董聪, 纪忠娟, 司佳, 韩晓冉, 刘晴, 程祥, 李海燕, 金向群. 花粉载药体系的润湿性调控、制备工艺优化与性能表征J. 药学学报, 2025, 60(6): 1911-1919. DOI: 10.16438/j.0513-4870.2024-1218
引用本文: 董聪, 纪忠娟, 司佳, 韩晓冉, 刘晴, 程祥, 李海燕, 金向群. 花粉载药体系的润湿性调控、制备工艺优化与性能表征J. 药学学报, 2025, 60(6): 1911-1919. DOI: 10.16438/j.0513-4870.2024-1218
DONG Cong, JI Zhong-juan, SI Jia, HAN Xiao-ran, LIU Qing, CHENG Xiang, LI Hai-yan, JIN Xiang-qun. Wettability regulation, preparation process optimization and performance characterization of pollen drug delivery systemsJ. Acta Pharmaceutica Sinica, 2025, 60(6): 1911-1919. DOI: 10.16438/j.0513-4870.2024-1218
Citation: DONG Cong, JI Zhong-juan, SI Jia, HAN Xiao-ran, LIU Qing, CHENG Xiang, LI Hai-yan, JIN Xiang-qun. Wettability regulation, preparation process optimization and performance characterization of pollen drug delivery systemsJ. Acta Pharmaceutica Sinica, 2025, 60(6): 1911-1919. DOI: 10.16438/j.0513-4870.2024-1218

花粉载药体系的润湿性调控、制备工艺优化与性能表征

Wettability regulation, preparation process optimization and performance characterization of pollen drug delivery systems

  • 摘要: 探究经磷酸处理后花粉在不同试剂处理后其润湿性的转变, 对润湿性转变后的花粉孢粉素载药体系的制备方法进行优化找到最佳碱处理条件, 并对其结构及表面形貌进行表征。本研究先对原花粉以及酸解后花粉润湿性进行分析, 借助接触角测试仪测量经各试剂处理后的酸解后花粉的水接触角, 并对可转变花粉润湿性的碱处理条件进行单因素试验, 采用响应面法并以甘油完全吸收时间为响应值探究影响亲水性花粉孢粉素载体制备条件优化, 并进行工艺参数验证及验证性试验, 最后通过傅里叶变换红外光谱、扫描电子显微镜对孢粉素进行表征。接触角测试表明酸解后花粉水接触角为135.1°, 经NaOH处理后转变为16°, 甘油接触角由140.8°转变为9.6°, 经单因素试验及响应面法优化处理得出最佳碱处理工艺并根据实际实验过程得到最终的优化条件为NaOH体积为105 mL即花粉体积的15倍量, NaOH浓度为1.5 mol·L-1, 搅拌时间为18 h, 搅拌温度为85 ℃。在此条件下分别进行党参花粉和荷花花粉的3次平行实验验证, 其中党参花粉结果平均值为58 s, 荷花花粉结果平均值为49 s, 且RSD均小于5%。通过润湿性研究发现在NaOH处理后花粉孢粉素由疏水性转变为亲水性, 根据响应面优化结果显示出, 所制备的碱处理后的花粉孢粉素的甘油完全吸收时间明显缩短, 水接触角接近0°, 具有较好的亲水性, 该过程重现性好, 制备工艺稳定可靠, 理论上将更利于亲水性药物的负载。

     

    Abstract: To investigate the transformation of wettability of phosphoric acid-treated pollen after treatment with different reagents, to optimize the preparation of the wettability-transformed pollen sporopollenin carrier system to find the optimal alkali treatment conditions, and to characterize its structure and surface morphology, we first analyzed the wettability of the original pollen and the acid-dissolved pollen, measured the water contact angle of the acid-dissolved pollen treated with each reagent with the help of a contact angle tester, conducted a one-way test on the alkali treatment conditions that could transform the wettability of the pollen, explored the influence of the optimization of the conditions for the preparation of the hydrophilic pollen sporopollenin carriers by using a response surface methodology and the glycerol absorption time as the response value, and carried out a validation and verification test on the process parameters. The process parameters were verified and validation tests were conducted, and finally the sporopollenin was characterized by FTIR and SEM. The contact angle test showed that the water contact angle of pollen after acid digestion was 135.1°, which was changed to 16° after NaOH treatment, and the contact angle of glycerol was changed from 140.8° to 9.6°. The best alkali treatment process was obtained through the optimization of one-factor test and response surface method, and the final optimization conditions were obtained according to the actual experimental process: the volume of NaOH was 105 mL, i.e., 15 times the volume of pollen, and the concentration of NaOH was 1.5 mol·L-1. The stirring time was 18 h, and the stirring temperature was 85 ℃. Under these conditions, three parallel experiments were carried out to verify the wettability of Codonopsis pollen and Lotus pollen respectively, in which the average value of Codonopsis pollen results was 58 s, and the average value of Lotus pollen results was 49 s, and the RSD was less than 5%. The wettability study revealed that pollen sporopollenin changed from hydrophobicity to hydrophilicity after NaOH treatment, and according to the results of response surface optimization, the prepared alkali-treated pollen sporopollenin showed a significantly shorter time for complete glycerol absorption and a better hydrophilicity with a water contact angle of close to 0°, which is a reproducible process and a stable and reliable preparative process, and theoretically, will be more conducive to the loading of hydrophilic drugs.

     

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