Transfersomes: a novel technique for transdermal drug delivery

Chaurasiya, Priyanka; Ganju, Eisha; Upmanyu, Neeraj; Ray, Sudhir Kumar; Jain, Prabhat

doi:10.22270/jddt.v9i1.2198

Cited by 72 publications

(48 citation statements)

References 17 publications

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“…The prepared suspension is subsequently mixed with buffer to yield a total lipid concentration. The resulting formulation is then sonicated, frozen and thawed respectively two to three times [ 1 , 49 ].…”

Section: Preparation Methodsmentioning

confidence: 99%

“…The resulting vesicles are swollen at room temperature. The obtained multilamellar lipid vesicles are further sonicated at room temperature [ 1 ].…”

Section: Preparation Methodsmentioning

confidence: 99%

“…They efficiently penetrate through the intact skin if applied under nonocclusive conditions; this specific nonocclusive state of the skin is required mainly to initiate a transepidermal osmotic gradient across the skin [ 1 , 54 ]. According to the study done by Cevc and Blume, hydrotaxis (xerophobia) is the permeation mechanism of transfersomes, which is further described as the transferosome’s moisture-seeking tendency towards deeper skin layers rather than dry outer background due to the state of moisture evaporation from the transfersomal formulation following its application on the skin (nonocclusive condition) [ 65 ].…”

Section: Mechanism Of Actionmentioning

confidence: 99%

“…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 ]. Therefore, several drug delivery systems have been developed and studied over the past decades to overcome these problems.…”

Section: Introductionmentioning

confidence: 99%

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Transfersomes: A Promising Nanoencapsulation Technique for Transdermal Drug Delivery

2020

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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.

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Section: Preparation Methodsmentioning

confidence: 99%

“…The resulting vesicles are swollen at room temperature. The obtained multilamellar lipid vesicles are further sonicated at room temperature [ 1 ].…”

Section: Preparation Methodsmentioning

confidence: 99%

Section: Mechanism Of Actionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Transfersomes: A Promising Nanoencapsulation Technique for Transdermal Drug Delivery

2020

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“…Transferosomes are recently used as carriers for the controlled and targeted delivery of drugs as proteins, peptides, hormones. 8 Cinnarizine is indicated for the treatment of the symptoms of Ménière's syndrome as vertigo. 9 Moreover, it improves the cerebral vascularization and relieves the migraine symptoms.…”

Section: Introductionmentioning

confidence: 99%

<p>Formulation and Characterization of Cinnarizine Targeted Aural Transfersomal Gel for Vertigo Treatment: A Pharmacokinetic Study on Rabbits</p>

Abdelmonem¹,

Hamed²,

Abdel-Halim³

et al. 2020

IJN

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Introduction and Aim: Cinnarizine is indicated orally for treating vertigo associated with Ménière's syndrome and has a local anesthetic effect as well. The present study aims to develop an aural Cinnarizine mucoadhesive transfersomal gel to overcome the first-pass metabolism. Methods: Eighteen Cinnarizine transfersomes were prepared by the thin-film hydration technique using different types of phosphatidylcholine and edge activators in different ratios. Formulae were tested for their appearance, entrapment efficiency, and in-vitro drug release after eight hours. F1, F4, F7, F9, F10, and F12 were selected to be examined for particle size, polydispersity index, and zeta potential. According to the previous parameters, F1 and F10 were incorporated into gels using different polymers according to factorial design 23. The eight gels were tested for appearance, pH, mucoadhesion, spreadability, drug content, in-vitro drug release after eight hours, and rheology. The transfersomal gel F1A was subjected to FTIR analysis and in-vivo pharmacokinetic study. Results: The transfersomal dispersion colors were ranging between the white and yellow. Their EE % ranged from 64.36±1.985% to 94.09±1.74%, and their in-vitro release percentages were between 61.82±1.92% and 95.92±1.18%. Also, the vesicles PS ranged from 212.3 ±30.05nm to 2150±35.35nm, DI from 0.238±0.134 to 1±0.00 and zeta potential from −57.5 ±2.54 to +4.73±1.57 mV. The transfersomal gels showed pseudoplastic behavior, pH range of 5.5 to 8, a mucoadhesive force of 169.188±1.26 to 321.212±6.94 (dyne/cm 2 ×10 2), spreadability of 40 ±7.03mm to 138 ±3.77mm, and in-vitro drug release of 81.63±1.128% to 97.78 ±0.102%. The IR spectra of the (drug-excipients) physical mixture revealed that there were no shifts of incompatibility. The in-vivo pharmacokinetic study illustrated that [AUC] 0-24 of F1A was significantly higher than that of tablets at (P< 0.05), equivalent to 703.563±26.470 and 494.256±9.621ɲg.hr/mL respectively. Conclusion: The study revealed that Cinnarizine aural mucoadhesive targeted delivery provides an improved systemic bioavailability over the conventional oral route.

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Ethosomes as Promising Transdermal Delivery Systems of Natural‐Derived Active Compounds

Emanet¹,

Ciofani²

2023

Advanced NanoBiomed Research

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Ethosomes are novel lipid‐based vesicular systems that demonstrate unique improvements in drug delivery with respect to other nanoparticles, especially for transdermal applications. Their high ethanol content strongly improves flexibility and deformability, which allows squeezing through the intercellular spaces without any drug leakage. The ethanol, moreover, contributes to increase the fluidity of the lipids of the cell membranes in dermal layers, allowing an in‐depth penetration of the nanostructures. Moreover, the high ethanol content of ethosomes allows the promotion of the encapsulation of either hydrophilic or lipophilic active agents, a feature particularly useful when it deals with natural extracts, a family of compounds characterized by a huge chemical variability. As a further advantage, being natural extracts often obtained in ethanol‐based solutions, their incorporation in ethosomes makes not necessarily expensive and time‐consuming procedures finalized at solvent removal. Following the initial exploitation of ethosomes, research focuses on the development of variants such as invasomes and transethosomes, which show improved drug encapsulation and delivery capacity. This review provides the state‐of‐the‐art on ethosomal research, with special attention on the encapsulation and delivery of natural extracts and their transdermal delivery.

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Transfersomes: a novel technique for transdermal drug delivery

Cited by 72 publications

References 17 publications

Transfersomes: A Promising Nanoencapsulation Technique for Transdermal Drug Delivery

Transfersomes: A Promising Nanoencapsulation Technique for Transdermal Drug Delivery

<p>Formulation and Characterization of Cinnarizine Targeted Aural Transfersomal Gel for Vertigo Treatment: A Pharmacokinetic Study on Rabbits</p>

Ethosomes as Promising Transdermal Delivery Systems of Natural‐Derived Active Compounds

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