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乙醇脂质体和传递体:原理、前景与实践

Ethosomes and Transfersomes: Principles, Perspectives and Practices.

作者信息

Garg Varun, Singh Harmanpreet, Bimbrawh Sneha, Singh Sachin Kumar, Gulati Monica, Vaidya Yogyata, Kaur Prabhjot

机构信息

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara -144411, Punjab, India.

出版信息

Curr Drug Deliv. 2017;14(5):613-633. doi: 10.2174/1567201813666160520114436.

Abstract

BACKGROUND

The success story of liposomes in the treatment of systemic infectious diseases and various carcinomas lead the scientists to the innovation of elastic vesicles to achieve similar success through transdermal route. In this direction, ethosomes and transfersomes were developed with the objective to design the vesicles that could pass through the skin. However, there is a lack of systematic review outlining the principles, method of preparation, latest advancement and applications of ethosomes and transfersomes. This review covers various aspects that would be helpful to scientists in understanding advantages of these vesicular systems and designing a unique nano vesicular delivery system.

METHODS

Structured search of bibliographic databases for previously published peer-reviewed research papers was explored and data was culminated in terms of principle of these vesicular delivery systems, composition, mechanism of actions, preparation techniques, methods for their characterization and their application.

RESULTS

A total of 182 papers including both, research and review articles, were included in this review in order to make the article comprehensive and readily understandable. The mechanism of action and composition of ethosomes and transfersomes was extensively discussed. Various methods of preparation such as, rotary film evaporation method, reverse phase evaporation method, vortex/ sonication method, ethanol injection method, freeze thaw methods, along with their advantages has been discussed. It was also discussed that both these elastic nanocarriers offer unique advantages of ferrying the drug across membranes, sustaining drug release as well as protecting the encapsulated bio actives from external environment. The enhanced bioavailability and skin penetration of ethosomes as compared to conventional vesicular delivery systems is attributed to the presence of ethanol in the bilayers while that for transfersomes accrues due to their elasticity along with their ability to retain their shape because of the presence of edge activators. Successful delivery of synthetic drugs as well as phytomedicines has been extensively reported through these vesicles.

CONCLUSION

Though these vesicular systems offer a good potential for rational drug delivery, a thoughtfully designed process is required to optimize the process variables involved. Industrial scale production of efficacious, safe, cost effective and stable formulations of both these delivery systems appears to be a pre-requisite to ensure their utility as the trans-dermal vehicles.

摘要

背景

脂质体在治疗全身性传染病和各种癌症方面的成功促使科学家们创新出弹性囊泡,以期通过透皮途径取得类似的成功。在此方向上,乙醇脂质体和传递体得以开发,目的是设计出能够穿透皮肤的囊泡。然而,目前缺乏对乙醇脂质体和传递体的原理、制备方法、最新进展及应用的系统综述。本综述涵盖了各个方面,有助于科学家理解这些囊泡系统的优势,并设计出独特的纳米囊泡递送系统。

方法

对文献数据库进行结构化检索,以查找先前发表的同行评审研究论文,并根据这些囊泡递送系统的原理、组成、作用机制、制备技术、表征方法及其应用对数据进行汇总。

结果

为使本文内容全面且易于理解,共纳入了182篇包括研究论文和综述文章在内的文献。文中广泛讨论了乙醇脂质体和传递体的作用机制及组成。探讨了多种制备方法,如旋转薄膜蒸发法、反相蒸发法、涡旋/超声法、乙醇注入法、冻融法及其优点。还讨论了这两种弹性纳米载体在跨膜运载药物、维持药物释放以及保护包封的生物活性物质免受外部环境影响方面具有独特优势。与传统囊泡递送系统相比,乙醇脂质体的生物利用度和皮肤渗透性增强归因于双层膜中乙醇的存在,而传递体的这一特性则源于其弹性以及由于边缘活化剂的存在而保持形状的能力。通过这些囊泡已广泛报道了合成药物以及植物药的成功递送。

结论

尽管这些囊泡系统在合理药物递送方面具有良好潜力,但需要精心设计流程以优化所涉及的工艺变量。对这两种递送系统进行有效、安全、经济且稳定的制剂的工业规模生产似乎是确保其作为透皮载体实用化的先决条件。

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