Tranexamic acid-fatty alcohol polyoxyethylene ether conjugation/PVA foam for venous sclerotherapy via vascular damage and inhibiting plasmin system.
10.1016/j.apsb.2025.03.032
- Author:
Jizhuang MA
1
;
Keda ZHANG
2
;
Wenhan LI
3
;
Yu DING
1
;
Yongfeng CHEN
1
;
Xiaoyu HUANG
1
;
Tong YU
1
;
Di SONG
1
;
Haoran NIU
1
;
Huichao XIE
2
;
Tianzhi YANG
4
;
Xiaoyun ZHAO
5
;
Xinggang YANG
1
;
Pingtian DING
2
Author Information
1. School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
2. College of Pharmacy, Shenzhen Technology University, Shenzhen 518118, China.
3. Ultrasound Department, Shengjing Hospital, China Medical University, Shenyang 110016, China.
4. Department of Basic Pharmaceutical Sciences, School of Pharmacy, Husson University, Bangor, ME 04401, USA.
5. School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China.
- Publication Type:Journal Article
- Keywords:
Fatty alcohol polyoxyethylene ether;
Fibrosis;
Foam preparation;
Matrix metalloproteinases;
Plasmin system;
Sclerotherapy;
Tranexamic acid;
Venous malformations
- From:
Acta Pharmaceutica Sinica B
2025;15(6):3291-3304
- CountryChina
- Language:English
-
Abstract:
Venous system diseases mainly include varicose veins and venous malformations of lower limbs and the genital system. Most of them are chronic diseases that cause serious clinical symptoms to patients and affect their health and quality of life. Sclerotherapy has become the first-line therapy for venous system diseases. However, there are problems such as incomplete fibrosis and vascular recanalization after sclerotherapy, and improper operation will cause serious adverse consequences. Therefore, exploring a safe and effective sclerotherapy strategy is essential for developing clinically successful sclerotherapy. To solve the above problems, we proposed a new sclerotherapy strategy with a dual mechanism of "vascular damage and plasmin (PLA) system inhibition." We intended to construct a novel cationic surfactant (AEOx-TA) by reacting tranexamic acid (TA), a parent structure, with fatty alcohol polyoxyethylene ether (AEOx) by ester bonds. AEOx-TA could damage vascular endothelium and initiate a coagulation cascade effect to induce thrombus. Furthermore, AEOx-TA could be degraded by esterase and release the parent drug, TA, which could inhibit the PLA system to inhibit the degradation of thrombus and extracellular matrix and promote the process of vascular fibrosis. In addition, such surfactant-based sclerosants have foam-forming properties, and they can be blended with polyvinyl alcohol (PVA) to prepare a highly stable foam formulation (AEOx-TA/P), which can achieve a precise drug delivery and prolonged drug retention time, thereby improving drug efficacy and reducing the risk of ectopic embolism. Overall, the novel cationic surfactant AEOx-TA provides a new avenue to resolve the bottleneck: surfactant sclerosants' efficiency is relatively low in the current sclerotherapy.
