Abbas Muhammad Naseer, Khan Saeed Ahmad, Sadozai Sajid Khan, Khalil Islam A, Anter Asem, Fouly Marwa El, Osman Ahmed H, Kazi Mohsin
Department of Pharmacy, Kohat University of Science and Technology, Kohat 26000, Pakistan.
Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, Austin, TX 78712, USA.
Polymers (Basel). 2022 Mar 11;14(6):1135. doi: 10.3390/polym14061135.
Antibiotics delivered through conventional dosage against ophthalmic infections show lower therapeutic efficacy due to their low residence time. Therefore, there is a great need to design and develop novel dosage forms that would increase the ocular residence time of antibiotics at the site of infection. This study describes the development of nanoparticles laden in situ gelling solution, intended to sustain antibiotic release for improved therapeutic efficiency. Oxytetracycline-loaded gelatin-polyacrylic acid nanoparticles were prepared and incorporated in poloxamer-N407 solution. The rheological properties of the system were studied concerning time and temperature. Moreover, in vivo biocompatibility of the system was ascertained using the Draize test and histological studies. Finally, the optimized formulation was evaluated for in vitro antibacterial activity against one of the most common keratitis causing bacteria, . Additionally, the in vivo efficacy was evaluated on the rabbit's eye conjunctivitis model. The formulation showed a sustained effect against keratitis; furthermore, the antibacterial activity was comparable with the commercial product.
通过常规剂量给药治疗眼部感染的抗生素,由于其停留时间短,治疗效果较低。因此,迫切需要设计和开发新型剂型,以增加抗生素在感染部位的眼部停留时间。本研究描述了载于原位凝胶溶液中的纳米颗粒的开发,旨在维持抗生素释放以提高治疗效率。制备了载有土霉素的明胶-聚丙烯酸纳米颗粒,并将其掺入泊洛沙姆-N407溶液中。研究了该体系在时间和温度方面的流变学性质。此外,使用Draize试验和组织学研究确定了该体系的体内生物相容性。最后,对优化后的制剂针对一种最常见的引起角膜炎的细菌进行了体外抗菌活性评估。此外,在兔眼结膜炎模型上评估了体内疗效。该制剂对角膜炎显示出持续的效果;此外,其抗菌活性与市售产品相当。