Fabrication of anti-inflammatory nano eye-drops composed of dexamethasone prodrugs

Fabrication of anti-inflammatory nano eye-drops composed of dexamethasone prodrugs
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地塞米松前药抗炎纳米滴眼液的研制

DOI:
10.1080/15421406.2023.2180212
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发表时间:
2023
影响因子:
0.7
通讯作者:
Kasai Hitoshi
Kasai Hitoshi
中科院分区:
化学4区
文献类型:
--
作者:
Tanita Keita;Iijima Mai;Koseki Yoshitaka;Sato Kota;Nakazawa Toru;Kasai Hitoshi

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药物分子不能适当地渗透到角膜,但纳米滴眼液可以用来改善眼内药物的渗透。我们用不同长度的碳链连接物在抗炎药中合成了地塞米松的同二聚体前药,建立了一种新的前药,并制备了相应的地塞米松纳米粒。较长的碳链连接物减小了纳米颗粒的尺寸,并增加了它们的耐水解性。制备的纳米粒渗透到大鼠眼内,然后水解释放药物。因此,纳米滴眼液似乎是开发眼内高渗透性抗炎药物的一种有前途的解决方案。
Drug molecules cannot suitably permeate the cornea, but nano eye-drops may be used to improve intraocular drug permeation. We synthesized a homodimeric prodrug of dexamethasone in an anti-inflammatory drug with carbon chain linkers of varying lengths to establish a new prodrug and fabricated the corresponding dexamethasone nanoparticles. A longer carbon chain linker reduces the size of the nanoparticles and increases their hydrolysis resistance. The fabricated nanoparticles permeate into rat eye and then hydrolyze to release the drug. Thus, nano eye-drops seem to be a promising solution for the development of anti-inflammatory drugs with high intraocular permeation.
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