【摘要】：目的:以自制材料乙交酯丙交酯共聚物-維生素E聚乙二醇1000琥珀酸酯(polylactide-co-glycolide-D-α-tocopheryl polyethylene glycol 1000 succinate,PLGA-TPGS)為載體制備脂蟾毒配基PLGA-TPGS納米粒(Resibufogenin-loaded PLGATPGS nanoparticles,RPTN),并以市售材料乙交酯丙交酯共聚物(PLGA)為載體制備脂蟾毒配基PLGA納米粒(RBG-loaded PLGA nanoparticles,RPN),體外評價和比較2種納米粒的質(zhì)量。方法:采用超聲乳化-溶劑揮發(fā)法制備RPTN和RPN,用透射電子顯微鏡和激光粒度儀分別測定二者的外觀、粒徑、表面電荷。采用反相高效液相色譜法,色譜柱為Hypersil C_(18)(4.6mm×250 mm,5μm),甲醇和0.05%冰醋酸溶液(9∶1)為流動相,檢測波長為298 nm,測定RBG在RPTN和RPN中的載藥量、包封率和體外釋放度。結(jié)果:RPTN和RPN的粒徑分別為152.3 nm和331.7 nm,載藥量和包封率分別為18.4%、79.3%和15.1%、68.6%。體外藥物釋放30 d時RPTN和RPN的體外累積釋放率分別為86.7%和72.3%,RPTN釋放較完全。結(jié)論:自制載體制備的RPTN比RPN粒徑更小,載藥量和包封率更大,體外有明顯的緩釋作用,釋放更完全。
[Abstract]:Objective: to prepare PLGA-TPGS nanoparticles (Resibufogenin-loaded PLGATPGS nanoparticles, 偽-tocopheryl polyethylene glycol 1000 succinate,PLGA-TPGS) using polylactide-co-glycolide-D- 偽-tocopheryl polyethylene glycol 1000 succinate,PLGA-TPGS as the carrier of glycolide copolymers and vitamin E polyethylene glycol 1000. The ligands of PLGA nanoparticles (RBG-loaded PLGA nanoparticles,RPN) were prepared by using (PLGA) as the carrier, and the quality of the two nanoparticles was evaluated and compared in vitro. Methods: RPTN and RPN, were prepared by phacoemulsification and solvent volatilization. The appearance, particle size and surface charge of RPTN and RPN, were measured by transmission electron microscope (TEM) and laser particle size analyzer respectively. Hypersil C18 column (4.6mm 脳 250 mm,5 渭 m), methanol and 0.05% glacial acetic acid solution (9:1) was used as mobile phase by RP-HPLC. The detection wavelength was 298 nm, to determine the drug loading of RBG in RPTN and RPN. Encapsulation efficiency and in vitro release. Results: the particle sizes of RPTN and RPN were 152.3 nm and 331.7 nm, respectively, and the entrapment efficiency were 18.4% and 15.1%, respectively. The cumulative release rates of RPTN and RPN were 86.7% and 72.3% respectively. Conclusion: compared with RPN, the RPTN prepared by self-made carrier has smaller particle size, larger drug loading and encapsulation efficiency, and has obvious slow-release effect and more complete release in vitro.
【作者單位】： 大連醫(yī)科大學基礎(chǔ)醫(yī)學院;大連醫(yī)科大學藥學院;大連醫(yī)科大學;
【基金】：遼寧省自然科學基金項目(編號:2015020308)
【分類號】：R94
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本文編號：2350963