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非诺贝特/随机甲基化 β-环糊精包载入羟丙甲纤维素 RL100 纳米粒的眼部给药系统研究。

Development of Fenofibrate/Randomly Methylated β-Cyclodextrin-Loaded Eudragit RL 100 Nanoparticles for Ocular Delivery.

机构信息

Faculty of Pharmaceutical Sciences, Chulalongkorn University, 254 Phyathai Road, Pathumwan, Bangkok 10330, Thailand.

Faculty of Pharmacy, Thammasat University, 99 Moo 18 Paholyothin Road, Klong Luang, Rangsit 12120, Pathum Thani, Thailand.

出版信息

Molecules. 2022 Jul 25;27(15):4755. doi: 10.3390/molecules27154755.

DOI:10.3390/molecules27154755
PMID:35897940
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9370055/
Abstract

Fenofibrate (FE) has been shown to markedly reduce the progression of diabetic retinopathy and age-related macular degeneration in clinical trials and animal models. Owing to the limited aqueous solubility of FE, it may hamper ocular bioavailability and result in low efficiency to treat such diseases. To enhance the solubility of FE, water-soluble FE/cyclodextrin (CD) complex formation was determined by a phase-solubility technique. Randomly methylated-β-CD (RMβCD) exhibited the best solubility and the highest complexation efficiency (CE) for FE. Additionally, water-soluble polymers (i.e., hydroxypropyl methyl cellulose and polyvinyl alcohol [PVA]) enhanced the solubility of FE/RMβCD complexes. Solid- and solution-state characterizations were performed to elucidate and confirm the formation of inclusion FE/RMβCD complex. FE-loaded Eudragit nanoparticle (EuNP) dispersions and suspensions were developed. The physicochemical properties (i.e., pH, osmolality, viscosity, particle size, size distribution, and zeta potential) were within acceptable ranges. Moreover, in vitro mucoadhesion, in vitro release, and in vitro permeation studies revealed that the FE-loaded EuNP eye drop suspensions had excellent mucoadhesive properties and sustained FE release. The hemolytic activity, hen's egg test on chorioallantoic membrane assay, and cytotoxicity test showed that the FE formulations had low hemolytic activity, were cytocompatible, and were moderately irritable to the eyes. In conclusion, PVA-stabilized FE/RMβCD-loaded EuNP eye drop suspensions were successfully developed, warranting further in vivo testing.

摘要

非诺贝特（FE）已在临床试验和动物模型中显示出可显著降低糖尿病视网膜病变和年龄相关性黄斑变性的进展。由于 FE 的水溶性有限，它可能会阻碍眼部生物利用度，并导致治疗这些疾病的效率低下。为了提高 FE 的溶解度，采用相溶解度技术确定了水溶性 FE/环糊精（CD）络合物的形成。随机甲基化-β-CD（RMβCD）对 FE 表现出最佳的溶解度和最高的络合效率（CE）。此外，水溶性聚合物（即羟丙基甲基纤维素和聚乙烯醇[PVA]）可提高 FE/RMβCD 配合物的溶解度。进行了固相与溶液状态的表征，以阐明并确认包合 FE/RMβCD 配合物的形成。制备了载 FE 的乙基纤维素纳米颗粒（EuNP）分散体和混悬液。理化性质（即 pH 值、渗透压、粘度、粒径、粒径分布和zeta 电位）均在可接受范围内。此外，体外黏膜黏附性、体外释放和体外渗透研究表明，载 FE 的 EuNP 滴眼混悬剂具有优异的黏膜黏附性和持续的 FE 释放。溶血活性、鸡胚绒毛尿囊膜试验和细胞毒性试验表明，FE 制剂的溶血活性低、细胞相容性好，对眼睛中度刺激性。总之，成功开发了 PVA 稳定的载 FE/RMβCD-EuNP 滴眼混悬剂，值得进一步进行体内试验。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/172d63819256/molecules-27-04755-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/ed147b894385/molecules-27-04755-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/57d314e158dd/molecules-27-04755-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/fedf546abbba/molecules-27-04755-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/4976ac8fd9a7/molecules-27-04755-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/7e6ac52c6a66/molecules-27-04755-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/c6bf70d177d2/molecules-27-04755-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/b94eb2580b1a/molecules-27-04755-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/1fb5fe52c85a/molecules-27-04755-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/7eeff487d3b3/molecules-27-04755-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/172d63819256/molecules-27-04755-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/ed147b894385/molecules-27-04755-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/57d314e158dd/molecules-27-04755-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/fedf546abbba/molecules-27-04755-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/4976ac8fd9a7/molecules-27-04755-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/7e6ac52c6a66/molecules-27-04755-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/c6bf70d177d2/molecules-27-04755-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/b94eb2580b1a/molecules-27-04755-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/1fb5fe52c85a/molecules-27-04755-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/7eeff487d3b3/molecules-27-04755-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9844/9370055/172d63819256/molecules-27-04755-g010.jpg

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