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鉴定基于传递体的药物传递系统中无活性赋形剂相关的潜在问题。

Identifying Underlying Issues Related to the Inactive Excipients of Transfersomes based Drug Delivery System.

机构信息

Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM's NMIMS, Mumbai, India.

出版信息

Curr Pharm Des. 2021;27(7):971-980. doi: 10.2174/1381612826666201016144354.

Abstract

Transfersomes are bilayer vesicles composed of phospholipid and edge activators, which are mostly surfactant. Transfersomes based drug delivery system has gained a lot of interest of the pharmaceutical researchers for their ability to improve drug penetration and permeation through the skin. Transdermal drug delivery via transfersomes has the potential to overcome the challenge of low systemic availability. However, this complex vesicular system has different issues to consider for developing a successful transdermal delivery system. One of the major ingredients, phospholipid, has versatile sources and variable effect on the vesicle size and drug entrapment in transfersomes. The other one, termed as edge activators or surfactant, has some crucial consideration of skin damage and toxicity depending upon its type and concentration. A complex interaction between type and concentration of phospholipid and surfactant was observed, which affect the physicochemical properties of transfersomes. This review focuses on the practical factors related to these two major ingredients, such as phospholipid and surfactant. The origin, purity, desired concentration, the susceptibility of degradation, etc. are the important factors for selecting phospholipid. Regarding surfactants, the major aspects are type and desired concentration. A successful development of transfersomes based drug delivery system depends on the proper considerations of these factors and practical aspects.

摘要

传递体是由磷脂和边缘活性剂(大多为表面活性剂)组成的双层囊泡。传递体给药系统因其能够提高药物透过皮肤的渗透和穿透能力,引起了制药研究人员的极大兴趣。通过传递体经皮给药有可能克服全身生物利用度低的挑战。然而,这种复杂的囊泡系统在开发成功的经皮给药系统时需要考虑不同的问题。其中主要成分之一的磷脂具有多种来源,对囊泡大小和传递体中药物包封的影响也不同。另一种被称为边缘活性剂或表面活性剂的成分,根据其类型和浓度,对皮肤损伤和毒性有一些关键的考虑因素。磷脂和表面活性剂的类型和浓度之间存在复杂的相互作用,影响传递体的物理化学性质。本文综述了与这两种主要成分(磷脂和表面活性剂)相关的实际因素。选择磷脂时需要考虑的重要因素包括来源、纯度、所需浓度、降解的易感性等。关于表面活性剂,主要方面是类型和所需浓度。传递体给药系统的成功开发取决于对这些因素和实际方面的适当考虑。

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