Saxena Vishal, Sadoqi Mostafa, Shao Jun
Department of Pharmacy and Administrative Sciences, College of Pharmacy and Allied Health Professions, St. John's University, 8000 Utopia Parkway, Jamaica, NY 11439, USA.
Int J Pharm. 2004 Jul 8;278(2):293-301. doi: 10.1016/j.ijpharm.2004.03.032.
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).
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.
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).
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.
本研究的目的是使用可生物降解聚合物聚(DL-乳酸-共-乙醇酸)(PLGA)制备负载吲哚菁绿(ICG)的可生物降解纳米颗粒。
采用改良的自发乳化溶剂扩散法制备包载ICG的PLGA纳米颗粒。为优化纳米颗粒制剂,研究了ICG类型、ICG用量和聚合物等制剂参数的影响。测定了纳米颗粒中ICG的包封率、纳米颗粒大小和zeta电位。通过原子力显微镜(AFM)进行表面表征,并测定ICG从纳米颗粒中的释放情况。
所有PLGA纳米颗粒制剂的平均直径在300-410nm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表现出更高的包封效率。所有负载吲哚菁绿的纳米颗粒制剂的纳米颗粒ICG含量几乎相似,并且随着聚合物用量的增加ICG包封率增加。当制剂中ICG:PLGA重量比达到1:800时,ICG包封率达到74%。AFM图像表明纳米颗粒几乎呈球形,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(在8小时内),随后是缓慢阶段释放约2%的ICG(在接下来的16小时内)。
制备了负载ICG的PLGA纳米颗粒并优化了制剂。制剂中聚合物用量的增加导致更高的ICG包封率。形成的纳米颗粒呈球形且表面多孔,并表现出基于整体基质系统的特征性释放模式。