118675-23-3

Upstream product

• 60-33-3 linoleic acid 
• 107-21-1 ethylene glycol 

Relevant academic research and scientific papers

An exosome-like programmable-bioactivating paclitaxel prodrug nanoplatform for enhanced breast cancer metastasis inhibition

Metastasis is closely associated with high breast cancer mortality. Although nanotechnology-based anti-metastatic treatments have developed rapidly, the anti-metastasis efficiency is still far from satisfactory, mainly due to the poor recognition of circulating tumor cells (CTCs) in blood. Herein, we developed an exosome-like sequential-bioactivating prodrug nanoplatform (EMPCs) to overcome the obstacle. Specifically, the reactive oxygen species (ROS)-responsive thioether-linked paclitaxel-linoleic acid conjugates (PTX-S-LA) and cucurbitacin B (CuB) are co-encapsulated into polymeric micelles, and the nanoparticles are further decorated with exosome membrane (EM). The resulting EMPCs could specifically capture and neutralize CTCs during blood circulation through the high-affinity interaction between cancer cell membrane and homotypic EM. Following cellular uptake, EMPCs first release CuB, remarkably blocking tumor metastasis via downregulation of the FAK/MMP signaling pathway. Moreover, CuB obviously elevates the intracellular oxidative level to induce a sequential bioactivation of ROS-responsive PTX-S-LA. In vitro and in vivo results demonstrate that EMPCs not only exhibit amplified prodrug bioactivation, prolonged blood circulation, selective targeting of homotypic tumor cells, and enhanced tumor penetration, but also suppress tumor metastasis through CTCs clearance and FAK/MMP signaling pathway regulation. This study proposes an integrated approach for mechanism-based inhibition of tumor metastasis and manifests a promising potential of programmable-bioactivating prodrug nanoplatform for cancer metastasis inhibition.

Cabazitaxel-fatty acid conjugate and nano preparation thereof

The invention belongs to the technical field of medicines, relates to an antitumor drug cabazitaxel-fatty acid conjugate as well as a preparation method and application thereof, and further relates to a nano preparation of the cabazitaxel-fatty acid conjugate and application thereof. The fatty acid is oleic acid or linoleic acid. In the cabazitaxel-fatty acid conjugate disclosed by the invention, hydroxyl of cabazitaxel is connected with carboxyl of oleic acid or linoleic acid through a disulfide bond. The cabazitaxel-linoleic acid conjugate or the cabazitaxel-linoleic acid conjugate can be self-assembled into nanoparticles, and the preparation is simple in preparation process and easy to industrialize; the sensitive drug release of the intracellular environment of a tumor part can be realized, the anti-tumor cell activity is higher, and the in-vivo pharmacokinetic property is better; most importantly, the nano preparation shows higher in-vivo tumor inhibition activity, and shows a more excellent in-vivo safety effect of the preparation at the same time.

Disulfide bond bridged docetaxel-fatty acid prodrugs and self-assembled nanoparticles thereof

According to the invention, a series of reduction-sensitive disulfide bond bridged docetaxel fatty acid prodrugs are designed and synthesized. The series of prodrugs can be self-assembled into a nano drug delivery system through a one-step nano precipitation method. The nano drug delivery system has the following advantages that: docetaxel is prepared into a disulfide bond connected prodrug, so that the system toxicity of a docetaxel parent drug is reduced, the parent drug can be specifically released in a high reduction environment in tumor cells, and the effects of synergy and toxicity reduction are achieved; the drug loading capacity is high, the use of a solubilizer with higher toxicity is avoided, and the tolerance and the compliance of a patient are expected to be improved; through the one-step nano precipitation method, the preparation process is simple, and large-scale production is easy; the nanoparticles are small and uniform in particle size and are easily enriched at a tumor part through an EPR effect; and surface modification is easy, and removal of a reticuloendothelial system can be slowed down through modification of PEG modification.

LIPIDS AND LIPID COMPOSITIONS FOR THE DELIVERY OF ACTIVE AGENTS

This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1–R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.