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Polystyrene Sulfonate Resin as an Ophthalmic Carrier for Enhanced Bioavailability of Ligustrazine Phosphate Controlled Release System

文献类型：期刊论文

作者Dong, Liyun2,3,5; Zhang, Hui2,3,5; Zhang, Guoqing2; Li, Falan2,3,5; Li, Mingwei2,3,5; Wang, Huihui2,3; Ye, Xinyue2,3,5; Ren, Xiaohong4; Zhang, Jiwen2,3,4,5; Peng, Can5
刊名JOURNAL OF PHARMACEUTICAL SCIENCES
出版日期2024-09-01
卷号113期号:9页码:2786-2794
关键词Sodium polystyrene sulfonate resin Ligustrazine phosphate Suspension Sustained-release Bioavailability
ISSN号0022-3549
DOI10.1016/j.xphs.2024.07.002
通讯作者Peng, Can(pengcan@ahtcm.edu.cn) ; Liu, Hongfei(liuhongfei@ujs.edu.cn) ; Wu, Li(wuli@simm.ac.cn)
英文摘要Topical ocular sustained-release drug delivery systems represent an effective strategy for the treatment of ocular diseases, for which a suitable carrier has yet to be sufficiently developed. Herein, an eye-compatible sodium polystyrene sulfonate resin (SPSR) was synthesized with a uniform particle size of about 3 mu m. Ligustrazine phosphate (LP) was adsorbed to SPSR by cation exchange to form LP@SPSR. LP@SPSR suspension eye drops were further developed using the combination of Carbopol 934P and xanthan gum as suspending agents. The LP@SPSR suspension showed a sustained release in vitro, which was consistent with the observed porcine corneal penetration ex vivo. Pharmacokinetics in tear fluid of rabits indicated that LP@SPSR suspension led to prolonged ocular retention of LP and a 2-fold improved the area under the drug concentration-time curve (AUC(0-t)). Pharmacokinetics in the aqueous humor of rabbits showed 2.8-fold enhancement in the AUC(0-t) compared to LP solution. The LP@SPSR suspension exhibited no cytotoxicity to human corneal epithelial cells, nor irritation was observed in rabbit eyes. Thus, the LP@SPSR suspension has been validated as a safe and sustained release system leading to enhanced ophthalmic bioavailability for treating ocular diseases. (c) 2024 American Pharmacists Association. Published by Elsevier Inc. All rights are reserved, including those for text and data mining, AI training, and similar technologies.
WOS关键词AQUEOUS FLARE ELEVATION ; ION-EXCHANGE RESINS ; DRUG-DELIVERY ; IN-VITRO ; VIVO EVALUATION ; XANTHAN GUM ; EYE DROPS ; TETRAMETHYLPYRAZINE ; FORMULATION ; SUSPENSION
资助项目National Natural Science Foundation of China[82273863]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:001311485000001
出版者ELSEVIER SCIENCE INC
源URL[http://119.78.100.183/handle/2S10ELR8/313332]  
专题中国科学院上海药物研究所
通讯作者Peng, Can; Liu, Hongfei; Wu, Li
作者单位1.Jiangsu Univ, Zhenjiang 212000, Peoples R China
2.Jiangsu Yunshi Pharmaceut Technol Co Ltd, Nantong 226133, Peoples R China
3.Yangtze Delta Drug Adv Res Inst, Nantong 226133, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201210, Peoples R China
5.Anhui Univ Chinese Med, Coll Pharm, Hefei 230012, Peoples R China
推荐引用方式
GB/T 7714		 Dong, Liyun,Zhang, Hui,Zhang, Guoqing,et al. Polystyrene Sulfonate Resin as an Ophthalmic Carrier for Enhanced Bioavailability of Ligustrazine Phosphate Controlled Release System[J]. JOURNAL OF PHARMACEUTICAL SCIENCES,2024,113(9):2786-2794.
APA Dong, Liyun.,Zhang, Hui.,Zhang, Guoqing.,Li, Falan.,Li, Mingwei.,...&Wu, Li.(2024).Polystyrene Sulfonate Resin as an Ophthalmic Carrier for Enhanced Bioavailability of Ligustrazine Phosphate Controlled Release System.JOURNAL OF PHARMACEUTICAL SCIENCES,113(9),2786-2794.
MLA Dong, Liyun,et al."Polystyrene Sulfonate Resin as an Ophthalmic Carrier for Enhanced Bioavailability of Ligustrazine Phosphate Controlled Release System".JOURNAL OF PHARMACEUTICAL SCIENCES 113.9(2024):2786-2794.

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来源：上海药物研究所

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