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Cross-linked chitosan-dextran sulphate vehicle system for controlled release of ciprofloxaxin drug: An ophthalmic application

机译:用于环丙沙星药物控制释放的交联壳聚糖-葡聚糖硫酸盐载体系统:眼科应用

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The major challenge associated with conventional eye-drop is the rapid drug loss due to precorneal defence barrier. In this context, controlled-release system of ciprofloxacin-conjugated chitosan (CS)-Dextran sulphate (DS) nanoparticles (NPs) have been synthesized, to increase the bioavailability. The formulated drug delivery vehicle was evaluated for its therapeutic value in the simulated tear fluidat pH 7.4. Ophthalmic microbes were tested with this formulation, to confirm the drug efficacy; which showed conducive therapeutic values of both MIC and MBC. Ocular irritancy test was performed using HET-CAM test, which showed that the CS-DS system did not yield any vascular response, offering it to be a non-irritant to the ocular surface. The release studies showed monotonous controlled-release for duration of 21h. A fine cross-linking between CS and DS has been demonstrated to form CS-DS NPs and their interaction with drug has been evaluated using conventional characterization tools. Graphical abstract Through this manuscript we communicate our work done to synthesise a vehicular system for controlled release of a specific drug, Ciprofloxacin for ophthalmic application. Ciprofloxacin is an ocular drug, mainly used in the form of eye-drop, which suffers from a standard demerit of commensurate wastage of drug due to eye irritancy and tear flow. This is mainly due to drug loss at precorneal barrier. In this context, through this manuscript, we discuss a system of cross-linked particles of chitosan (CS)-Dextran sulphate, through which the drug is released in controlled fashion. Particle size analysis, structural chemistry, drug loading percentages have been carefully brought out using conventional characterization tools. The cationic polymer chitosan was cross-linked with anionic dextran sulphate sodium which significantly increased the ciprofloxacin loading efficiency (83%) and sustained release of ciprofloxacin at 21h. The formulated drug delivery vehicle has been evaluated for its therapeutic value in the simulated tear fluid at pH 7.4. Ophthalmic microbes were tested with this formulation, to confirm the drug efficacy; via the derived values of MIC and MBC. Ocular irritancy tests have been performed using HET-CAM test. The release studies showed an initial burst release and further controlled-release for duration of 21h. Display Omitted.
机译:与常规滴眼剂相关的主要挑战是由于角膜前防御屏障导致的快速药物流失。在这种情况下,已合成了环丙沙星偶联的壳聚糖(CS)-硫酸右旋糖酐(DS)纳米颗粒(NPs)的控释系统,以提高生物利用度。评价配制的药物递送载体在pH 7.4的模拟泪液中的治疗价值。用该制剂测试眼科微生物,以确认药物功效;显示出MIC和MBC的有益治疗价值。使用HET-CAM测试进行眼刺激性测试,结果表明CS-DS系统不会产生任何血管反应,从而使其对眼表无刺激性。释放研究显示21h的单调控释。已证明CS和DS之间的精细交联形成CS-DS NP,并已使用常规表征工具评估了它们与药物的相互作用。图形摘要通过本手稿,我们传达了为合成用于控释眼药的特定药物环丙沙星的车辆系统所做的工作。环丙沙星是一种眼药,主要以眼药水的形式使用,由于眼睛刺激和流泪,该药具有相应的药物浪费标准。这主要是由于角膜前屏障处的药物流失。在这种情况下,通过本手稿,我们讨论了壳聚糖(CS)-右旋糖酐硫酸盐的交联颗粒体系,通过该体系以受控方式释放药物。粒度分析,结构化学,药物载量百分比已使用常规表征工具仔细进行了估算。阳离子聚合物壳聚糖与阴离子葡聚糖硫酸钠进行交联​​,可显着提高环丙沙星的负载效率(83%)并在21h持续释放环丙沙星。已经评估了配制的药物递送载体在pH 7.4的模拟泪液中的治疗价值。用该制剂测试眼科微生物,以确认药物功效;通过MIC和MBC的推导值。使用HET-CAM测试已经进行了眼刺激测试。释放研究表明最初的爆发释放和进一步的控释持续了21h。显示省略。

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