Enhanced transdermal bioavailability of testosterone propionate via surfactant-modified ethosomes

Meng, Siwei; Chen, Zaixing; Yang, Liqun; Zhang, Wei; Liu, Danhua; Guo, Jing; Yanmin, Guan; Li, Jianxin

doi:10.2147/ijn.s46748

Cited by 53 publications

(22 citation statements)

References 25 publications

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“…Many researchers have reported superior properties of transethosomes over classical ethosomes. [17][18][19][20][21][22][23][24][25][26][27][28][29][30] Different types of edge activators and penetration enhancers have been investigated to produce ethosomal systems with better characteristics. Transethosomes were reported to entrap drugs with molecular weights ranging from 130.077 Da to 200-325 kDa.…”

Section: Transethosomesmentioning

confidence: 99%

“…It was noted that the addition of only 0.2% w/w of hexadecyltrimethylammonium bromide was sufficient to change the ζ-potential of ethosomal system. 20 They suggested that this positively charged ζ-potential may enhance the skin-permeation properties of the ethosomal system, due to attraction with the negatively charged skin surface.…”

Section: Hexadecyltrimethylammonium Bromidementioning

confidence: 99%

“…It was found to reduce vesicular size and to increase the solubility of the drug and entrapment efficiency. 20 Shen et al used Cremophor RH-40 in the formulation of transethosomes of artesunate and febrifugine; however, the vesicles were unstable and needle crystals had formed after 5 days. 27 …”

Section: Cremophormentioning

confidence: 99%

“…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.…”

mentioning

confidence: 99%

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

Abdulbaqi

Darwis

Khan

et al. 2016

IJN

282

179

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Ethosomal systems are novel lipid vesicular carriers containing a relatively high percentage of ethanol. These nanocarriers are especially designed for the efficient delivery of therapeutic agents with different physicochemical properties into deep skin layers and across the skin. Ethosomes have undergone extensive research since they were invented in 1996; new compounds were added to their initial formula, which led to the production of new types of ethosomal systems. Different preparation techniques are used in the preparation of these novel carriers. For ease of application and stability, ethosomal dispersions are incorporated into gels, patches, and creams. Highly diverse in vivo models are used to evaluate their efficacy in dermal/transdermal delivery, in addition to clinical trials. This article provides a detailed review of the ethosomal systems and categorizes them on the basis of their constituents to classical ethosomes, binary ethosomes, and transethosomes. The differences among these systems are discussed from several perspectives, including the formulation, size, ζ-potential (zeta potential), entrapment efficiency, skin-permeation properties, and stability. This paper gives a detailed review on the effects of ethosomal system constituents, preparation methods, and their significant roles in determining the final properties of these nanocarriers. Furthermore, the novel pharmaceutical dosage forms of ethosomal gels, patches, and creams are highlighted. The article also provides detailed information regarding the in vivo studies and clinical trials conducted for the evaluation of these vesicular systems.

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Section: Transethosomesmentioning

confidence: 99%

Section: Hexadecyltrimethylammonium Bromidementioning

confidence: 99%

Section: Cremophormentioning

confidence: 99%

mentioning

confidence: 99%

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

Abdulbaqi

Darwis

Khan

et al. 2016

IJN

282

179

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“…The quantity of surfactant in artesunate-loaded ethosomes was another important factor that affected the particle size and EE. 31,32 By introducing Tween 80 into the ethosomes, the particle size and EE of ethosomes decreased little by little (Figure 3). The Tween 80 in lipid vesicles could increase the fluidity of the membrane structure and soften the membrane structure.…”

Section: The Effects Of Phospholipid and Surfactant On Artesunate-loamentioning

confidence: 99%

Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement

Shen¹,

Liu²,

Zhang³

et al. 2015

IJN

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Malaria is still a serious public health problem in some parts of the world. The problems of recurrence and drug resistance are increasingly more serious. Thus, it is necessary to develop a novel antimalarial agent. The objectives of this study were to construct a novel compound antimalarial transdermal nanosystem–ethosomal cataplasm, to investigate its characteristics and efficiency, and to systematically explore the penetration-enhancing mechanisms of ethosomal cataplasm. Artesunate-loaded ethosomes and febrifugine-loaded ethosomes were prepared, and their characteristics were evaluated. Drug-loaded ethosomes were incorporated in the matrix of cataplasm to form the compound antimalarial ethosomal cataplasm. With the help of ethosomal technology, the accumulated permeation quantity of artesunate significantly increased at 8 hours after administration, which was 1.57 times as much as that of conventional cataplasm. Soon after administration, the ethosomal cataplasm could make a large quantity of antimalarial drug quickly penetrate through skin, then the remaining drug in the ethosomal cataplasm could be steadily released. These characteristics of ethosomal cataplasm are favorable for antimalarial drugs to kill Plasmodium spp. quickly and prevent the resurgence of Plasmodium spp. As expected, the ethosomal cataplasm showed good antimalarial efficiency in this experiment. The negative conversion rates were 100% and the recurrence rates were 0% at all dosages. The mechanism of penetration enhancement of the ethosomal cataplasm was systematically explored using an optics microscope, polarization microscope, and transmission electron microscopy. The microstructure, ultrastructure, and birefringent structure in skin were observed. Data obtained in this study showed that the application of ethosomal technology to antimalarial cataplasm could improve the transdermal delivery of drug, enhance the efficacy, and facilitate practical application in clinic.

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Nanotechnology‐Based Applications for Transdermal Delivery of Therapeutics

Yellepeddi

Donnelly

Singh

2015

Novel Delivery Systems for Transdermal and Intradermal Drug Delivery

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Enhanced transdermal bioavailability of testosterone propionate via surfactant-modified ethosomes

Cited by 53 publications

References 25 publications

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

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

Compound antimalarial ethosomal cataplasm: preparation, evaluation, and mechanism of penetration enhancement

Nanotechnology‐Based Applications for Transdermal Delivery of Therapeutics

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