Development and evaluation of Panax notoginseng saponins contained in an in situ pHtriggered gelling system for sustained ocular posterior segment drug delivery  

用于眼后段持续给药的原位pH触发凝胶系统中三七总皂苷的研制与评价

作　　者：Peng Lu Renxing Wang Yue Xing Yanquan Gao Qingqing Zhang Bin Xing Ying Zhang Changxiang Yu Xinfu Cai Qiang Shang Dereje Kebebe Jiaxin Pi Zhidong Liu 卢鹏;王仁兴;岳兴;高艳泉;张清清;邢斌;张颖;于昌祥;蔡新富;尚强;Dereje Kebebe;皮嘉欣;刘志东(天津中医药大学组分中药国家重点实验室,天津;教育部现代中药发现与制备技术工程研究中心,天津;南京中医药大学药学系,南京中医药大学附属医院,苏州;四川光大制药有限公司,彭州;彭州市抗病毒中药产业化四川工程研究中心,彭州;吉马大学卫生研究所药学院,埃塞俄比亚)

机构地区：[1]State Key Laboratory of Component-Based Chinese Medicine,Tianjin University of Traditional Chinese Medicine,Tianjin,China [2]Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique,Ministry of Education,Tianjin,China [3]Department of pharmacy,Suzhou TCM Hospital Affiliated to Nanjing University of Chinese Medicine,Suzhou,China [4]Sichuan Guangda Pharmaceutical Co.LTD,Pengzhou,China [5]Sichuan Engineering Research Center of Antiviral Traditional Chinese Medicine Industrialization,Pengzhou,China [6]School of Pharmacy,Institute of Health,Jimma University,Jimma,Ethiopia

出　　处：《Acupuncture and Herbal Medicine》2021年第2期107-121,共15页针灸和草药（英文）

摘　　要：Objective:This study aimed to lay the foundation for the research on Panax notoginseng saponins(PNS)in pH-sensitive in situ gel and the development and improvement of related preparations.Methods:We used Carbopol■940,a commonly used pH-sensitive polymer,and the thickener hydroxypropyl methylcellulose(HPMC E4M)as an ophthalmic gel matrix to prepare an ophthalmic in situ gel of PNS.In addition,formula optimization was performed by assessing gelling capability with the results of in vitro release studies.In vitro(corneal permeation,rheological,and stability)and in vivo(ocular irritation and preliminary pharmacokinetics in the vitreous)studies were also performed.Results:The results demonstrated that the in situ gelling systems containing PNS showed a sustained release of the drug,making it an ideal ocular delivery system for improving posterior ocular bioavailability.Conclusions:This study lays the foundation for the research of PNS contained in an in situ pH-triggered gel as well as the development and improvement of related preparations.It concurrently traditional Chinese medicine with a contemporary in situ gelling approach to provide new directions for the treatment of posterior ocular diseases such as diabetic retinopathy.目的:为三七总皂苷(PNS)在pH敏感型原位凝胶中的研究及相关制剂的开发和改进奠定基础。方法:我们使用Carbopol■940(一种常用的pH敏感聚合物)和增稠剂羟丙基甲基纤维素(HPMC E4M)作为眼用凝胶基质来制备PNS眼用原位凝胶。此外,通过评估凝胶能力和体外释放研究结果进行配方优化。还进行了体外(角膜渗透、流变学和稳定性)和体内(眼部刺激和玻璃体的初步药代动力学)研究。结果:研究表明,含有三七总皂苷的原位凝胶系统显示出药物的缓释性,使其成为改善眼后生物利用度的理想眼部给药系统。结论:本研究为原位pH触发凝胶中PNS的研究及相关制剂的开发和改进奠定了基础。同时,它将传统中药与现代原位凝胶技术相结合,为糖尿病视网膜病变等后眼病的治疗提供了新的方向。

关 键 词：Carbopol■940 Hydroxypropyl methylcellulose Panax notoginseng saponins pH-triggered gelling system Sustained release drug delivery 

分 类 号：R283.6[医药卫生—中药学]