The supramolecular self-assembly of 5-fluorouracil and caffeic acid through cocrystallization strategy opens up a new way for the development of synergistic antitumor pharmaceutical cocrystal

Abstract

In order to give full play to the preponderances of cocrystallization technique in improving the biopharmaceutical limitations in vitro and ameliorating the pharmacokinetic properties in vivo together with heightening the...

Cocrystallization-driven self-assembly with vanillic acid offers a new opportunity for surmounting fast and excessive absorption issues of antifungal drug 5-fluorocytosine: a combined theoretical and experimental research

“…To date, although many efforts have been devoted to the exploration of antimycotic agents, the routine guidelines for new drug development hardly satisfy the urgent requirement for the rapid creation of effective antifungal drugs within a short period, owing to the features of being time-consuming and high-cost along with having a low success rate. 6 Consequently, it is quite reasonable and necessary for the optimization of existing drugs to improve their efficacy and reduce toxicity. 5-Fluorocytosine (FCY, Scheme 1) is the priority drug used in tablet form for the clinical prevention and control of fungal infections, due to the high sensitivity to systemic fungal infections caused by Candida and Cryptococcus .…”

Diffusion and Flux Improvement of Drugs through Complexation

“…The biopharmaceutical limitations and pharmacokinetic properties of antimetabolic chemotherapy drug 5-fluorouracil (FL) was studied using caffeic acid (CF), a well-known hydroxycinnamic acid. 103 The crystalline binary solid was isolated as a dihydrate cocrystal (FL−CF•2H 2 O). FL and CF are connected via acid-amide synthon of R 2 2 (8) graph set notation.…”

The First Cocrystallization of Milrinone with Nutraceuticals: The Adjusting Effects of Hydrophilicity/Hydrophobicity in Cavities on the In Vitro/In Vivo Properties of the Cocrystals

“…Of all the CCFs available, phenolic acids, because of their unique structure feature containing both hydroxyl and carboxyl groups on their benzene ring that can provide universal hydrogen-bonding sites, , have been viewed as the ideal candidate CCFs during the assembling of pharmaceutical cocrystals. Lately, some phenolic acids have been successfully cocrystallized with certain APIs for constructing pharmaceutical cocrystals, − which has laid the foundation for the cocrystallization of phenolic acids with MLN. More importantly, a number of phenolic acids possessing excellent physicochemical properties can be used as natural nutraceuticals with potential health benefits, playing important roles in the human dietary and health protective.…”

“…From the perspective of practicality and medicinal function, the existing nutraceuticals among phenolic acids, except for healthcare, have been proven to have obvious biological and pharmacological effects in the antimicrobial, anticancer, and antiinflammatory, especially the spacious application prospect in the prevention and treatment of cardiovascular diseases with the low toxicity and reliable safety. , Therefore, in view of the unique superiority of phenolic acid nutraceuticals, they are significant as feasible CCFs in the pharmaceutical cocrystallization field. So far, although phenolic acid nutraceuticals as CCFs have been widely used in the amelioration of antibacterial and antitumor drugs via cocrystallization techniques, , there is almost nothing in the study of optimizing the properties and efficacy of cardiovascular drugs. According to these reasons, the design and preparation of MLN-phenolic acid nutraceutical cocrystals are of great significance to explore and evaluate the influence of phenolic acids with different substituents on in vivo/in vitro pharmaceutical performances of MLN, thus laying the application foundation for various phenolic acid nutrients in regulating and improving cardiovascular drugs by cocrystallization techniques.…”