Tamarind seed polysaccharide (TSP) uses in ophthalmic drug delivery

Matheus Augusto de Castro, Wallace Mateus Prata, A. Silva-Cunha
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引用次数: 1

Abstract

author: matheuscastro123@hotmail.com Abstract At present, ophthalmic drug delivery remains a major challenge, given the eye's protective structure and susceptibility to irritation, resulting in poor patient adherence. In order to overcome these constraints, new formulations are continually being developed. The inclusion of Galactoxyloglucan (Tamarind seed polysaccharide (TSP) in such formulations, a natural substance extracted from the seeds of Tamarindus indica , has shown great potential due to its physicochemical properties, high biocompatibility and safety profile. Such properties, have led to its use in formulations for the treatment of dry eye disease, glaucoma, and bacterial keratitis, as well as in dilating eye drops used in eye examinations. In this article, we highlight the most recent TSP-based ophthalmologic formulations, which indicate that this polymer is a strong candidate to reduce adverse effects, improve patient tolerability and rufloxacin administration resulted in slightly higher intraocular drug levels than rufloxacin alone, as shown by the values observed in uninfected (4.62 g/ml; P 0.01), P. aeruginosa -infected (5.63 g/ml; P 0.01), and S. aureus-infected (6.91 g/ml; P 0.001) eyes. In the cornea, TSP-rufloxacin was slightly more effective than rufloxacin alone in regulating P. aeruginosa bacterial proliferation. With regard to S. aureus, TSP-rufloxacin administration resulted in a significant drop in corneal bacteria relative to both rufloxacin-treated and ofloxacin-treated eyes (P 0.05). A further study was conducted evaluating different formulations of rufloxacin (RUF) with TSP, namely two pH 7.2 suspensions of non-salified rufloxacin base, one of which was thickened with TSP; two pH 7.2 solutions of RUF obtained using hydroxypropyl- β cyclodextrin (CD), one with TSP; and two pH 5.0 solutions of rufloxacin hydrochloride (RUF-HCl), one containing TSP 33 . In this study, the suspension containing TSP showed twice the concentration in aqueous humor compared to S-RUF (187.88 vs 67.63 min µg/mL), given the viscosity potential of the polysaccharide. Additionally, pH levels were also shown to influence drug concentration, since the concentration was higher at pH 7.2 when compared to the same formulation at pH 5.0. Rufloxacin solubilization in HP- β -CD (pH 7.2) irrespective of whether or not it contained TSP, showed, poor performance in the final concentration. This could be explained by the fact that the drug interacted strongly with the cyclodextrins and that
罗望子多糖(TSP)用于眼科给药
摘要目前,由于眼睛的保护结构和对刺激的易感性,导致患者依从性差,眼科给药仍然是一个重大挑战。为了克服这些限制,人们不断开发新的配方。半乳糖葡聚糖(罗望子籽多糖)是一种从罗望子种子中提取的天然物质,由于其理化性质、高生物相容性和安全性,在该配方中具有很大的应用潜力。这种特性导致其用于治疗干眼病、青光眼和细菌性角膜炎的配方,以及用于眼科检查的扩张眼药水。在本文中,我们重点介绍了最新的基于tsp的眼科配方,这些配方表明该聚合物是减少不良反应,提高患者耐受性的强候选物,并且鲁氟沙星给药导致比单独使用鲁氟沙星略高的眼内药物水平,如在未感染的患者中观察到的值(4.62 g/ml;P < 0.01),铜绿假单胞菌感染(5.63 g/ml;金黄色葡萄球菌感染(6.91 g/ml;P 0.001)。在角膜中,tsp - ruflo沙星对铜绿假单胞菌细菌增殖的调节效果略高于单独使用ruflo沙星。对于金黄色葡萄球菌,tsp - ru氟沙星治疗组与氧氟沙星治疗组相比,角膜细菌数量显著下降(P < 0.05)。进一步研究了ru氟沙星(ru氟沙星)与TSP的不同配方,即两种pH为7.2的非乳化ru氟沙星碱混悬液,其中一种用TSP增稠;用羟丙基- β环糊精(CD)制备两种pH值为7.2的RUF溶液,一种用TSP;盐酸茹氟沙星溶液(RUF-HCl)两份pH 5.0溶液,其中一份含有tsp33。在本研究中,考虑到多糖的黏度电位,含有TSP的悬浮液的浓度是S-RUF的两倍(187.88 vs 67.63 minµg/mL)。此外,pH水平也显示影响药物浓度,因为与pH为5.0的相同配方相比,pH为7.2的浓度更高。在HP- β - cd (pH 7.2)中,无论是否含有TSP,鲁氟沙星的增溶效果都不理想。这可以用药物与环糊精的强烈相互作用来解释
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