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Moxifloxacin Hydrochloride-Loaded Eudragit® RL 100 and Kollidon® SR Based Nanoparticles: Formulation, In vitro Characterization and Cytotoxicity
Combinatorial Chemistry & High Throughput Screening ( IF 1.6 ) Pub Date : 2021-02-28 , DOI: 10.2174/1386207323666200428091945
Gülsel Yurtdaş Kırımlıoğlu 1 , Sinan Özer 1 , Gülay Büyükköroğlu 2 , Yasemin Yazan 1
Affiliation  

Background: Considering the low ocular bioavailability of conventional formulations used for ocular bacterial infection treatment, there is a need to design efficient novel drug delivery systems that may enhance precorneal retention time and corneal permeability.

Aim and Objective: The current research focuses on developing nanosized and non-toxic Eudragit® RL 100 and Kollidon® SR nanoparticles loaded with moxifloxacin hydrochloride (MOX) for its prolonged release to be promising for effective ocular delivery.

Methods: In this study, MOX incorporation was carried out by spray drying method aiming ocular delivery. In vitro characteristics were evaluated in detail with different methods.

Results: MOX was successfully incorporated into Eudragit® RL 100 and Kollidon® SR polymeric nanoparticles by a spray-drying process. Particle size, zeta potential, entrapment efficiency, particle morphology, thermal, FTIR, NMR analyses and MOX quantification using HPLC method were carried out to evaluate the nanoparticles prepared. MOX loaded nanoparticles demonstrated nanosized and spherical shape while in vitro release studies demonstrated modified-release pattern, which followed the Korsmeyer-Peppas kinetic model. Following the successful incorporation of MOX into the nanoparticles, the formulation (MOX: Eudragit® RL 100, 1:5) (ERL-MOX 2) was selected for further studies because of its better characteristics like cationic zeta potential, smaller particle size, narrow size distribution and more uniform prolonged release pattern. Moreover, ERLMOX 2 formulation remained stable for 3 months and demonstrated higher cell viability values for MOX.

Conclusion: In vitro characterization analyses showed that non-toxic, nano-sized and cationic ERL-MOX 2 formulation has the potential of enhancing ocular bioavailability.



中文翻译:

装载有盐酸莫西沙星的 Eudragit® RL 100 和 Kollidon® SR 纳米颗粒:配方、体外表征和细胞毒性

背景:考虑到用于眼部细菌感染治疗的常规制剂的眼部生物利用度低,需要设计有效的新型药物递送系统,以提高角膜前保留时间和角膜通透性。

目的和目的:目前的研究重点是开发纳米尺寸和无毒的 Eudragit® RL 100 和 Kollidon® SR 纳米颗粒,其中负载有盐酸莫西沙星 (MOX) 的缓释,有望用于有效的眼部给药。

方法:在这项研究中,MOX 掺入是通过喷雾干燥法进行的,目的是眼部给药。用不同的方法详细评估了体外特性。

结果:通过喷雾干燥工艺成功地将 MOX 加入 Eudragit® RL 100 和 Kollidon® SR 聚合物纳米粒子中。进行粒径、zeta 电位、截留效率、颗粒形态、热、FTIR、NMR 分析和使用 HPLC 方法的 MOX 定量以评估制备的纳米颗粒。负载 MOX 的纳米粒子显示出纳米尺寸和球形,而体外释放研究显示出缓释模式,其遵循 Korsmeyer-Peppas 动力学模型。在成功将 MOX 掺入纳米粒子后,选择配方 (MOX: Eudragit® RL 100, 1:5) (ERL-MOX 2) 进行进一步研究,因为它具有更好的特性,如阳离子 zeta 电位、较小的粒径、窄尺寸分布和更均匀的缓释模式。而且,

结论:体外表征分析表明,无毒、纳米尺寸的阳离子 ERL-MOX 2 制剂具有提高眼部生物利用度的潜力。

更新日期:2021-02-18
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