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基于萘非那酮的环糊精微粒治疗眼部炎症的体外和离体评价

In Vitro and Ex Vivo Evaluation of Nepafenac-Based Cyclodextrin Microparticles for Treatment of Eye Inflammation.

作者信息

Lorenzo-Veiga Blanca, Diaz-Rodriguez Patricia, Alvarez-Lorenzo Carmen, Loftsson Thorsteinn, Sigurdsson Hakon Hrafn

机构信息

Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, Iceland.

Departamento de Ingeniería Química y Tecnología Farmacéutica, Facultad de Ciencias de la Salud, Universidad de la Laguna (ULL), Campus de Anchieta, 38200 La Laguna (Tenerife), Spain.

出版信息

Nanomaterials (Basel). 2020 Apr 9;10(4):709. doi: 10.3390/nano10040709.

DOI:10.3390/nano10040709
PMID:32283583
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7221994/
Abstract

The aim of this study was to design and evaluate novel cyclodextrin (CD)-based aggregate formulations to efficiently deliver nepafenac topically to the eye structure, to treat inflammation and increase nepafenac levels in the posterior segment, thus attenuating the response of inflammatory mediators. The physicochemical properties of nine aggregate formulations containing nepafenac/γ-CD/hydroxypropyl-β (HPβ)-CD complexes as well as their rheological properties, mucoadhesion, ocular irritancy, corneal and scleral permeability, and anti-inflammatory activity were investigated in detail. The results were compared with a commercially marketed nepafenac suspension, Nevanac 3 mg/mL. All formulations showed microparticles, neutral pH, and negative zeta potential (-6 to -27 mV). They were non-irritating and nontoxic and showed high permeation through bovine sclera. Formulations containing carboxymethyl cellulose (CMC) showed greater anti-inflammatory activity, even higher than the commercial formulation, Nevanac 0.3%. The optimized formulations represent an opportunity for topical instillation of drugs to the posterior segment of the eye.

摘要

本研究的目的是设计并评估新型环糊精（CD）基聚集体制剂，以有效地将萘非那酮局部递送至眼组织，治疗炎症并提高萘非那酮在后段的水平，从而减弱炎症介质的反应。详细研究了九种含有萘非那酮/γ-环糊精/羟丙基-β（HPβ）-环糊精复合物的聚集体制剂的物理化学性质及其流变学性质、粘膜粘附性、眼刺激性、角膜和巩膜渗透性以及抗炎活性。将结果与市售的萘非那酮混悬液Nevanac 3 mg/mL进行比较。所有制剂均显示出微粒、中性pH值和负的zeta电位（-6至-27 mV）。它们无刺激性且无毒，并显示出通过牛巩膜的高渗透性。含有羧甲基纤维素（CMC）的制剂表现出更大的抗炎活性，甚至高于市售制剂Nevanac 0.3%。优化后的制剂为将药物局部滴注到眼后段提供了机会。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/544ead07d3c2/nanomaterials-10-00709-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/40ad910ababc/nanomaterials-10-00709-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/e273580b34a5/nanomaterials-10-00709-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/e19eacc27140/nanomaterials-10-00709-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/64a11b7d92fd/nanomaterials-10-00709-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/f4d0e854e262/nanomaterials-10-00709-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/5ae74cef6e6a/nanomaterials-10-00709-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/16e8614a5dd2/nanomaterials-10-00709-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/a19f4d41e41a/nanomaterials-10-00709-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/544ead07d3c2/nanomaterials-10-00709-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/40ad910ababc/nanomaterials-10-00709-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/e273580b34a5/nanomaterials-10-00709-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/e19eacc27140/nanomaterials-10-00709-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/64a11b7d92fd/nanomaterials-10-00709-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/f4d0e854e262/nanomaterials-10-00709-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/5ae74cef6e6a/nanomaterials-10-00709-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/16e8614a5dd2/nanomaterials-10-00709-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/a19f4d41e41a/nanomaterials-10-00709-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a62/7221994/544ead07d3c2/nanomaterials-10-00709-g009.jpg

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