Construction and evaluation of a phospholipid-based phase transition in situ gel system for brexpiprazole

作者全名："Tao, Ran; Liu, Li; Xiong, Yingxin; Zhang, Qianyu; Lv, Xiangyu; He, Linbo; Ren, Fang; Zhou, Lu; Chen, Baoyan; Wu, Kexin; Zhang, Yan; Chen, Huali"

作者地址："[Tao, Ran; Zhang, Qianyu; Ren, Fang; Zhou, Lu; Chen, Baoyan; Wu, Kexin; Chen, Huali] Chongqing Med Univ, Coll Pharm, Chongqing 400042, Peoples R China; [Liu, Li; Xiong, Yingxin; Lv, Xiangyu; He, Linbo; Zhang, Yan] Yaopharma Co Ltd, 100 Xingguang Ave, Chongqing 401121, Peoples R China"

通信作者："Chen, HL (通讯作者)，Chongqing Med Univ, Coll Pharm, Chongqing 400042, Peoples R China.; Zhang, Y (通讯作者)，Yaopharma Co Ltd, 100 Xingguang Ave, Chongqing 401121, Peoples R China."

来源：DRUG DELIVERY AND TRANSLATIONAL RESEARCH

ESI学科分类：PHARMACOLOGY & TOXICOLOGY

WOS号：WOS:000985432200001

JCR分区：Q1

影响因子：5.7

年份：2023

卷号：　

期号：　

开始页：　

结束页：　

文献类型：Article; Early Access

关键词：Phospholipids; In situ gel; Long-acting injection; Sustained-release; Schizophrenia

摘要："The objective of this study was to develop phospholipid-based injectable phase transition in situ gels (PTIGs) for the sustained release of Brexpiprazole (Brex). Phospholipid (Lipoid S100, S100) and stearic acid (SA) were used as the gel matrix which was dissolved in biocompatible solvent medium-chain triglyceride (MCT), N-methyl pyrrolidone (NMP), and ethanol to obtain PTIGs solution. The Brex PTIG showed a solution condition of low viscosity in vitro and was gelatinized in situ in vivo after subcutaneous injection. Both in vitro release assay and in vivo pharmacokinetics study in SD rats displayed that Brex in PTIGs could achieve a sustained release, compared with brexpiprazole solution (Brex-Sol) or brexpiprazole suspension (Brex-Sus). The Brex-PTIGs had good degradability and biocompatibility in vivo with rare inflammation at the injection site. Among the three Brex-PTIG formulations, Brex-PTIG-3 with the SA in the formulation had the greatest gelation viscosity, the lowest initial release rate, and the most stable release profile with sustained release of up to 60 days. The above results indicated that, as a novel drug delivery system, the Brex-PTIGs offered a new option for the clinical treatment of patients with schizophrenia."

基金机构：Program of Postgraduate Joint Training Base of Chongqing; Science and Technology Research Program of Chongqing Municipal Education Commission [KJQN202000407]

基金资助正文："The study leading to the reported results was funded by the Program of Postgraduate Joint Training Base of Chongqing (Chongqing Medical University & Yaopharma Co., Ltd joint training base for postgraduate in pharmacy) (to Huali Chen and Yan Zhang), and the Science and Technology Research Program of Chongqing Municipal Education Commission (grant no. KJQN202000407; to Huali Chen)."