Ethosomes, binary ethosomes and transfersomes of terbinafine hydrochloride: A comparative study

Abstract

The aim of this study was to compare the skin permeation of liposomes, transfersomes and ethosomes of lamivudine under non-occlusive conditions. The liposome and transfersomes prepared by thin film hydration method and ethosomes were prepared by slight modification on hot method. The Liposomal formulation (LP1) ethosomal formulation (ET2) and transfersomal (TF2) formulation showed highest entrapment 49.76 ± 2.1%, 81.97 ± 1.5% and 83.81 ± 1.4%, optimal nanometric size range 515 ± 4.6 nm, 374 ± 8.9nm and 315 ± 8.5nm and smallest polydispersity index0.529±0.019,0.432± 0.011 and 0.422± 0.009 respectively. The results of skin fluorescence experiments showed that penetration depth and fluorescence intensity of calcein from ethosomes and transfersomes was much greater than that from liposomes. Stability studies indicated that there was no significant physical change in vesicular formulation for 45 days at different temperatures. The in vitro result indicates that liposome retrain on the surface of skin due to poor permeation power, transfersomes improve penetrates of lamivudine and made drug easiest to accumulate in the skin. Ethosomes enhances permeation the drug to the deeper layer of skin and enter into systemic circulation rather than skin deposition. Transferosomes and ethosomes are able to cross the stratumcorneum and permeate drug to deeper tissue compare to liposomes.

Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials

“…Significant decrease in particle size from 103.7±0.9 nm to 76.3±0.5 nm was achieved when PG concentration was increased from 0% to 20% v/v. 13 Zhou et al observed that the entrapment efficiency of sophoridine, matrine, sophocarpine, and lehmanine extracted from Sophora alopecuroides increased significantly when PG was incorporated into the ethosomal system with a ratio of ethanol to PG of 1:1 (total alcohol 45%). 11 Other researchers have suggested that the presence of ethanol and PG in ethosomes provides better solubility of drugs, and hence higher entrapment efficiency and improved drug distribution throughout the vesicle.…”

“…64 It was introduced by Touitou in 1996, 5 and involves the preparation of the organic phase and aqueous phase separately. The organic phase is obtained by dissolving the phospholipids (in addition to surfactants or penetration enhancer for transethosomes) in ethanol or mixture of solvents (ethanol/PG) for the preparation of binary ethosomes, 13 at room temperature, 73 or at 30°C. 6 The aqueous phase used is either water, 44,74,75 buffer solution, 76,77 or normal saline solution.…”

“…The highest skin deposition of terbinafine was obtained in ethosomes containing ethanol:PG at a ratio of 7:3. 13 Therefore, it can be concluded that the ratio of ethanol:PG should be optimized in binary ethosomes in order to get higher drug permeation. Binary ethosomes were found to be stabler than classical ethosomes when stored at 4°C.…”

“…121 Similar findings related to this subject suggested that ethosomes are able to enhance the dermal delivery of drugs under occlusive and nonocclusive conditions. 6,13,122 ethosomal creams There have only been two studies reporting the formulation of ethosomal creams. Both of these involved the incorporation of Curcuma longa extract-loaded ethosomal systems in a cream base as a photoprotective and antiwrinkle agent.…”

“…9,11,13,20,27,140 However, few studies were continued for 1 year or more. Classical ethosome suspensions of minoxidil, testosterone, 6 and trihexyphenidyl HCl 43 were found to be stable for 2 years, while a classical ethosome gel of erythromycin was found to be stable for ~1 year.…”