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转脂体:高效透皮给药的革命性纳米系统。

Transfersomes: a Revolutionary Nanosystem for Efficient Transdermal Drug Delivery.

机构信息

Department of Pharmacy, Quaid-i-Azam University, Islamabad, 45320, Pakistan.

School of Pharmaceutical Sciences of Wenzhou Medical University, Wenzhou, People's Republic of China.

出版信息

AAPS PharmSciTech. 2021 Dec 1;23(1):7. doi: 10.1208/s12249-021-02166-9.

Abstract

Transdermal delivery system has gained significance in drug delivery owing to its advantages over the conventional delivery systems. However, the barriers of stratum corneum along with skin irritation are its major limitations. Various physical and chemical techniques have been employed to alleviate these impediments. Among all these, transfersomes have shown potential for overcoming the associated limitations and successfully delivering therapeutic agents into systemic circulation. These amphipathic vesicles are composed of phospholipids and edge activators. Along with providing elasticity, edge activator also affects the vesicular size and entrapment efficiency of transfersomes. The mechanism behind the enhanced permeation of transfersomes through the skin involves their deformability and osmotic gradient across the application site. Permeation enhancers can further enhance their permeability. Biocompatibility; capacity for carrying hydrophilic, lipophilic as well as high molecular weight therapeutics; deformability; lesser toxicity; enhanced permeability; and scalability along with potential for surface modification, active targeting, and controlled release render them ideal designs for efficient drug delivery. The current review provides a brief account of the discovery, advantages, composition, synthesis, comparison with other cutaneous nano-drug delivery systems, applications, and recent developments in this area.

摘要

经皮给药系统因其优于传统给药系统的优势,在药物传递中具有重要意义。然而,角质层的障碍以及皮肤刺激是其主要的局限性。已经采用了各种物理和化学技术来减轻这些障碍。在所有这些方法中,传递体显示出克服相关限制并成功将治疗剂递送到全身循环的潜力。这些两亲性囊泡由磷脂和边缘活性剂组成。边缘活性剂除了提供弹性外,还影响传递体的囊泡大小和包封效率。传递体通过皮肤增强渗透的背后机制涉及它们的变形性和在应用部位的渗透梯度。渗透增强剂可以进一步提高它们的渗透性。生物相容性;携带亲水性、亲脂性以及高分子量治疗剂的能力;变形性;较小的毒性;增强的渗透性;可扩展性以及表面改性、主动靶向和控制释放的潜力使它们成为高效药物传递的理想设计。本综述简要介绍了传递体的发现、优势、组成、合成、与其他皮肤纳米药物传递系统的比较、应用以及该领域的最新进展。

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