distribution
CLC: R283
Type: Master's thesis
Year: 2011
Downloads: 241
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Abstract


Curcumin (Curcumin, CUR) for yellow bisphenol compounds, with a variety of pharmacological effects of the anti-tumor, anti-inflammatory, anti-viral, anti-oxidation. But its water-soluble nature of instability, rapid in vivo metabolism, low bioavailability, has seriously hampered its development and application. How to improve all aspects of the CUR shortcomings prepared bioavailability, a low dosage CUR formulation has become in recent years, pharmaceutical workers problems to be solved. Hydrophobic - hydrophilic segment amphiphilic block copolymers can be assembled to form spontaneously in aqueous solution with core - shell structure of supramolecular aggregates micelles in an orderly manner, in the shell of hydrophilic segments to avoid drugs and The contact of the water environment, stable polymeric micelles to avoid the identification of the reticuloendothelial system in the body; hydrophobic segments kernel provides a hydrophobic microenvironment, to increase the solubility of poorly soluble substances in the water environment. Class micelles can improve the water solubility of the lipophilic drug, improved drug release characteristics to achieve targeted drug release control. Firstly, PLGA-PEG-PLGA block copolymer synthesis, structural characterization and study. On this basis, the PLGA-PEG-PLGA package contains CUR micelles Preparation, assay methods, and particle size distribution determined by the critical micelle concentration of the block copolymer, blank and drug-loaded micelles drug-loaded micelles zeta potential and microscopic morphology and in vitro release behavior. At the same time, the HPLC method for the extraction and quantitative analysis of plasma and tissues CUR CUR drug-loaded micelles pharmacokinetic properties and tissue distribution. The study found that using the the water dialysis method of preparing CUR of PLGA-PEG-PLGA micelle, its encapsulation rate average of 70.03 ± 0.34%, the drug loading average of 6.4 ± 0.02%, an average particle diameter of 26.29nm calculated Medicine The solubility of 1.47mg/ml zeta potential-0.7lmV. The in vitro release of CUR micelles in vitro release presents the first burst release after sustained-release characteristics, in line with the two-phase double exponential kinetic model. Pharmacokinetic studies have shown that CUR micelles drug area under the curve, mean residence time, elimination half-life and distribution half-life is higher than that of the control preparation, control preparations were 1.31 times, 2.67 times, 2.48 times and 4.54 times. , But also reduces the the CUR total plasma clearance rate and peak concentration. Half-life, the average residence time of the extension, and a lower total clearance, suggesting a duration of action in vivo the micelle may extend CUR. The tissue distribution study found that, compared with the CUR control preparation CUR micelles in brain, lung Ce values ??were 2.00 and 1.02; the relatively uptake rate (Relative uptake efficiency, RUE) 14.31,5.56; relative target rate (Relative targeting efficiency, RTE) 247.22% and 34.72%, respectively, indicating that the micelles could significantly promote the distribution and concentration of CUR in the brain and lungs.

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CLC: > Medicine, health > Chinese Medicine > Of Pharmacy > Chinese medicine processing,preparation
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