Naringin-loaded polymeric micelles as buccal tablets: formulation, characterization, in vitro release, cytotoxicity and histopathology studies
Naringin-loaded polymeric micelles as buccal tablets: formulation, characterization, in vitro release, cytotoxicity and histopathology studies
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DOI：
10.1080/10837450.2020.1715427
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发表时间：
2020-01-21
影响因子：
3.4
通讯作者：
Zhang, Jiye
中科院分区：
文献类型：
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作者：
Fan, Huihui;Zhang, Peipei;Zhang, Jiye
柚皮苷（Naringin，NG）具有抗炎、抗癌、抗溃疡等多种生物学作用，但由于其溶解性差，口服溶出度低，目前尚无临床制剂。在这项研究中，为了克服这些问题，NG封装到MPEG-PCL胶束（NGM）通过使用薄膜水合方法。NMG具有典型的核壳结构，具有小粒径（23.95 ± 0.51 nm）、高载药量和包封效率。体外释放实验表明，NG包封在胶束中后，其溶出度增加。NGM在细胞毒性和组织病理学研究中是无毒的。此外，将冻干后的NGMs直接压片制成口含片时，NG在模拟口腔条件下的释放速度高于对照片，8h累积溶出度为93.13%。总之，NGMs和NGBTs代表了一种有前途的NG给药系统，具有改善当前口腔疾病治疗的潜力。
Naringin (NG) has been proved to have numerous notable biological effects, including anti-inflammatory effect, anti-cancer effect, and anti-ulcer effect, yet there are no clinical preparations of naringin due to its poor solubility and low dissolution rate after oral administration. In this study, in order to overcome these problems, NG was encapsulated into MPEG-PCL micelles (NGMs) by using a thin-film hydration method. NMGs were in a typical core-shell structure, with a mall particle size (23.95 +/- 0.51 nm), high drug loading, and encapsulation efficiency. In vitro release of NGMs indicated that the dissolution of NG was increased after being encapsulated in the micelles. NGMs were nontoxic in the cytotoxicity and histopathology studies. Furthermore, when the freeze-dried NGMs were compressed into buccal tablets (NGBTs) by direct compression, the release speed of NG under simulated oral cavity condition from NGBTs was higher than the control tablets, with the accumulated dissolution at 93.13% in 8 hours. In conclusion, NGMs and NGBTs represent a promising drug delivery system for NG, which has the potential to improve the current treatment of oral diseases.