Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, China.
School of Light Industry, Beijing Technology and Business University, Beijing 100048, China.
Molecules. 2022 Jul 19;27(14):4613. doi: 10.3390/molecules27144613.
Chrysomycin A, a compound derived from marine microorganisms, proved to have a specific great in vitro inhibitory effect on methicillin-resistant (MRSA). It exhibits high safety for the skin, as well as a better therapeutic effect than the current clinical drug, vancomycin. Nevertheless, its poor water solubility highly limits the application and reduces the bioavailability. In view of this, we developed a cream of chrysomycin A (CA) to enhance the solubility for the treatment of skin infection, while avoiding the possible toxicity caused by systemic administration. A comprehensive orthogonal evaluation system composed of appearance, spreading ability, and stability was established to find the optimal formula under experimental conditions. The final product was odorless and easy to be spread, with a lustrous, smooth surface. The particle size of the product met Chinese Pharmacopoeia specifications and the entire cream showed long-term stability in destructive tests. The in vitro and in vivo studies indicated that CA cream had a similar anti-MRSA activity to commercially available mupirocin, showing its potential as an efficacious topical delivery system for skin infections treatment.
棘霉素 A 是一种来源于海洋微生物的化合物，已被证明对耐甲氧西林金黄色葡萄球菌（MRSA）具有特殊的体外抑制作用。它对皮肤安全性高，治疗效果优于目前的临床药物万古霉素。然而，其较差的水溶性极大地限制了其应用，降低了生物利用度。鉴于此，我们开发了棘霉素 A 乳膏以提高其水溶性，用于治疗皮肤感染，同时避免全身给药可能引起的毒性。建立了一个由外观、铺展能力和稳定性组成的综合正交评价体系，以在实验条件下找到最佳配方。最终产品无味且易于铺展，表面有光泽、光滑。产品的粒径符合中国药典的规定，整个乳膏在破坏性试验中表现出长期稳定性。体外和体内研究表明，CA 乳膏对市售莫匹罗星具有相似的抗 MRSA 活性，表明其作为一种有效的局部递药系统，具有治疗皮肤感染的潜力。
