Page 128 - 201811

第 35 卷第 11 期 精 细 化 工 Vol.35, No.11
2018 年 11 月 FINE CHEMICALS Nov. 2018

医药与日化原料
靶向光敏剂 NaYF ∶Yb,Tm@NaGdF ∶Yb@TiO @
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PEI-PAA-FA 的制备和性能

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毛 艳 ，梁天华 ，胡小锋 ，董孟杰 ，刘振锋 ，宫培军
（1. 浙江师范大学 “先进催化材料”教育部重点实验室，浙江 金华 321004；2. 浙江大学 医学院附属
第一医院 核医学科 PET 中心，浙江 杭州 310003）
摘要：采用水解法用 TiO 2 包覆上转换纳米粒子 NaYF 4 :Yb,Tm@NaGdF 4 :Yb，然后修饰聚乙烯亚胺（PEI）和聚丙
烯酸（PAA）并偶联叶酸（FA），制备了叶酸受体靶向纳米光敏剂（NaYF 4 ∶Yb,Tm@NaGdF 4 ∶Yb@TiO 2 @PEI-
PAA-FA）。借助 XRD 和 TEM 表征 NaYF 4 ∶Yb,Tm@NaGdF 4 ∶Yb@TiO 2 的物相和形貌，FTIR 和 Zeta 电位证实
有机成分的成功修饰，并测试了产物的上转换发光光谱。结果表明：在 980 nm 近红外光（NIR）下，纳米光敏
剂存在下的 1,3-二苯基异苯并呋喃溶液吸收光谱的降低证明了单线态氧的产生。此外，纳米光敏剂可以载带阿
霉素（DOX），最大载药率为 50.8%，包封率为 84.7%。载药后的纳米光敏剂中 DOX 释放对介质具有 pH 响应
性，在 NIR 照射的酸性介质（pH=5.0）中 12 h 的累积缓释率为 38.1%，远高于中性介质（pH=7.4）的 10.4%。
关键词：上转换纳米粒子；二氧化钛；阿霉素；叶酸；药物缓释；光动力治疗；化疗；医药原料
中图分类号：TQ427.7; O648 文献标识码：A 文章编号：1003-5214 (2018) 11-1914-07

Preparation and Properties of Targeting Photosensitizer

NaYF 4∶Yb,Tm@NaGdF 4∶Yb@TiO 2@PEI-PAA-FA

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MAO Yan , LIANG Tian-hua , HU Xiao-feng , DONG Meng-jie ,
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LIU Zhen-feng , GONG Pei-jun
（1. Key Laboratory of the Ministry of Education for Advanced Catalysis Materials, Zhejiang Normal University,
Jinhua 321004, Zhejiang, China; 2. PET Center, Department of Nuclear Medicine, the First Affiliated Hospital, College
of Medicine, Zhejiang University, Hangzhou 310003, Zhejiang, China）
Abstract: Folate receptor-targeted nanophotosensitizer (NaYF 4 ∶Yb,Tm@NaGdF 4 ∶Yb@TiO 2 @PEI-PAA-FA)
was prepared by coating TiO 2 on the upconversion nanoparticles NaYF 4∶Yb,Tm@NaGdF 4∶Yb via a
hydrolysis method, followed by modification with polyethyleneimine (PEI) and polyacrylic acid (PAA) and
subsequent conjugation of folic acid (FA). XRD and TEM were used to characterize the crystal structure
and morphology of the inorganic components of the nanophotosensitizer. FTIR and Zeta potential were
used to verify the binding of these organic components. Upconversion luminescence spectra of the samples
were also measured. The decrease in the absorbance of 1,3-diphenylisobenzofuran solution in the presence
of the nanophotosensitizer under 980 nm near-infrared (NIR) laser irradiation indicated the singlet oxygen
was produced from the nanophotosensitizer. Besides, the photosensitizer could carry doxorubicin (DOX),
the maximum drug loading efficiency was 50.8% and the encapsulation efficiency was 84.7%. The DOX
release from the nanophotosensitizer was sensitive to the pH value of the buffer. As the DOX-loaded
nanophotosensitizer was suspended in an acidic buffer of pH=5.0 and exposed to NIR laser irradiation for 12 h,
the cumulative release of DOX was 38.1%, much higher than that obtained from a neutral buffer (pH=7.4),
which was 10.4%.

收稿日期：2017-11-07; 定用日期：2018-02-12; DOI: 10.13550/j.jxhg.20170908
基金项目：浙江省公益技术应用研究计划项目（2016C31014）；浙江省自然科学基金（LY16H180002）；浙江师范大学“先进催化材料”
教育部重点实验室和“固体表面反应化学”浙江省重点实验室开放课题基金（2017-15）；国家级大学生创新创业训练计划（201710345018）
作者简介：毛 艳（1992—），女，硕士生。联系人：宫培军（1978—），男，副教授，E-mail：skygpj@zjnu.cn。