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Carboxymethyl Cellulose-Coated Tacrolimus Nonspherical Microcrystals for Improved Therapeutic Efficacy of Dry Eye.
Macromolecular Bioscience ( IF 4.4 ) Pub Date : 2020-06-15 , DOI: 10.1002/mabi.202000079 Caijie Zhang 1 , Yingying Zheng 2 , Min Li 3 , Zhongfang Zhang 1 , Lianqing Chang 1 , Mingyue Ai 3 , Jingjie Wang 4 , Shaozhen Zhao 1 , Chen Li 3 , Zhimin Zhou 3
Macromolecular Bioscience ( IF 4.4 ) Pub Date : 2020-06-15 , DOI: 10.1002/mabi.202000079 Caijie Zhang 1 , Yingying Zheng 2 , Min Li 3 , Zhongfang Zhang 1 , Lianqing Chang 1 , Mingyue Ai 3 , Jingjie Wang 4 , Shaozhen Zhao 1 , Chen Li 3 , Zhimin Zhou 3
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Dry eye (DE) is a highly prevalent ocular surface disease which affects the quality of life and results in low working efficiency. Frequent instillation is required due to low bioavailability of conventional eye drops. The aim of this study is to develop a novel formulation of tacrolimus (TAC), routinely prescribed for DE, by combination of the microcrystal technology and layer‐by‐layer assembly. First, nonspherical tacrolimus microcrystals (TAC MCs) are synthesized by antisolvent‐induced precipitation. These TAC MCs are modified by alternate deposition of poly(allylamine hydrochloride) (PAH) and carboxymethyl cellulose (CMC) subsequently to obtain CMC‐coated TAC MCs (TAC‐(PAH/CMC)3). The resultant formulations are evaluated in vivo in a mouse DE model induced by an intelligently controlled environmental system. Compared with commercially available TAC eye drops and the TAC MCs counterpart, TAC‐(PAH/CMC)3 exhibits superior therapeutic performance with reduced drug instillation frequency, which is attributed to the nonspherical geometry of MCs, the lubricant, mucoadhesive effect of CMC, and the anti‐inflammatory function of TAC. Therefore, TAC‐(PAH/CMC)3 represents a better option for the management of DE.
中文翻译：
羧甲基纤维素包覆的他克莫司非球面微晶可改善干眼症的治疗功效。
干眼症（DE）是一种高度流行的眼表疾病，会影响生活质量并导致工作效率低下。由于常规滴眼液的生物利用度低，因此需要频繁滴注。这项研究的目的是结合微晶技术和逐层组装技术，开发一种常规用于DE的他克莫司（TAC）制剂。首先，通过反溶剂诱导的沉淀法合成非球形他克莫司微晶（TAC MC）。通过交替沉积聚烯丙胺盐酸盐（PAH）和羧甲基纤维素（CMC）来修饰这些TAC MC，随后获得涂有CMC的TAC MC（TAC‐（PAH / CMC）3）。在由智能控制的环境系统诱导的小鼠DE模型中对所得制剂进行体内评估。与市售的TAC滴眼剂和TAC MC的同类产品相比，TAC-（PAH / CMC）3具有优异的治疗性能，降低了药物滴注频率，这归因于MC的非球形几何形状，润滑剂，CMC的粘膜粘附作用和TAC的抗炎功能。因此，TAC-（PAH / CMC）3是DE管理的更好选择。
更新日期：2020-06-15
中文翻译：
羧甲基纤维素包覆的他克莫司非球面微晶可改善干眼症的治疗功效。
干眼症（DE）是一种高度流行的眼表疾病，会影响生活质量并导致工作效率低下。由于常规滴眼液的生物利用度低，因此需要频繁滴注。这项研究的目的是结合微晶技术和逐层组装技术，开发一种常规用于DE的他克莫司（TAC）制剂。首先，通过反溶剂诱导的沉淀法合成非球形他克莫司微晶（TAC MC）。通过交替沉积聚烯丙胺盐酸盐（PAH）和羧甲基纤维素（CMC）来修饰这些TAC MC，随后获得涂有CMC的TAC MC（TAC‐（PAH / CMC）3）。在由智能控制的环境系统诱导的小鼠DE模型中对所得制剂进行体内评估。与市售的TAC滴眼剂和TAC MC的同类产品相比，TAC-（PAH / CMC）3具有优异的治疗性能，降低了药物滴注频率，这归因于MC的非球形几何形状，润滑剂，CMC的粘膜粘附作用和TAC的抗炎功能。因此，TAC-（PAH / CMC）3是DE管理的更好选择。
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