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基于具有抗菌活性的普朗尼克胶束的药物递送系统

Drug Delivery Systems Based on Pluronic Micelles with Antimicrobial Activity.

作者信息

Popovici Corina, Popa Marcel, Sunel Valeriu, Atanase Leonard Ionut, Ichim Daniela Luminita

机构信息

"Cristofor Simionescu" Faculty of Chemical Engineering and Environmental Protection, "Gheorghe Asachi" Technical University of Iasi, 700050 Iasi, Romania.

Academy of Romanian Scientists, 050045 Bucharest, Romania.

出版信息

Polymers (Basel). 2022 Jul 25;14(15):3007. doi: 10.3390/polym14153007.

Abstract

Bacterial oral diseases are chronic, and, therefore, require appropriate treatment, which involves various forms of administration and dosing of the drug. However, multimicrobial resistance is an increasing issue, which affects the global health system. In the present study, a commercial amphiphilic copolymer, Pluronic F127, was used for the encapsulation of 1-(5'-nitrobenzimidazole-2'-yl-sulphonyl-acetyl)-4-aryl-thiosemicarbazide, which is an original active pharmaceutical ingredient (API) previously synthesized and characterized by our group, at different copolymer/API weight ratios. The obtained micellar systems, with sizes around 20 nm, were stable during 30 days of storage at 4 °C, without a major increase of the Z-average sizes. As expected, the drug encapsulation and loading efficiencies varied with the copolymer/API ratio, the highest values of 84.8 and 11.1%, respectively being determined for the F127/API = 10/1 ratio. Moreover, in vitro biological tests have demonstrated that the obtained polymeric micelles (PMs) are both hemocompatible and cytocompatible. Furthermore, enhanced inhibition zones of 36 and 20 mm were observed for the sample F127/API = 2/1 against and , respectively. Based on these encouraging results, it can be admitted that these micellar systems can be an efficient alternative for the treatment of bacterial oral diseases, being suitable either by injection or by a topical administration.

摘要

细菌性口腔疾病是慢性疾病,因此需要适当的治疗,这涉及药物的各种给药形式和剂量。然而,多重微生物耐药性问题日益严重,影响着全球卫生系统。在本研究中,一种商业两亲共聚物泊洛沙姆F127被用于包封1-(5'-硝基苯并咪唑-2'-基-磺酰基-乙酰基)-4-芳基-硫代氨基脲,这是我们小组先前合成并表征的一种原创活性药物成分(API),采用不同的共聚物/API重量比。所获得的胶束系统尺寸约为20 nm,在4℃下储存30天期间稳定,Z-平均尺寸没有大幅增加。正如预期的那样,药物包封率和载药率随共聚物/API比例而变化,对于F127/API = 10/1的比例,分别确定了最高值84.8%和11.1%。此外,体外生物学测试表明,所获得的聚合物胶束(PMs)具有血液相容性和细胞相容性。此外,对于样品F127/API = 2/1,分别观察到对[具体细菌1]和[具体细菌2]的增强抑菌圈为36和20 mm。基于这些令人鼓舞的结果,可以认为这些胶束系统可以成为治疗细菌性口腔疾病的有效替代方案,适合注射或局部给药。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e2ef/9331063/580ccd228fa9/polymers-14-03007-g001.jpg

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