Indocyanine green-loaded biodegradable nanoparticles: preparation, physicochemical characterization and in vitro release
Indocyanine green-loaded biodegradable nanoparticles: preparation, physicochemical characterization and in vitro release
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DOI：
10.1016/j.ijpharm.2004.03.032
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发表时间：
2004-07-08
影响因子：
5.8
通讯作者：
Shao, J
中科院分区：
文献类型：
--
作者：
Saxena, V;Sadoqi, M;Shao, J
目的：本研究的目的是利用可生物降解的聚合物聚（DL - 乳酸 - 羟基乙酸）（PLGA）开发负载吲哚菁绿（ICG）的可生物降解纳米粒子。
方法：采用改良的自乳化溶剂扩散法制备包裹ICG的PLGA纳米粒子。为优化纳米粒子配方，研究了配方参数如ICG的种类、ICG的量以及聚合物的影响。测定了纳米粒子中ICG的包封率、纳米粒子大小和zeta电位。通过原子力显微镜（AFM）进行表面表征，并测定了ICG从纳米粒子中的释放情况。
结果：所有PLGA纳米粒子配方的平均直径均在300 - 410 nm范围内，多分散指数（PI）在0.01 - 0.06范围内。与吲哚菁绿碘化钠盐相比，吲哚菁绿显示出更高效的包封率。所有负载吲哚菁绿的纳米粒子配方中纳米粒子的ICG含量几乎相似，并且随着聚合物量的增加，ICG包封率增加。当配方中ICG : PLGA重量比达到1 : 800时，ICG包封率达到74%。AFM图像表明纳米粒子几乎呈球形，表面有许多孔隙。释放模式包括两个阶段，初始指数阶段释放约78%的ICG（8小时内），随后是缓慢阶段释放约2%的ICG（接下来的16小时内）。
结论：制备了负载ICG的PLGA纳米粒子并优化了配方。配方中聚合物量的增加导致更高的ICG包封率。形成的纳米粒子呈球形，表面多孔，呈现出基于整体基质系统的特征性释放模式。（C）2004 Elsevier B.V.保留所有权利。
Purpose: The objective of this study is to develop indocyanine green (ICG)-loaded biodegradable nanoparticles by using biodegradable polymer, poly(DL-lactic-co-glycolic acid) (PLGA). Method: PLGA nanoparticles entrapping ICG were prepared by a modified spontaneous emulsification solvent diffusion method. To optimize the nanoparticle formulation, the influence of formulation parameters such as types of ICG, amount of ICG and the polymer were investigated. The ICG entrapment in nanoparticles, nanoparticle size and zeta potential were determined. The surface characterization was performed by atomic force microscopy (AFM) and the release of ICG from nanoparticles was determined. Results: All PLGA nanoparticle formulations were found to have the mean diameter within the range of 300-410 nm with polydispersity index (PI) within the range of 0.01-0.06. Indocyanine green showed more efficient entrapment as compared to indocyanine green sodium iodide salt. All indocyanine,green-loaded nanoparticle formulations were found to have almost similar ICG content of nanoparticles and showed increase in ICG entrapment with increase in the amount of polymer. The ICG entrapment reached 74% when ICG: PLGA weight ratio in the formulation reached 1:800. AFM images indicated that the nanoparticles were almost spherical in shape and had numerous pores on their surfaces. The release pattern consisted of two phases, with initial exponential phase releasing about 78% of ICG (within 8 h) followed by a slow phase releasing about 2% of ICG (within next 16 h). Conclusions: ICG-loaded PLGA nanoparticles were prepared and the formulation was optimized. The increase in amount of polymer in formulation leads to higher ICG entrapment. Nanoparticles formed were spherical and had porous surfaces and exhibited the characteristic release pattern of a monolithic matrix based system. (C) 2004 Elsevier B.V. All rights reserved.