Mahor Alok, Prajapati Sunil Kumar, Verma Amita, Gupta Rishikesh, Iyer Arun K, Kesharwani Prashant
Institute of Pharmacy, Bundelkhand University, Jhansi, India.
Institute of Pharmacy, Bundelkhand University, Jhansi, India.
J Colloid Interface Sci. 2016 Dec 1;483:132-138. doi: 10.1016/j.jcis.2016.08.018. Epub 2016 Aug 10.
The current research focuses on developing positively charged gelatin nanoparticles loaded with moxifloxacin for its effective ocular delivery and controlled release in corneal eye layer. We selected type A gelatin because of its biodegradable and non-toxic nature as the polymer of choice for fabricating the nanoparticles by a modified two step desolvation technique. The produced nanoparticles were positively charged (+24±0.12mV) with a narrow particle size of 175±1.11nm as measured by dynamic light scattering (DLS). The in-vitro drug release from the nanoformulations exhibited a burst effect in the first hour followed by a controlled release of the drug for the subsequent 12h. The Korsmeyer-Peppas model showed better linearity and the formulations displayed non-Fickian drug release pattern. The optimized formulation was assessed for its utility as an anti-bacterial agent and its effectiveness was tested on the corneal eye surface of rabbits. The in-vivo tolerance tests revealed that the drug loaded nano-formulations was non-irritant to the ocular tissues indicating its safety. The in-vivo anti-bacterial activity of the nanosuspension was more effective against S. aureus than the commercially market product, MoxiGram®. Microbiological efficacy assessed against B. subtilus using cup-plate method suggested that our fabricated nanosuspension possess better anti-microbial activity as compared to the commercial agent, MoxiGram® revealing promising potentials for the currently developed gelatin based nanoformualtions.
当前的研究聚焦于开发负载莫西沙星的带正电荷明胶纳米颗粒,以实现其在眼角膜层的有效眼部递送和控释。我们选择A型明胶,因其具有可生物降解和无毒的特性,作为通过改良的两步去溶剂化技术制备纳米颗粒的首选聚合物。通过动态光散射(DLS)测量,所制备的纳米颗粒带正电荷(+24±0.12mV),粒径狭窄,为175±1.11nm。纳米制剂的体外药物释放最初1小时呈现突释效应,随后12小时为药物的控释。Korsmeyer-Peppas模型显示出更好的线性,并且制剂呈现非Fickian药物释放模式。对优化后的制剂作为抗菌剂的效用进行了评估,并在兔眼角膜表面测试了其有效性。体内耐受性测试表明,载药纳米制剂对眼组织无刺激性,表明其安全性。纳米混悬液对金黄色葡萄球菌的体内抗菌活性比市售产品MoxiGram®更有效。使用杯碟法对枯草芽孢杆菌进行的微生物学功效评估表明,与市售药剂MoxiGram®相比,我们制备的纳米混悬液具有更好的抗菌活性,这揭示了当前开发的基于明胶的纳米制剂具有广阔的应用前景。