摘要
以聚乙二醇-聚乳酸-聚乙醇酸嵌段共聚物(PEG-PLGA)为囊材,添加脱镁叶绿酸作为光敏剂,采用复乳法制备了光响应的眼镜蛇神经毒素纳米囊。以纳米囊的包封率、载药量和粒径为指标,采用单因素法对纳米囊的制备条件进行优化;以差示量热扫描分析其热流变性能,并以累积释药量研究其光控释行为。优化的PEGPLGA、眼镜蛇神经毒素及光敏剂脱镁叶绿酸质量配比为40∶12.5∶1,获得的纳米囊包封率为72.3%±3.6%,载药量为15.1%±1.3%,平均粒径为(862±23)nm,电位为(-46.5±3.8)m V,呈紧密球形,光敏剂分布在囊壳;在650 nm半导体激光照射30 min,体外释放明显加快。该纳米囊在不光照时具有增强药物稳定和缓释作用,而红光可促进药物释放,因而可实现光控靶向。
The cobra neurotoxin （CNT） nanocapsule with photoresponse performance was prepared via double emulsion method by using polyethylene glycol-polylactic acid-polyglycolic acid block copolymer （PEG-PLGA） as capsule material, pheophorbide as photosensitizer. The effect of preparation conditions on the encapsulation efficiency, drug loading and particle size of nanocapsule was investigated by single factor experiments. The thermo rheological properties of sample were studied by differential scanning calorimetry （ DSC）, and the drug release behavior was evaluated by the cumulative release amount. The results showed that when the mass ratio of PEG-PLGA, CNT and pheophorbide was 40： 12.5：1, the encapsulation efficiency of the obtained nanocapsule was 72.3% ± 3.6%, and the drug loading of the nanocapsule was 15.1% ±1.3% ,with an average particle size of （862 ±23 ） nm. The zeta potential of the nanocapsule reached （ -46. 5 ± 3. 8） inV. Additionally, the nanocapsule exhibited a tight spherical shape and pheophorbide was scattered in the outer layer of the nanocapsule. Drug release in vitro was obviously accelerated under illumination of 650 nm for 30 rain with semiconductor laser. The resulting nanocapsule can keep drug stable and slow release without illumination, but can quicken drug release under red light illumination. Thus, it can realize light-controllod drug release and targeted therapy.
出处
《精细化工》
EI
CAS
CSCD
北大核心
2017年第8期907-911,共5页
Fine Chemicals
基金
国家自然科学基金(81173646)
广州市科技计划项目(1563000123)~~
关键词
聚乙二醇-聚乳酸-聚乙醇酸嵌段共聚物
眼镜蛇神经毒素
光响应
纳米囊
光控靶向
医药与日化原料
polyethylene glycol-polylactic acid-polyglycolic acid block copolymer
cobra neurotoxin
photoresponse
nanocapsule
light-controlled targeting
drug and cosmetic materials
