Transfersomes: A Promising Nanoencapsulation Technique for Transdermal Drug Delivery.

Shakthi Apsara Thejani Opatha,Varin Titapiwatanakun,Romchat Chutoprapat

doi:10.3390/pharmaceutics12090855

Shakthi Apsara Thejani Opatha, Varin Titapiwatanakun + Show 1 more

Open Access

https://doi.org/10.3390/pharmaceutics12090855

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Journal: Pharmaceutics	Publication Date: Sep 9, 2020
Citations: 239	License type: CC BY 4.0

Affiliation: Chulalongkorn University

Abstract

Transdermal delivery systems have gained much interest in recent years owing to their advantages compared to conventional oral and parenteral delivery systems. They are noninvasive and self-administered delivery systems that can improve patient compliance and provide a controlled release of the therapeutic agents. The greatest challenge of transdermal delivery systems is the barrier function of the skin’s outermost layer. Molecules with molecular weights greater than 500 Da and ionized compounds generally do not pass through the skin. Therefore, only a limited number of drugs are capable of being administered by this route. Encapsulating the drugs in transfersomes are one of the potential approaches to overcome this problem. They have a bilayered structure that facilitates the encapsulation of lipophilic and hydrophilic, as well as amphiphilic, drug with higher permeation efficiencies compared to conventional liposomes. Transfersomes are elastic in nature, which can deform and squeeze themselves as an intact vesicle through narrow pores that are significantly smaller than its size. This review aims to describe the concept of transfersomes, the mechanism of action, different methods of preparation and characterization and factors affecting the properties of transfersomes, along with their recent applications in the transdermal administration of drugs.

Highlights

An efficacious, successful therapeutic treatment cannot be achieved in most cases, often due to many reasons, such as the occurrence of hepatic first-pass metabolism, adverse side effects, the rejection of invasive treatments and poor patient compliance [1]
Transfersomes are composed of phospholipids and edge activator (EA), which is a membrane-softening agent that facilitates the ultra-deformable property of the transfersomes
The results showed that transfersomes had increased the biological potency and prolonged effect, as well as the reduced therapeutic dosage [101,102]

Summary

Introduction

Successful therapeutic treatment cannot be achieved in most cases, often due to many reasons, such as the occurrence of hepatic first-pass metabolism, adverse side effects, the rejection of invasive treatments and poor patient compliance [1]. Conventional liposomes have limitations, such as the poor encapsulation efficiency of hydrophilic drugs, an unstable membrane that results in leaky behavior and a short half-life [10,11,12] These major obstacles have led to the discovery and development of other novel vesicles such as niosomes, sphingosomes, bilosomes, chitosomes, transfersomes, ethosomes and invasomes. Some ionic amphiphiles such as dicetyl phosphate (negatively charged molecule) and stearylamine (positively charged molecule) are used in the niosomes for enhancing the entrapment efficiency, efficacy and stability [14] They are identified as a better drug carrier system over liposomes due to considering factors such as a high chemical stability, high bioavailability, high entrapment efficiency and being inexpensive. It has been concluded that transfersomes may significantly improve the risk–benefit ratio of topical triamcinolone acetonide [27]

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