Salvi Vedanti, Pawar Pravin
Department of Pharmaceutics (PG), Gourishankar Institute of Pharmaceutical Education & Research, Limb, Survey No.990, NH-4, Satara-4150415, MS, India.
Department of Pharmaceutics, Annasaheb Dange College of B Pharmacy, Ashta, Tal-Walwa, Dist. Sangli-415301, MS, India.
Pharm Nanotechnol. 2020;8(2):133-147. doi: 10.2174/2211738508666200313140902.
Bacterial conjunctivitis is a serious ocular infection if left untreated. It is caused by several species of bacteria like Pseudomonas, Staphylococcus and Mycobacterium.
The present investigation explores the development and characterization of moxifloxacin hydrochloride and ketorolac tromethamine combination loaded Eudragit RL 100 nanosuspension for ocular drug delivery in order to overcome the problems associated with conventional dosage forms.
The nanosuspension prepared by nanoprecipitation technique showed successful entrapment of both water-soluble drugs in the polymer matrix indicated by their % entrapment efficiencies.
Formulations showed a mean particle size <200 nm with narrow size distribution and positive surface charge due to the presence of quaternary ammonium groups of Eudragit RL100. FTIR study revealed compatibility among the components, while a reduction in the crystallinity of formulation was observed in the PXRD study. The release of both the drugs was found to be sustained in nanosuspension as compared to commercial eyedrops. Ex vivo studies showed increased transcorneal permeation of drugs from nanosuspension, where approximately 2.5-fold and 2-fold increase in the permeation was observed for moxifloxacin hydrochloride and ketorolac tromethamine, respectively. The formulation was stable at 4°C and room temperature.
Due to their sustained release, positive surface charge and higher transcorneal permeation, this will be a promising ocular drug delivery.
细菌性结膜炎若不治疗会成为一种严重的眼部感染。它由多种细菌引起，如假单胞菌、葡萄球菌和分枝杆菌。
本研究探索载有盐酸莫西沙星和酮咯酸氨丁三醇组合的Eudragit RL 100纳米混悬液用于眼部给药的研发及特性，以克服传统剂型相关的问题。
通过纳米沉淀技术制备的纳米混悬液显示两种水溶性药物成功包封于聚合物基质中，这由它们的包封率表明。
制剂平均粒径<200 nm，粒径分布窄，且由于Eudragit RL100季铵基团的存在而带正表面电荷。傅里叶变换红外光谱研究揭示了各成分间的相容性，而粉末X射线衍射研究中观察到制剂结晶度降低。与市售眼药水相比，纳米混悬液中两种药物的释放均为持续释放。离体研究显示纳米混悬液中药物的角膜透过性增加，其中盐酸莫西沙星和酮咯酸氨丁三醇的透过性分别增加约2.5倍和2倍。该制剂在4℃和室温下稳定。
由于其持续释放、正表面电荷和较高的角膜透过性，这将是一种有前景的眼部给药方式。
