Department of Pharmaceutics, Chandigarh College of Pharmacy, Mohali, (Punjab) 140307, India.
Department of Pharmaceutical Sciences and Technology, Maharaja Ranjit Singh Punjab Technical University, Bathinda, Punjab, India.
Int J Biol Macromol. 2019 Feb 1;122:1-9. doi: 10.1016/j.ijbiomac.2018.10.155. Epub 2018 Oct 24.
In the present investigation, sulfated derivatives of Okra fruit gum (OFG) with the degree of substitution (DS) ranging from 0.39 to 1.13 were synthesized using chlorosulfonic acid/pyridine (CSA/Py) reagents under the umbrella of Box-Behnken Design (BBD) of Response Surface Methodology (RSM) to optimize the reaction conditions. The extracted gum was characterized for particle size, zeta-potential, surface morphology, architectural arrangement, mechanical and rheological chattels, pharmacological properties etc. The optimal reaction conditions of sOFG (sulfated okra fruit gum) were included ratio of CSA/Py, 0.28; reaction time, 3.05 h and reaction temperature, 58.74 °C. A high DS of 1.004 was procured at optimized conditions that was analogous to the predicted value. The sOFG was investigated to be advanced over the immensely used polysaccharide sodium alginate in mechanical and rheological attributes. Also, pharmacological properties including anticoagulant and antimicrobial property of sOFG were superior as compared to OFG. In conclusion, sulfation of OFG under the shed of BBD offered a superior DS that could be further explored for wide usage as pharmaceutical excipient for designing health care products.
在本研究中，使用氯磺酸/吡啶（CSA/Py）试剂，通过响应面法（RSM）的 Box-Behnken 设计（BBD），合成了取代度（DS）范围为 0.39 至 1.13 的黄秋葵胶的硫酸化衍生物。提取的胶进行了粒径、Zeta 电位、表面形态、结构排列、力学和流变学特性、药理学特性等特性的表征。sOFG（硫酸化黄秋葵胶）的最佳反应条件包括 CSA/Py 比为 0.28；反应时间为 3.05 小时，反应温度为 58.74°C。在优化条件下获得了高达 1.004 的高 DS，与预测值相似。与广泛使用的多糖海藻酸钠相比，sOFG 在力学和流变学特性方面具有优势。此外，sOFG 的药理学特性，包括抗凝和抗菌特性，优于 OFG。总之，BBD 下的 OFG 硫酸化提供了更高的 DS，可以进一步探索作为设计保健产品的药物赋形剂的广泛用途。
