Cheng Kuo-Chung, Hu Chia-Chien, Li Chih-Ying, Li Shih-Chi, Cai Zhi-Wei, Wei Yang, Don Trong-Ming
Department of Chemical Engineering and Biotechnology, National Taipei University of Technology, Taipei 10608, Taiwan.
Department of Chemical and Materials Engineering, Tamkang University, New Taipei City 251301, Taiwan.
Polymers (Basel). 2022 Oct 26;14(21):4538. doi: 10.3390/polym14214538.
Pectin/chitosan hydrochloride (CHC) particles containing theophylline were prepared by a spray-drying apparatus coupled with a continuous feeding ultrasonic atomizer and a heating column. The formation of the submicron particles was investigated at various compositions of pectin solutions added with a chitosan hydrochloride or calcium chloride solution as a crosslinking agent. Scanning electron microscopic (SEM) images showed the pectin/chitosan hydrochloride particles had spherical and smooth surfaces. Depending on the feeding concentrations, the produced particles had diameters in the range of 300 to 800 nm with a narrow size distribution. Furthermore, the theophylline (TH)-loaded pectin/CHC particles were also prepared by the same apparatus. The TH release from the submicron particles in phosphate-buffered saline at 37 °C was monitored in real-time by a UV-Visible spectrophotometer. The Ritger-Peppas model could well describe the TH release profiles. All the diffusional exponents () of the release systems were greater than 0.7; thus, the transport mechanism was not a simple Fickian diffusion. Particularly, the value was 1.14 for the TH-loaded particles at a pectin/CHC weight ratio of 5/2, which was very close to the zero-order drug delivery ( = 1). Therefore, the constant drug-release rate could be achieved by using the spray-dried pectin/CHC particles as the drug carrier.
采用配备连续进料超声雾化器和加热柱的喷雾干燥装置制备了含茶碱的果胶/壳聚糖盐酸盐（CHC）颗粒。在添加壳聚糖盐酸盐或氯化钙溶液作为交联剂的不同果胶溶液组成下，研究了亚微米颗粒的形成情况。扫描电子显微镜（SEM）图像显示，果胶/壳聚糖盐酸盐颗粒表面呈球形且光滑。根据进料浓度，所制备颗粒的直径范围为300至800 nm，粒径分布较窄。此外，还通过同一装置制备了负载茶碱（TH）的果胶/CHC颗粒。在37℃下，用紫外可见分光光度计实时监测亚微米颗粒在磷酸盐缓冲盐水中的TH释放情况。Ritger-Peppas模型能够很好地描述TH释放曲线。所有释放系统的扩散指数（）均大于0.7；因此，传输机制不是简单的菲克扩散。特别是，果胶/CHC重量比为5/2时，负载TH的颗粒的 值为1.14，非常接近零级药物递送（ = 1）。因此，通过使用喷雾干燥的果胶/CHC颗粒作为药物载体，可以实现恒定的药物释放速率。
