眼睛给药:特别提到纳米颗粒

Swarnali Das, Preeti K. Suresh
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引用次数: 38

摘要

随着新的、更有效的药物和生物反应调节剂的出现,眼科药物的控制和持续递送仍然是制药药物递送领域的一个主要重点领域,这些药物的生物半衰期可能也很短。临床治疗的主要目的是在作用部位提供和维持足够的药物浓度。在眼部给药过程中,由于眼部保护机制的生理限制,导致药物的吸收较差,只有极少部分的药物能穿透角膜到达眼内组织。眼睛的解剖、生理和生物化学使这个器官对外来物质具有高度的抵抗力。配方师面临的一个重大挑战是在不造成永久性组织损伤的情况下绕过眼睛的保护屏障。更新,更灵敏的诊断技术和新的治疗药物的发展继续提供高疗效的眼部输送系统。传统的眼液、悬浮液和药膏剂型不再是这些适应症的最佳治疗方法。与传统的递送系统相比,纳米颗粒和纳米悬浮液显示出更好的应用。据报道,聚合物纳米颗粒对角膜、虹膜和结膜没有任何刺激作用,因此似乎是眼科药物递送的合适惰性载体。以纳米颗粒悬浮液形式使用药物的好处是:减少剂量,延长药物释放时间,提高感染组织中的药物浓度,延长纳米颗粒在角膜表面的停留时间,降低药物的全身毒性。关键词:纳米;聚合物;眼;生物利用度
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Drug delivery to eye: Special reference to nanoparticles
Controlled and sustained delivery of ophthalmic drugs continues to remain a major focus area in the field of pharmaceutical drug delivery with the emergence of new, more potent drugs and biological response modifiers that may also have very short biological half-lives. The major objective of clinical therapeutics is to provide and maintain adequate concentration of drugs at the site of action. In ocular drug delivery, the physiological constraints imposed by the protective mechanisms of the eye lead to poor absorption of drugs with very small fractions of the instilled dose penetrating the cornea and reaching the intraocular tissues. The anatomy, physiology, and biochemistry of the eye render this organ highly impervious to foreign substances. A significant challenge to the formulator is to circumvent the protective barriers of the eye without causing permanent tissue damage. Development of newer, more sensitive diagnostic techniques and novel therapeutic agents continue to provide ocular delivery systems with high therapeutic efficacy. Conventional ophthalmic solution, suspension, and ointment dosage forms no longer constitute optimal therapy for these indications. Nanoparticles and nanosuspensions are showing a better application as compare to conventional delivery sysyems. Polymer nanoparticles proposed are reported to be devoid of any irritant effect on cornea, iris, and conjunctiva and thus appear to be a suitable inert carrier for ophthalmic drug delivery. The benefits of having the drug in the form of a nanoparticulate suspension are: reduction in the amount of dose, drug release for a prolonged period of time, higher drug concentrations in the infected tissue, longer residence time of nanoparticles on the cornea surface, reduction systemic toxicity of drug. Keywords: Nanoparticle; polymer; ocular; bioavailability
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