Biological safety and stable sustained-release of the drug are two crucial issues involved in the formulation of paclitaxel.Focusing on these issues, by using the FDA approved polylactide as carrier material, soybean ...Biological safety and stable sustained-release of the drug are two crucial issues involved in the formulation of paclitaxel.Focusing on these issues, by using the FDA approved polylactide as carrier material, soybean lecithin as surfactant and maltodextrin as thickener, paclitaxel loaded PLA microspheres were simply prepared by solvent evaporation, thus guaranteeing the biological safety. The introduction of maltodextrin as a thickener aided to a stable sustained-release of paclitaxel. Surface morphology, particle size, drug loading rate, encapsulation efficiency and in vitro drug release behavior were investigated.Biological safety evaluations such as acute toxicity, allergies, hemolysis, skin stimulation and genotoxicity test were also carried out. Results showed that the obtained microspheres were biocompatible and could release paclitaxel at a desirable constant rate.Therefore, the simply prepared paclitaxel formulation with good biological safety and desirable release behavior exhibited great potential of local injection of paclitaxel for the clinical use in the future.展开更多
Poly(L-lactide)-b-poly(ethylene glycol)(PLLA-PEG) microspheres containing dexamethasone(Dex) have been fabricated using a spray-drying technique.Porous poly(lactic-co-glycolic acid)(PLGA) scaffolds were prepared using...Poly(L-lactide)-b-poly(ethylene glycol)(PLLA-PEG) microspheres containing dexamethasone(Dex) have been fabricated using a spray-drying technique.Porous poly(lactic-co-glycolic acid)(PLGA) scaffolds were prepared using a method combining thermally induced phase separation and porogen leaching.A post-seeding technique was used to immobilize Dex-containing PLLA-PEG microspheres on porous PLGA scaffolds,and drug-containing microspheres-scaffolds(MS-S) were obtained.Simple Dex-containing scaffolds(D-S) were also made as the control by directly dissolving Dex in the PLGA solution during scaffold fabrication.The morphologies of microspheres and scaffolds were studied by scanning electron microscopy.Drug release profiles of both MS-S and D-S were determined under cyclic loading and shaking water bath,respectively.The cumulative release of Dex was measured using an ultraviolet visible spectrophotometer.The results show that the incorporation of Dex and microspheres had little effect on the overall morphology of the porous PLGA scaffolds.Cyclic loading significantly accelerated the release of Dex from the drug-containing scaffolds.Compared with D-S,MS-S reduced the drug release rate.The controlled drug delivery of tissue engineering scaffolds under cyclic loading is a key factor to mimic the in vivo mechanical environments and achieve optical clinical efficacy.展开更多
The effect of branching on the blood circulation and tumor targeting of polymer nanovehicles in vivo was investigated in this study. For the purpose, star-branched poly(lactic acid) and poly(2-methacryloyloxyethyl pho...The effect of branching on the blood circulation and tumor targeting of polymer nanovehicles in vivo was investigated in this study. For the purpose, star-branched poly(lactic acid) and poly(2-methacryloyloxyethyl phosphorylcholine)(PLA-PMPC)copolymers with umbrella-type AB3,(AB3)_(2), and(AB3)_(3) architecture were synthesized by branching at the PLA core. Micelles self-assembled from these copolymers were used to evaluate the effect of core branching on blood circulation and tumor targeting. The results showed that branching changed the behavior of polymeric self-assembly in solution, thereby changing the size and surface anti-fouling performance of the polymeric micelles. Moreover, star-branched copolymer micelles with a higher branching degree allowed their payload to persist better in blood(half-time prolonged from 7.1, 8.6 to 13.8 h) and for a 1.72-fold higher content at the tumor site. These studies suggest that raising the branching degree of amphiphilic copolymer potentially offers a promising strategy for the design of carriers capable of enhanced circulation and targeting in vivo.展开更多
基金supported by the National Natural Science Foundation of China(Grant Nos.51073118,51473119)
文摘Biological safety and stable sustained-release of the drug are two crucial issues involved in the formulation of paclitaxel.Focusing on these issues, by using the FDA approved polylactide as carrier material, soybean lecithin as surfactant and maltodextrin as thickener, paclitaxel loaded PLA microspheres were simply prepared by solvent evaporation, thus guaranteeing the biological safety. The introduction of maltodextrin as a thickener aided to a stable sustained-release of paclitaxel. Surface morphology, particle size, drug loading rate, encapsulation efficiency and in vitro drug release behavior were investigated.Biological safety evaluations such as acute toxicity, allergies, hemolysis, skin stimulation and genotoxicity test were also carried out. Results showed that the obtained microspheres were biocompatible and could release paclitaxel at a desirable constant rate.Therefore, the simply prepared paclitaxel formulation with good biological safety and desirable release behavior exhibited great potential of local injection of paclitaxel for the clinical use in the future.
基金support from the National Natural Science Foundation of China (Grant Nos 10672015 & 30828008)
文摘Poly(L-lactide)-b-poly(ethylene glycol)(PLLA-PEG) microspheres containing dexamethasone(Dex) have been fabricated using a spray-drying technique.Porous poly(lactic-co-glycolic acid)(PLGA) scaffolds were prepared using a method combining thermally induced phase separation and porogen leaching.A post-seeding technique was used to immobilize Dex-containing PLLA-PEG microspheres on porous PLGA scaffolds,and drug-containing microspheres-scaffolds(MS-S) were obtained.Simple Dex-containing scaffolds(D-S) were also made as the control by directly dissolving Dex in the PLGA solution during scaffold fabrication.The morphologies of microspheres and scaffolds were studied by scanning electron microscopy.Drug release profiles of both MS-S and D-S were determined under cyclic loading and shaking water bath,respectively.The cumulative release of Dex was measured using an ultraviolet visible spectrophotometer.The results show that the incorporation of Dex and microspheres had little effect on the overall morphology of the porous PLGA scaffolds.Cyclic loading significantly accelerated the release of Dex from the drug-containing scaffolds.Compared with D-S,MS-S reduced the drug release rate.The controlled drug delivery of tissue engineering scaffolds under cyclic loading is a key factor to mimic the in vivo mechanical environments and achieve optical clinical efficacy.
基金supported by the National Natural Science Foundation of China (Grant No. 51773151)。
文摘The effect of branching on the blood circulation and tumor targeting of polymer nanovehicles in vivo was investigated in this study. For the purpose, star-branched poly(lactic acid) and poly(2-methacryloyloxyethyl phosphorylcholine)(PLA-PMPC)copolymers with umbrella-type AB3,(AB3)_(2), and(AB3)_(3) architecture were synthesized by branching at the PLA core. Micelles self-assembled from these copolymers were used to evaluate the effect of core branching on blood circulation and tumor targeting. The results showed that branching changed the behavior of polymeric self-assembly in solution, thereby changing the size and surface anti-fouling performance of the polymeric micelles. Moreover, star-branched copolymer micelles with a higher branching degree allowed their payload to persist better in blood(half-time prolonged from 7.1, 8.6 to 13.8 h) and for a 1.72-fold higher content at the tumor site. These studies suggest that raising the branching degree of amphiphilic copolymer potentially offers a promising strategy for the design of carriers capable of enhanced circulation and targeting in vivo.
