Characteristics of Cholesteryl Cetyl Carbonate Liquid Crystals as Drug Delivery Systems

R. Chuealee, P. Aramwit, T. Srichana
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引用次数: 5

Abstract

A thermotropic liquid crystals of cholesteryl cetyl carbonate was investigated as a novel nanosystem for delivery of lipophilic drugs. The aims were to synthesize, characterize and develop a formulation for amphotericin B (AmB) in cholesteryl cetyl carbonate liquid crystals. Cholesteryl cetyl carbonate was synthesized and identified by thin layer chromatography (TLC), flash column chromatography, Fourier transformed infrared (FTIR) spectroscopy, mass spectrometry (MS) and Nuclear magnetic resonance spectroscopy (NMR). X-ray diffraction (XRD), transmission electron microscope (TEM), polarized light microscope and differential scanning calorimetry (DSC) were employed to characterize liquid crystals properties. Cholesteryl cetyl carbonate structure is composed of three parts; steroid planar nucleus, hydrocarbon chains and carbonate linkage between the two parts of steroid ring and hydrocarbon chain from fatty alcohol. The phase transition temperatures appeared at around 8 and 36degC and cubic-shaped formation were observed in a micrograph at room temperature. The formulations of AmB in liquid crystals after physical mixing with a sugar revealed high content uniformity and had good characteristics of dry powder forms. It caused low toxicity to red blood cells.
胆固醇-十六烷基碳酸酯液晶作为药物传递系统的特性
研究了一种热致性的碳酸胆固醇十六烷基酯液晶作为一种新型的亲脂性药物的纳米递送系统。目的是合成、表征和研制一种含胆固醇十六烷基碳酸酯液晶两性霉素B (AmB)的配方。采用薄层色谱(TLC)、闪光柱色谱(flash column chromatography)、傅里叶变换红外光谱(FTIR)、质谱(MS)和核磁共振(NMR)等方法合成了碳酸胆甾醇十六烷基酯,并对其进行了鉴定。采用x射线衍射(XRD)、透射电镜(TEM)、偏振光显微镜(偏振光显微镜)和差示扫描量热法(DSC)表征了液晶的性质。碳酸胆甾醇十六烷基结构由三部分组成;甾烷平面核、烃链和碳酸盐键之间的甾烷环和烃链的两部分来自脂肪醇。相变温度在8°c和36°c左右,室温下显微镜下观察到立方形状的相变。与糖物理混合后的AmB液晶配方具有较高的含量均匀性和良好的干粉形态特征。它对红细胞的毒性很低。
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