PEFLOXACINE MESILATE-LOADED AND OFLOXACIN-LOADED POLYETHYLCYANOACRYLATE NANOPARTICLES - CHARACTERIZATION OF THE COLLOIDAL DRUG CARRIER FORMULATION
PEFLOXACINE MESILATE-LOADED AND OFLOXACIN-LOADED POLYETHYLCYANOACRYLATE NANOPARTICLES - CHARACTERIZATION OF THE COLLOIDAL DRUG CARRIER FORMULATION
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DOI：
10.1002/jps.2600840721
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发表时间：
1995-07-01
影响因子：
3.8
通讯作者：
FURNERI, PM
中科院分区：
文献类型：
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作者：
FRESTA, M;PUGLISI, G;FURNERI, PM
氟喹诺酮类药物，甲磺酸过氟沙星（PFX）和氧氟沙星（OFX）包埋在聚烷基氰基丙烯酸酯（PECA）纳米颗粒中，可以为其生物应用提供一些优势；例如，提高其生物利用度，控制药物在血液中的释放时间，减少细菌耐药性的形成。采用掺入法或吸附法将这两种药物装入PECA聚合物体中。这两种方法都能影响纳米颗粒的大小、分子量、释放谱和药物-聚合物的结合。掺入方法，特别是OFX系统，实现了PECA纳米颗粒悬浮液，其平均尺寸值比没有药物时高三倍。相比之下，PFX系统的变化可以忽略不计。制备过程也影响了纳米颗粒的储存稳定性。各种纳米颗粒制剂的分子量值也受到影响；也就是说，负载pfx的系统显示出平均分子量值的增强，而负载ofx的系统则观察到平均分子量值的降低。吸附法制备的纳米颗粒在粒径、分子量、储存稳定性等方面均与不含药物制备的纳米颗粒无明显差异。在掺入制备过程中获得的胶体系统的纳米颗粒负载能力更高。两种制备工艺的药物释放均为双相。负载氟喹诺酮的纳米颗粒对标准菌株的抗菌活性比游离药物增强2 ~ 50倍。
The entrapment of fluoroquinolones, perfloxacine mesilate (PFX) and ofloxacin (OFX), in polyalkylcyanoacrylate (PECA) nanoparticles could offer some advantages for their biological application; for examples, increasing their bioavailability, controlling the drug time-release in blood, and reducing the formation of bacterial resistance. To load these two drugs in PECA polymeric bulk, the incorporation or adsorption method was performed. These two methods were capable of influencing nanoparticle size, molecular weight, release profile, and drug-polymer association. The incorporation method, particularly for the OFX system, achieved PECA nanoparticle suspensions with a mean size value three times higher than that obtained in the absence of the drug. In contrast, negligible changes were observed for PFX systems. This preparation process also influenced the nanoparticle storage stability. The molecular weight values of the various nanoparticle preparations were also influenced; that is, the PFX-loaded systems showed an enhancement in the average molecular weight values, whereas a reduction was observed for OFX-loaded systems. The adsorption method showed no particular difference in particle size, molecular weight, and storage stability compared with nanoparticles prepared without the drugs. The nanoparticle loading capacity was higher for the colloidal systems obtained following the incorporation preparation procedure. The release of drug from the nanoparticles was biphasic for both preparation processes. The fluoro-quinolone-loaded nanoparticles showed an enhancement of the antimicrobial activity against standard bacteria strains from 2- to 50-fold compared with the free drugs.