(488d) Green Synthesis of Magnolol Multicomponent Crystals for Improved Natural Antibiotics and Customizable Release Profiles

Green and eco-friendly antibiotic is one of the challenges facing the global pharmaceutical industry. Antibiotics are widely consumed in clinic, livestock and agriculture, increasing annually. Non-biodegradable antibiotics cause widespread and persistent pollution of ecosystems, setting off microbial resistance storms. Developing new antibiotics is the main strategy to solve resistance, and natural products are the important sources of drugs. However, the common poor physiochemical properties of natural products prevent it from clinic. Additionally, it is difficult and challenged to customize release and antibacterial activity of antibiotics without loading materials, but crystal engineering is a potential powerful tool to overcome these challenges.

Magnolol is a natural antibiotic, but poor physicochemical properties result in low bioavailability. In this work, the building blocks of multicomponent materials were manipulated by designing different isomers to achieve precise tuning of release profiles with good gradients and improved antibacterial activity. Three novel multicomponent crystalline solids were synthesized from magnolol and isomeric coformers by mechanochemistry. It was found that the multicomponent crystals achieved the customizable release profile of magnolol by manipulating the substituent positions of the isomers and complexation. Antibacterial activity test showed that bioactivity on two bacteria was significantly improved by designed multicomponent crystals. In addition, the variable statistical analysis indicated that the coformers controlled the dissolution behavior and further stabilized the improvement. This contributes to the efficient use of antibiotics and seeks to customize therapy for the needs of specific individuals.

In conclusion, the properties of magnolol multicomponent crystals can be manipulated through the predesign of building blocks. Crystal engineering provides an efficient strategy to control the release of drugs and meet individual biological differences and various treatment needs.