开发并表征了一种包含可溶性和不溶性模型药物的共聚胶束。
Development and characterization of a copolymeric micelle containing soluble and insoluble model drugs.
机构信息
Department of Pharmaceutics, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Yazd, Iran.
Department of Medicinal Chemistry, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Yazd, Iran.
出版信息
PLoS One. 2023 May 25;18(5):e0286251. doi: 10.1371/journal.pone.0286251. eCollection 2023.
OBJECTIVES
Micelles are nano-sized particles with a core-shell structure that are made by natural or synthetic polymers or copolymers. The aim of this study was to develop and characterize a copolymeric micelle using two polymers loaded with hydrophilic and lipophilic drugs.
METHODS
Poly(ethylene glycol) and poly(ε-caprolactone) (PEG-PCL) were used to form a copolymeric micelle which was further loaded with either moxifloxacin or clarithromycin as hydrophilic and lipophilic drug samples, respectively. Characterization tests were done including fourier transform-infrared (FT-IR) spectroscopy, proton nuclear magnetic resonance (1H NMR) spectroscopy, encapsulation efficiency, particle size, zeta potential, polydispersity index, transmission electron microscopy, and in-vitro release test.
RESULTS
The construction of the copolymer was confirmed by the results of FT-IR and 1H NMR spectroscopy tests. The encapsulation efficiency test exhibited that loading was about 50% for twelve formulations. Particle size, zeta potential, polydispersity index, and transmission electron microscopy confirmed the formation of monodispersed, uniform, and nano-sized micelles with a few negative charges. The kinetic model of release was fitted to the Higuchi model.
CONCLUSIONS
Polymeric micelles consisting of PEG-PCL copolymer were loaded with adequate concentrations of hydrophilic (moxifloxacin) and lipophilic (clarithromycin) model drugs, with a mean particle size under 300 nm. Therefore, copolymeric micelles can be used as a suitable drug delivery system for mucous membranes and skin.
目的
胶束是由天然或合成聚合物或共聚物制成的具有核壳结构的纳米级颗粒。本研究旨在开发和表征一种由两种载有亲水性和疏水性药物的聚合物制成的胶束。
方法
使用聚乙二醇（PEG）和聚（ε-己内酯）（PCL）形成一种胶束，进一步将莫西沙星或克拉霉素分别作为亲水性和疏水性药物样品载入其中。进行了傅里叶变换红外（FT-IR）光谱、质子核磁共振（1H NMR）光谱、包封效率、粒径、zeta 电位、多分散指数、透射电子显微镜和体外释放试验等表征测试。
结果
FT-IR 和 1H NMR 光谱测试结果证实了共聚物的构建。包封效率测试表明，12 种配方的载药量约为 50%。粒径、zeta 电位、多分散指数和透射电子显微镜证实了单分散、均匀和纳米级胶束的形成，带有少量负电荷。释放动力学模型拟合到 Higuchi 模型。
结论
由 PEG-PCL 共聚物组成的聚合物胶束载有足够浓度的亲水性（莫西沙星）和疏水性（克拉霉素）模型药物，平均粒径小于 300nm。因此，胶束可以用作粘膜和皮肤的合适药物传递系统。
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