63101-32-6Relevant articles and documents
Co-delivery of bufalin and nintedanib via albumin sub-microspheres for synergistic cancer therapy
Xu, Ying,Liu, Yulong,Liu, Qi,Lu, Shengzhe,Chen, Xiaolin,Xu, Wenrong,Shi, Feng
, p. 705 - 718 (2021)
Albumin nanoparticles represent an approved anti-tumor drug delivery system. However, there is only one albumin nanoparticle product (paclitaxel-albumin nanoparticle) on the market. The application of albumin carriers is limited by the lack of universal preparation technology and insufficient targeting effect. Herein, we developed multifunctional albumin sub-microspheres prepared by coaxial-electrospray technology to co-delivery bufalin and nintedanib for tumor-targeted combination therapy. The biguanide and ursodeoxycholic acid dual-modified multifunctional albumin was synthesized to enhance the anti-tumor effect and tumor target efficiency. Coaxial-electrospray technology was utilized in preparing albumin sub-microspheres with a core-shell structure that enables payload efficiency and stability. More importantly, the in vitro and in vivo experiments demonstrated that the multifunctional albumin sub-microspheres possessed superior tumor target efficiency. Furthermore, nintedanib and bufalin combined therapy relieved the tumor microenvironment and exerted a synergistic therapeutic effect. Therefore, this work provides a novel method for fabricating an albumin-based drug delivery system and a potential efficient combination therapeutic strategy for tumor treatment.
Method for synthesizing 1-(p-CARBOXYPHENYL)BIGUANIDE HYDROCHLORIDE)
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Paragraph 0008, (2016/10/31)
The invention discloses a method for synthesizing 1-(p-CARBOXYPHENYL)BIGUANIDE HYDROCHLORIDE) and belongs to derivatives of biguanidino-containing guanidine. The method comprises the following steps: adding p-aminobenzoic acid and hydrochloric acid into a reaction vessel according to a mass ratio, carrying out full stirring so as to completely dissolve p-aminobenzoic acid, then, adding dicyandiamide into the solution in a staged manner, heating the solution to the temperature of 120 DEG C, and carrying out reaction for 0.5-4 hours; after the reaction ends, stopping heating and stirring, and concentrating the reaction solution so as to boil off the majority of water in the system; adding acetone into the residue so as to precipitate the product out of the residue; and carrying out filtration, recrystallizing the obtained solid with an acetone-water mixed solvent, and then, carrying out vacuum drying, thereby obtaining the p-biguanidino benzoic acid hydrochloride. According to the method provided by the invention, the synthesis process is short in time, high in yield, and low in cost, is simple, easy and safe and can achieve clean production, the industrial production is facilitated, and the yield of the 1-(p-CARBOXYPHENYL)BIGUANIDE HYDROCHLORIDE) is higher than 80.0%.