Aim Polylactic acid (PLA) or polylactide-co-glycolide (PLGA) was used asbiodegradable and biocom-patible carriers to achieve sustained release ofestradial-PLGA/PLA-Microspheres (E_2-PLGA/PLA-MS). THF was added in the ...Aim Polylactic acid (PLA) or polylactide-co-glycolide (PLGA) was used asbiodegradable and biocom-patible carriers to achieve sustained release ofestradial-PLGA/PLA-Microspheres (E_2-PLGA/PLA-MS). THF was added in the organic phase to study itseffects on the properties of MS. Methods MS were formed by an emulsification-solvent extractionmethod with mixture of ethyl acetate (EtoAc) and tetrahydrofuran (THF) as the organic solvents, andthen the properties and in vitro drug release behavior were examined. Results The results indicatedthat the drug loading efficiency decreased when THF added, but when the ratio of EtoAc was more than50% , there was no obvious effect of THF ratio, but the particle size increased accordingly. Thecarriers' properties and the drug contents were the main factors influencing the in vitro drugrelease. Conclusions By controlling the technology and formulation, we can get sustained-release E_2biodegradable microsperes with proper particle size, drug content and low burst-release, althoughTHF with readily solubility in water was used in the organic phase.展开更多
The nanoparticles of polylactide (PLA) and poly(lactide-co-glycolide) (PLGA) were prepared by the bi-nary organic solvent diffusion method. The yield, particle size and size distribution of these nanoparticles wereeva...The nanoparticles of polylactide (PLA) and poly(lactide-co-glycolide) (PLGA) were prepared by the bi-nary organic solvent diffusion method. The yield, particle size and size distribution of these nanoparticles wereevaluated. The yield of nanoparticles prepared by this method is over 90%, and the average size of the nanoparticlesis between 130-180 nm. In order to clarify the effect of the organic solvent used in the system on nanoparticle yieldand size, the cloud points of PLA and PLGA were examined by cloud point titration. The results indicate that theyields of nanoparticles increase with the increase of ethanol in the acetone solution and attain the maximum at thecloud point of ethanol, while the size of nanoparticles decreases with the increase of ethanol in the acetone solutionand attains the minimum at the cloud point of ethanol. The optimal composition ratio of binary organic solvents coin-cides to that near the cloud point and the optimal condition of binary organic solvents can be predicted.展开更多
文摘Aim Polylactic acid (PLA) or polylactide-co-glycolide (PLGA) was used asbiodegradable and biocom-patible carriers to achieve sustained release ofestradial-PLGA/PLA-Microspheres (E_2-PLGA/PLA-MS). THF was added in the organic phase to study itseffects on the properties of MS. Methods MS were formed by an emulsification-solvent extractionmethod with mixture of ethyl acetate (EtoAc) and tetrahydrofuran (THF) as the organic solvents, andthen the properties and in vitro drug release behavior were examined. Results The results indicatedthat the drug loading efficiency decreased when THF added, but when the ratio of EtoAc was more than50% , there was no obvious effect of THF ratio, but the particle size increased accordingly. Thecarriers' properties and the drug contents were the main factors influencing the in vitro drugrelease. Conclusions By controlling the technology and formulation, we can get sustained-release E_2biodegradable microsperes with proper particle size, drug content and low burst-release, althoughTHF with readily solubility in water was used in the organic phase.
基金Project ( 2001AA218011) supported by the National High Technology Development "863" Program of China
文摘The nanoparticles of polylactide (PLA) and poly(lactide-co-glycolide) (PLGA) were prepared by the bi-nary organic solvent diffusion method. The yield, particle size and size distribution of these nanoparticles wereevaluated. The yield of nanoparticles prepared by this method is over 90%, and the average size of the nanoparticlesis between 130-180 nm. In order to clarify the effect of the organic solvent used in the system on nanoparticle yieldand size, the cloud points of PLA and PLGA were examined by cloud point titration. The results indicate that theyields of nanoparticles increase with the increase of ethanol in the acetone solution and attain the maximum at thecloud point of ethanol, while the size of nanoparticles decreases with the increase of ethanol in the acetone solutionand attains the minimum at the cloud point of ethanol. The optimal composition ratio of binary organic solvents coin-cides to that near the cloud point and the optimal condition of binary organic solvents can be predicted.