Ji-ying Men, Bao-jiao Gao, Zhi-ping Chen. PREPARATION OF GRAFTED MICROSPHERES CPVA-g-PSSS AND STUDIES ON THEIR CHARACTER OF DRUG CARRYING AND COLON-SPECIFIC DRUG DELIVERY FOR 5-FLUOROURACIL. [J]. Acta Polymerica Sinica (9):943-951(2012)
DOI:
Ji-ying Men, Bao-jiao Gao, Zhi-ping Chen. PREPARATION OF GRAFTED MICROSPHERES CPVA-g-PSSS AND STUDIES ON THEIR CHARACTER OF DRUG CARRYING AND COLON-SPECIFIC DRUG DELIVERY FOR 5-FLUOROURACIL. [J]. Acta Polymerica Sinica (9):943-951(2012) DOI: 10.3724/SP.J.1105.2012.12003.
PREPARATION OF GRAFTED MICROSPHERES CPVA-g-PSSS AND STUDIES ON THEIR CHARACTER OF DRUG CARRYING AND COLON-SPECIFIC DRUG DELIVERY FOR 5-FLUOROURACIL
The graft-polymerization of sodium 4-styrene sulfonate (SSS) was performed on the surfaces of crosslinked polyvinyl alcohol (CPVA) microspheres using cerium salt-hydroxyl group redox initiation system
and the grafted microspheres CPVA-g-PSSS
on which the strong anionic polyelectrolyte PSSS was grafted
was obtained.The chemical structure and physicochemistry characters of CPVA-g-PSSS microspheres were adequately characterized by infrared spectrum (FTIR)
scanning electron microscope (SEM) and determination of zeta potential.On this basis
the adsorption property of CPVA-g-PSSS microspheres for 5-fluorouracil (5-FU)
namely the drug carrying ability
was mainly investigated and the adsorption mechanism was discussed.The in vitro release behavior of the drug-carried microspheres was also examined.The experimental results show that cerium salt-hydroxyl group redox initiation system can effectively initiate the graft polymerization of SSS on CPVA microspheres
and under the suitable conditions
the grafting degree of PSSS can reach 16.1 g/100g.In the acidic medium
the grafted microspheres CPVA-g-PSSS exhibit very strong adsorption ability for 5-FU by driving of electrostatic interaction.The adsorption capacity can get up to 105 mg/g
displaying the high efficiency of drug-loading.The in vitro release behavior of the drug-carrying microspheres is highly pH-dependent.In the medium of pH=1
the drug is not released
while in the medium of pH=7.4
the burst release phenomenon will be produced
displaying an excellent colon-specific drug delivery behavior.
关键词
对苯乙烯磺酸钠交联聚乙烯醇微球接枝聚合5-氟尿嘧啶pH依赖性结肠定位释放
Keywords
Sodium 4-styrene sulfonateCrosslinked polyvinyl alcohol microspheresGraft polymerization5-FluorouracilpH-dependenceColon-specific drug delivery