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载万古霉素的 N,N-十二烷基甲基聚亚乙基亚胺纳米粒经透明质酸修饰用于治疗细菌性眼内炎:制备、表征和眼部生物相容性。

Vancomycin-loaded N,N-dodecyl,methyl-polyethylenimine nanoparticles coated with hyaluronic acid to treat bacterial endophthalmitis: Development, characterization, and ocular biocompatibility.

机构信息

School of Pharmacy, Federal University of Ouro Preto, Ouro Preto, Minas Gerais 35.400-000, Brazil.

Chemistry Department, Federal University of Minas Gerais, Belo Horizonte, Minas Gerais 31.270-901, Brazil.

出版信息

Int J Biol Macromol. 2021 Feb 1;169:330-341. doi: 10.1016/j.ijbiomac.2020.12.057. Epub 2020 Dec 10.

Abstract

Vancomycin-loaded N,N-dodecyl,methyl-polyethylenimine nanoparticles coated with hyaluronic acid (VCM-DMPEI nanoparticles/HA) were synthesized as an adjuvant for the treatment of bacterial endophthalmitis. The nanoparticles were formulated by experimental statistical design, thoroughly characterized, and evaluated in terms of bactericidal activity and both in vitro and in vivo ocular biocompatibility. The VCM-DMPEI nanoparticles/HA were 154 ± 3 nm in diameter with a 0.197 ± 0.020 polydispersity index; had a + 26.4 ± 3.3 mV zeta potential; exhibited a 93% VCM encapsulation efficiency; and released 58% of the encapsulated VCM over 96 h. VCM and DMPEI exhibited a synergistic bactericidal effect. The VCM-DMPEI nanoparticles/HA were neither toxic to ARPE-19 cells nor irritating to the chorioallantoic membrane. Moreover, the VCM-DMPEI nanoparticles/HA did not induce modifications in retinal functions, as determined by electroretinography, and in the morphology of the ocular tissues. In conclusion, the VCM-DMPEI nanoparticles/HA may be a useful therapeutic adjuvant to treat bacterial endophthalmitis.

摘要

载万古霉素的 N,N-十二烷基甲基-聚乙二烯亚胺纳米颗粒用透明质酸(VCM-DMPEI 纳米颗粒/HA)包被,作为治疗细菌性眼内炎的佐剂。通过实验统计设计合成纳米颗粒,对其进行了全面的表征,并从杀菌活性以及体外和体内眼组织相容性两方面进行了评估。VCM-DMPEI 纳米颗粒/HA 的直径为 154 ± 3nm,多分散指数为 0.197 ± 0.020;具有 +26.4 ± 3.3mV 的 ζ 电位;包封效率为 93%,96h 内释放 58%的包封万古霉素。万古霉素和 DMPEI 表现出协同杀菌作用。VCM-DMPEI 纳米颗粒/HA 对 ARPE-19 细胞既无毒性,也对鸡胚尿囊膜无刺激性。此外,电视网膜图和眼组织形态学检查均表明,VCM-DMPEI 纳米颗粒/HA 不会引起视网膜功能的改变。综上所述,VCM-DMPEI 纳米颗粒/HA 可能是治疗细菌性眼内炎的一种有用的治疗佐剂。

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