New Method to Prepare Mitomycin C Loaded PLA-Nanoparticles with High Drug Entrapment Efficiency.
New Method to Prepare Mitomycin C Loaded PLA-Nanoparticles with High Drug Entrapment Efficiency.
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DOI：
10.1007/s11671-009-9312-z
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发表时间：
2009-04-21
影响因子：
--
通讯作者：
Zhang Q
中科院分区：
文献类型：
--
作者：
Hou Z;Wei H;Wang Q;Sun Q;Zhou C;Zhan C;Tang X;Zhang Q
经典的用于将水溶性丝裂霉素C（MMC）包封在PLA纳米颗粒中的双乳液溶剂扩散技术由于药物快速分配到外部水相而遭受低包封效率。本文采用一种新的单乳化溶剂挥发法制备了MMC载聚乳酸纳米粒，其中大豆磷脂酰胆碱（SPC）通过与MMC形成复合物来改善MMC的脂溶性。在单因素实验的基础上，采用正交设计法考察了聚乳酸分子量、聚乳酸与SPC的质量比、MMC与SPC的质量比、油相与水相的体积比4个主要影响因素对药物包封率的影响。在pH 7.2的PBS中在37 °C下进行药物释放研究，使用UV/维斯光谱仪在365 nm下进行药物分析。以经典方法制备的MMC-PLA为对照。在优化条件下制备的MMC-SPC-PLA纳米粒粒径均匀（594 nm），药物包封率高达94.8%，而PLA-MMC微粒粒径为6.44 μm，药物包封率为34.5%。MMC的释放呈双相性，即先有突释效应，然后是30天的累积释放，PLA-MMC-SPC纳米粒的累积释放率为50.17%，PLA-MMC颗粒的累积释放率为74.1%。对复合物的红外光谱分析表明，复合物的高脂溶性可能是由于复合物形成过程中MMC与SPC之间存在弱的物理相互作用。结果表明，与传统方法相比，该方法具有粒径小、粒径分布均匀、包封率高、药物缓释时间长等优点。
The classical utilized double emulsion solvent diffusion technique for encapsulating water soluble Mitomycin C (MMC) in PLA nanoparticles suffers from low encapsulation efficiency because of the drug rapid partitioning to the external aqueous phase. In this paper, MMC loaded PLA nanoparticles were prepared by a new single emulsion solvent evaporation method, in which soybean phosphatidylcholine (SPC) was employed to improve the liposolubility of MMC by formation of MMC–SPC complex. Four main influential factors based on the results of a single-factor test, namely, PLA molecular weight, ratio of PLA to SPC (wt/wt) and MMC to SPC (wt/wt), volume ratio of oil phase to water phase, were evaluated using an orthogonal design with respect to drug entrapment efficiency. The drug release study was performed in pH 7.2 PBS at 37 °C with drug analysis using UV/vis spectrometer at 365 nm. MMC–PLA particles prepared by classical method were used as comparison. The formulated MMC–SPC–PLA nanoparticles under optimized condition are found to be relatively uniform in size (594 nm) with up to 94.8% of drug entrapment efficiency compared to 6.44 μm of PLA–MMC microparticles with 34.5% of drug entrapment efficiency. The release of MMC shows biphasic with an initial burst effect, followed by a cumulated drug release over 30 days is 50.17% for PLA–MMC–SPC nanoparticles, and 74.1% for PLA–MMC particles. The IR analysis of MMC–SPC complex shows that their high liposolubility may be attributed to some weak physical interaction between MMC and SPC during the formation of the complex. It is concluded that the new method is advantageous in terms of smaller size, lower size distribution, higher encapsulation yield, and longer sustained drug release in comparison to classical method.
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