Zhang Pei, Guo Huixia, Liu Chenguang
College of Marine Life Sciences, Ocean University of China, Qingdao 266003, China.
Department of Life Science, Luoyang Normal University, Luoyang 471022, China.
Polymers (Basel). 2020 Feb 11;12(2):408. doi: 10.3390/polym12020408.
Micro-molecular drugs have special advantages to cope with challenging diseases, however their structure, physical and chemical properties, stability, and pharmacodynamics have more requirements for the way they are delivered into the body. Carrier-based drug delivery systems can circumvent many limited factors of drug delivery and increase their bioavailability. In this context, stable drug nanocarriers of alkaline amino acids (arginine, Arg) modified conjugated linoleic acid-carboxymethyl chitosan (CLA-CMCS) conjugate were developed, which could generate supramolecular micelles to effectively encapsulate the tyrosinase inhibitor phenylethyl resorcinol (PR). The resulting CCA-NPs were spherical nanoparticles with a mean size around 175 nm. The 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay and cellular uptake investigation demonstrated that the CCA-NPs were non-cytotoxic and had excellent cell transport ability. In addition, these CCA-NPs were able to effectively deliver PR and inhibited melanin formation to reduce pigmentation by enhancing cellular uptake. In conclusion, our research indicated that nanocarriers based on self-assembly amphiphilic polymers constituted a promising and effective drug delivery system in hyperpigmentation targeting.
小分子药物在应对具有挑战性的疾病方面具有特殊优势，然而其结构、物理化学性质、稳定性和药效学对其进入体内的方式有更多要求。基于载体的药物递送系统可以规避药物递送的许多限制因素并提高其生物利用度。在此背景下，开发了碱性氨基酸（精氨酸，Arg）修饰的共轭亚油酸-羧甲基壳聚糖（CLA-CMCS）共轭物的稳定药物纳米载体，其可以产生超分子胶束以有效包封酪氨酸酶抑制剂苯乙基间苯二酚（PR）。所得的CCA-NPs为球形纳米颗粒，平均尺寸约为175nm。3-(4,5-二甲基-2-噻唑基)-2,5-二苯基-2-H-四氮唑溴盐（MTT）试验和细胞摄取研究表明，CCA-NPs无细胞毒性且具有优异的细胞转运能力。此外，这些CCA-NPs能够有效递送PR并通过增强细胞摄取来抑制黑色素形成以减少色素沉着。总之，我们的研究表明基于自组装两亲聚合物的纳米载体在靶向色素沉着过度方面构成了一种有前景且有效的药物递送系统。
