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制备和评价冻干脱乙酰壳聚糖纳米纤维/壳聚糖微球作为一种缓释赋形剂。

Preparation and evaluation of freeze dried surface-deacetylated chitin nanofiber/sacran pellets for use as an extended-release excipient.

机构信息

Faculty of Pharmaceutical Sciences, Sojo University, 4-22-1 Ikeda, Nishi-ku, Kumamoto 860-0082, Japan.

Graduate School of Engineering, Tottori University, Tottori 680-8533, Japan.

出版信息

Int J Biol Macromol. 2019 Mar 1;124:888-894. doi: 10.1016/j.ijbiomac.2018.11.225. Epub 2018 Nov 26.

Abstract

Pelleted preparations were formulated from sacran (Sac), an anionic, sulfated, carboxyl-containing polysaccharide, which is extracted from the Japanese indigenous cyanobacterium Aphanothece sacrum, and surface-deacetylated chitin nanofibers (SDACNF). The use of this material as an extended-release excipient for tetrahydrocurcumin (THC), a model drug that is used to treat wounds via its radical scavenging ability was examined. The THC used in the study was complexed with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), which increases its water solubility. The radical scavenging activity of the THC/HP-β-CD complex (molar ratio of 1:1) was significantly higher than the values for SDACNF or Sac alone. The rate of release of THC from the Sac/SDACNF pellets containing the THC/HP-β-CD complex decreased with increasing Sac content in the pellet, suggesting that Sac/SDACNF (1:1) and Sac alone pellets function as extended-release excipients for THC. The findings reported here indicate that this can be attributed to the ability of the Sac component to retain fluids, thus extending the effects of the drug. In view of the above experimental outcomes, i.e. wound healing efficacy, fluid absorption, retention and the extended drug release of the system indicates that this preparation, in the appropriate ratios, has the potential for use as a controlled-release drug in wound healing.

摘要

将硫酸化、含羧基的阴离子多糖 sacran(Sac)和经过表面脱乙酰化的壳聚糖纳米纤维(SDACNF)制成微丸制剂。该材料可用作四氢姜黄素(THC)的控释赋形剂,THC 是一种治疗伤口的模型药物,具有清除自由基的能力。研究中使用的 THC 与 2-羟丙基-β-环糊精(HP-β-CD)形成复合物,从而增加了其水溶性。THC/HP-β-CD 复合物(摩尔比为 1:1)的自由基清除活性明显高于 SDACNF 或 Sac 单独使用时的活性。载有 THC/HP-β-CD 复合物的 Sac/SDACNF 微丸中 THC 的释放速率随微丸中 Sac 含量的增加而降低,表明 Sac/SDACNF(1:1)和 Sac 单独的微丸可作为 THC 的控释赋形剂。这里报道的研究结果表明,这归因于 Sac 成分保留液体的能力,从而延长了药物的作用。鉴于上述实验结果,即伤口愈合效果、液体吸收、保留和系统的延长药物释放表明,该制剂在适当的比例下,有可能作为一种用于伤口愈合的控释药物。

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