Moxifloxacin loaded gelatin nanoparticles for ocular delivery: Formulation and in-vitro, in-vivo evaluation

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• 作者：Alok Mahor^a ; ^{alokmpharma@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; Sunil Kumar Prajapati^a ; Amita Verma^b ; ^{amitaverma.dr@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; Rishikesh Gupta^a ; Arun K. Iyer^c ; ^d ; Prashant Kesharwani^c ; ^{prashantdops@gmail.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Moxifloxacin ; Gelatin ; Ocular tissues ; In-vivo tolerance ; Staphylococcus aureus ; Bacillus subtilus
• 刊名：Journal of Colloid and Interface Science
• 出版年：2016
• 出版时间：1 December 2016
• 年：2016
• 卷：483
• 期：Complete
• 页码：132-138
• 全文大小：1082 K

文摘

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 ± 0.12 mV) with a narrow particle size of 175 ± 1.11 nm 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 12 h. 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.