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用于曲安奈德眼部递药的聚合物胶束：在兔眼炎性模型中的制备和评价。

Polymeric micelles for the ocular delivery of triamcinolone acetonide: preparation and evaluation in a rabbit ocular inflammatory model.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, South Valley University, Qena, Egypt.

Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt.

出版信息

Drug Deliv. 2020 Dec;27(1):1115-1124. doi: 10.1080/10717544.2020.1797241.

DOI:10.1080/10717544.2020.1797241
PMID:32720545
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7470058/
Abstract

The aim of this study was to prepare triamcinolone acetonide (TA)-loaded poly(ethylene glycol)--poly(ε-caprolactone) (PEG--PCL) and poly(ethylene glycol)--poly(lactic acid) (PEG--PLA) micelles as a potential treatment of ocular inflammation. The micelles were evaluated for particle size, drug loading capacity and drug release kinetics. Selected micellar formulations were dispersed into chitosan hydrogel and their anti-inflammatory properties were tested in rabbits using a carrageenan-induced ocular inflammatory model. Particle size ranged from 59.44 ± 0.15 to 64.26 ± 0.55 nm for PEG--PCL and from 136.10 ± 1.57 to 176.80 ± 2.25 nm for PEG--PLA micelles, respectively. The drug loading capacity was in the range of 6-12% and 15-25% for PEG--PCL and PEG--PLA micelles, respectively and was dependent on the drug/polymer weight ratio. TA aqueous solubility was increased by 5- and 10-fold after loading into PEG--PCL and PEG--PLA micelles at a polymer concentration as low as 0.5 mg/mL, respectively. PEG--PLA micelles suspended in chitosan hydrogel were able to sustain the drug release where only 42.8 ± 1.6% drug was released in one week. TA/PEG--PLA micelles suspended in chitosan hydrogel had better anti-inflammatory effects compared with the plain drug hydrogel or the drug micellar solution. Complete disappearance of the corneal inflammatory changes was observed for the micellar hydrogel. These results confirm the potential of PEG--PLA micelles suspended in chitosan hydrogel to enhance the anti-inflammatory properties of triamcinolone acetonide.

摘要

本研究旨在制备曲安奈德（TA）负载的聚乙二醇-聚（ε-己内酯）（PEG-PCL）和聚乙二醇-聚乳酸（PEG-PLA）胶束，作为眼部炎症的潜在治疗方法。评估了胶束的粒径、载药量和药物释放动力学。选择的胶束制剂分散在壳聚糖水凝胶中，并在兔中使用角叉菜胶诱导的眼内炎症模型测试其抗炎特性。PEG-PCL 胶束的粒径范围为 59.44±0.15 至 64.26±0.55nm，PEG-PLA 胶束的粒径范围为 136.10±1.57 至 176.80±2.25nm。载药量范围分别为 6-12%和 15-25%，取决于药物/聚合物的重量比。TA 的水溶解度在低至 0.5mg/mL 的聚合物浓度下分别提高了 5 倍和 10 倍，负载到 PEG-PCL 和 PEG-PLA 胶束中。悬浮在壳聚糖水凝胶中的 PEG-PLA 胶束能够持续释放药物，其中仅在一周内释放了 42.8±1.6%的药物。悬浮在壳聚糖水凝胶中的 TA/PEG-PLA 胶束与普通药物水凝胶或药物胶束溶液相比具有更好的抗炎效果。胶束水凝胶可使角膜炎症变化完全消失。这些结果证实了悬浮在壳聚糖水凝胶中的 PEG-PLA 胶束增强曲安奈德抗炎特性的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec7b/7470058/6ca8d0655835/IDRD_A_1797241_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec7b/7470058/48fe6c695a30/IDRD_A_1797241_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec7b/7470058/222bba584e39/IDRD_A_1797241_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec7b/7470058/6e443dd6f86b/IDRD_A_1797241_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec7b/7470058/1c91f673b757/IDRD_A_1797241_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec7b/7470058/6ca8d0655835/IDRD_A_1797241_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec7b/7470058/48fe6c695a30/IDRD_A_1797241_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec7b/7470058/222bba584e39/IDRD_A_1797241_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec7b/7470058/6e443dd6f86b/IDRD_A_1797241_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec7b/7470058/1c91f673b757/IDRD_A_1797241_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec7b/7470058/6ca8d0655835/IDRD_A_1797241_F0005_C.jpg

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