壳聚糖微粒载药穿心莲提取物关键参数的筛选

Melissa Yushan Ng, R. Hasham, R. Sabtu, M. Idris, Illani Abdul Rahman
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摘要

穿心莲(Andrographis paniculata)是马来西亚常见的药用植物。然而,阻碍其临床价值的主要挑战是其在水环境中的低生物利用度和溶解度,这可以通过将其纳入纳米载体系统来改善。因此,本研究旨在筛选影响AP萃取物负载壳聚糖微颗粒开发的关键因素。9种配方(编码为F1至F9)在不同的壳聚糖与三聚磷酸盐(TPP)质量比(2:1,4:1和6:1)和反应时间(30,60和90分钟)下使用单因素一次(OFAT)技术进行测试,并通过其粒径,多分散指数(PDI)和包封效率(EE)进行表征。进一步对最佳配方进行ζ电位(ζ-电位)、形貌和稳定性表征。首次筛选发现F2为最佳配方,其粒径为0.595±0.014 μm, PDI为0.284±0.011,EE为81.18±5.53%。进一步测试表明,该配方的ζ-电位为6.4±1.51 mV,分散的微粒子呈球形,表面光滑。微颗粒在4°C下也很稳定,14天后大小变化很小。综上所述,这些结果表明,将AP提取物包埋在壳聚糖- tpp微颗粒中具有良好的特性和稳定性,可以进一步研究将AP作为靶向部位递送治疗活性的一种形式。
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Screening of Critical Variables of Andrographis paniculata Extract Loaded onto Chitosan Microparticles
Andrographis paniculata (AP) is a medicinal plant commonly found in Malaysia. However, the main challenges hindering its clinical values is its low bioavailability and solubility in aqueous environment which can be improved by incorporating it into a nanocarrier system. Therefore, this study was conducted to screen the critical variables involved in the development of AP extract-loaded chitosan microparticles. Nine formulations (coded as F1 to F9) at varying chitosan-to-tripolyphosphate (TPP) mass ratio (2:1, 4:1, and 6:1) and reaction time (30, 60, and 90 minutes) were tested utilizing the onefactor-at-a-time (OFAT) technique and characterized by means of their particle size, polydispersity index (PDI), and encapsulation efficiency (EE). The best formulation was further characterized for its zeta potential (ζ-potential), morphology, and stability. F2 was discovered as the best formulation in the first screening with a particle size of 0.595 ± 0.014 μm, PDI of 0.284 ± 0.011, and EE of 81.18 ± 5.53%. Further testing on the formulation revealed a ζ-potential of 6.4 ±1.51 mV with a spherical and smooth-surface microparticles in dispersion. The microparticles were also stable at 4 °C with minimal change in size after 14 days. In conclusion, these results show that entrapment of AP extract into chitosan-TPP microparticles were achievable at good characteristics and stability and could be further studied as a form for delivering therapeutic activities of AP at targeted site.
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