Solid Lipid Nanoparticles for Ocular Delivery of Posaconazole: Design, Optimization and Evaluation Assay

Ali Asram Sağıroğlu
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Abstract

Extended Abstract Ocular drug delivery continues challenging due to the unique anatomic and physiological properties of the eye. Although the drugs are easily applied topically to the eye, different barriers such as the cornea, conjunctiva, blood-aqueous barrier, and blood-retinal barrier limit the reaching of the drugs to the target area [1]. In addition, due to some effective mechanisms such as blinking, tear turnover and drainage, the duration of the applied formulation in the eye area is very limited. For these reasons, drugs administered by the ocular route cannot reach the target area at the desired concentration and cannot remain in the ocular area for a sufficient period of time [2]. Conventional dosage forms cannot indicate enough efficacy since they are quickly removed from the eye surface by eyelid movements and tears [3]. Therefore, it is significant to design a suitable ocular drug delivery system to increase the bioavailability of drugs. To overcome the problem of bioavailability in ocular drug delivery, it was planned to prepare solid lipid nanoparticles (SLN) systems that are using for their penetration enhancer effect in different barriers of the eye SLN are nanometer-sized particles prepared with solid lipids at room and body temperature and stabilized with emulsifiers. The use of SLN in ocular drug delivery has been increasing in recent years thanks to its advantages such as not showing toxicity problems, having high penetration ability in different barriers of the eye, increasing the ocular bioavailability and being suitable for large-scale production In addition, SLN enables autoclave sterilization,
固体脂质纳米颗粒眼给药泊沙康唑:设计、优化和评价
由于眼睛独特的解剖和生理特性,眼部给药仍然具有挑战性。虽然药物很容易局部作用于眼睛,但角膜、结膜、血水屏障、血视网膜屏障等不同屏障限制了药物到达靶区[1]。此外,由于一些有效的机制,如眨眼,泪液周转和引流,应用配方在眼睛区域的持续时间是非常有限的。由于这些原因,经眼路给药的药物不能以理想的浓度到达靶区,也不能在眼区停留足够的时间[2]。传统的剂型不能显示足够的功效,因为它们会通过眼睑运动和眼泪迅速从眼睛表面去除[3]。因此,设计合适的眼部给药系统以提高药物的生物利用度具有重要意义。为了克服眼部给药的生物利用度问题,计划制备固体脂质纳米颗粒(SLN)系统,该系统用于在眼睛的不同屏障中发挥渗透增强作用。SLN是在室温和体温下由固体脂质制备的纳米级颗粒,并用乳化剂稳定。近年来,SLN在眼部给药中的应用越来越多,因为它具有无毒问题,在眼睛的不同屏障中具有很高的穿透能力,提高了眼部生物利用度,适合大规模生产等优点。此外,SLN可以实现高压灭菌,
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