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Novel Oleyl Amine-modified Polymannuronic Acid Micelle Loading Tacrolimus for Therapy of Allergic Conjunctivitis

Cong, Mengyi, Wu, Zhongyu, Xu, Xuelian, Yin, Jiaqi, Li, Hongxia, Zhuang, Bo, Wang, Cheng, Zhao, Xia
International journal of biological macromolecules 2017
animal models, biocompatibility, biodegradability, conjunctivitis, cytotoxicity, drugs, encapsulation, hydrophobicity, medication adherence, micelles, nanocarriers, nanoparticles, nuclear magnetic resonance spectroscopy, particle size, patients, tacrolimus
Marine polysaccharide-based nanomaterial attracted considerable attention due to its biocompatibility and biodegradability. Here, a novel polymannuronic acid derivative (PM-C18) was synthesized as nanocarrier modified with hydrophobic oleyl amine. Its structure was confirmed by Fourier-transformed infrared spectrometry and nuclear magnetic resonance. To investigate its function, we developed tacrolimus (FK506) loaded nanoparticle by self-assembling PM-C18 and studied its drug loading, cytotoxicity and mechanism of in vitro release. Furthermore, we established a mouse model of allergic conjunctivitis (AC) to evaluate the efficacy of FK506 loaded PM-C18. The results indicated that PM-C18 carrier can encapsule FK506 with high drug loading (18%) and average particle size of 110.34±1.6nm. The release mechanism was diffusion initially followed a lasting release induced by swelling and collapse of PM-C18. One-week treatment with FK506 loaded PM-C18 efficiently relieved the symptoms of AC, which indicated it could serve as a potential ophthalmic drug for patients with AC. Compared with FK506 ophthalmic suspension, FK506 loaded PM-C18 improved medication adherence. Most importantly, we developed a novel versatile nanomaterial of PM-C18 which could encapsule other active agents for more applications.