Transethosomes: Utilization in Novel Drug Delivery System

 

Rani Mishra, Kamlesh Dashora, Praveen Khirwadkar, Tanu Bhargava

Institute of Pharmacy, Vikram University, Ujjain (M.P.) Pin 456010.

*Corresponding Author E-mail: hanumanaleauf002@gmail.com

 

ABSTRACT:

The stratum Corneum which is believed to work as a barrier for drug delivery. The transdermal route is one of the most popular ways to administer medication because of its easy permeability.  The novel- vesicular carrier among them which has the ability to penetrate the stratum corneum.  Vesicular carrier include liposomes, Niosomes, transferosomes, ethosomes and Transethosomes. Transethosomes   are more effective as compared to ethosomes and transferosomes because it contain more amount of ethanol with edge activator which increase the stratum corneum permeation. In this article reviewed detail about advantage and disadvantage, methods of preparation and evaluation of Transethosomes and various works which are done in Transethosomes in the treatment of various kinds of diseases.

 

KEYWORDS: Transdermal drug delivery, Vesicular Nano- Carrier, Transethosomes.

 

 


INTRODUCTION:

Oral administration is presently the most common way of medicine delivery. While this has the advantage of being simple to administer, it also has a number of drawbacks, including poor bioavailability due to hepatic metabolism (first pass) and the potential for rapid blood level spikes (both high and low), necessitating high and/or frequent dosing, which can be both costly and inconvenient. Continuous intravenous infusion is seen to be a superior mode of drug administration, not only because it avoids hepatic “first pass” metabolism, but also because it keeps the drug level in the body steady and long-lasting1. Skin is regarded as the largest organ of the human body. From a pharmaceutical point of view, it offers advantages over other routes of administration, including avoidance of the first-pass metabolism, smaller fluctuations in plasma drug levels for repeated administration, and good patient compliance2.

 

 

Transdermal route is considered as patient friendly as various gastrointestinal side effects of oral drugs can be avoided by choosing this delivery path. This route of drug delivery is capable to maintain therapeutically effective concentration of the drug in the body for prolonged time periods by avoiding first pass effect3. Transdermal drug delivery is the movement of drug formulation from the healthy and intact stratum corneum layer of skin to the systemic circulation of the body4.

 

Vesicular Nano- Carrier:

Stratum corneum or horny layer of the skin represents the challenging barrier that does not permit the crossing of most of the drugs, except lipophilic drugs and those with low molecular weight. Vesicular Nano-carrier or ultra-deformable vesicles (UDV) recently represent a promising approach for the advanced and improved transdermal delivery of drugs. Deformable vesicles like Transethosomal formulations show the advantages of being nontoxic and stable thermodynamically. Deformable vesicles have been used as a tool for dermal and transdermal delivery of many substances like peptides and proteins. Also, their production is very simple and easy to scale up5. Currently, there are various types of UDV that have been successfully developed for both pharmaceuticals and cosmeceuticals, particularly transferosomes, ethosomes, and, more recently, transethosomes6.

Transethosomes:

Liposomal carriers have been studied for transdermal drug delivery since the 1980s. Conventional liposomes (CLs) show drawback of less permeation into the deeper region of skin and they accumulate at the outer layer of stratum corneum7. So, new classes of liposomes like deformable liposomes (DLs) and ethosomes (ELs) came into   existence later on8. DLs are also recognised as ‘Transferosomes’ and they are the liposomes having addition of edge activator like span 60, span 25, span 80, tween 20, tween 60, tween 80, sodium deoxy-cholate, and sodium cholate9.  Transferosomes show more effective Transdermal delivery compared to CLs due to their high flexibility because of the presence of edge activators in them10. Transferosomes improve skin deposition of many drugs, however, they can’t reach the stratum corneum deep enough11. On the other hand, ethosomal systems were introduced in 1998 containing high levels of ethanol in their formula, which resulted in improved drug absorption through the skin due to the result of ethanol mixing in lipid bilayer vesicles and enhancing saturation of SC lipids12. Transethosomes are recent vesicular Nano-carrier systems that have the advantages of both transferosomes and ethosomes13.

 

 

 Figure: Composition of Transethosomes

 

Mechanism of Transethosomes

Transethosomes are a novel lipid formulation that contains phospholipids, high-concentration ethanol (30–40%), edge activators such tween 20/60/80, span 60/65/80, sodium cholate or sodium deoxy-cholate, and water. As they indicate, both ethosomes and transferosomes have advantages. The size varies from 40 nm to 200 nm, depending on the medicine. The presence of ethanol separates the Transethosomal system from other vesicular systems14. It is thought that the first part of mechanism is due to ‘ethanol effect’, whereby intercalation of the ethanol into intercellular lipids increasing lipid fluidity and decreases the density of the lipid bilayer. Lipid layer of stratum corneum is fluidized by impact of ethanol and its high concentration in Transethosomes that promote malleability and flexibility of these systems enhancing their penetration through tiny openings formed in stratum corneum due to fluidization. Alcohol amount in vesicular system also control its diameter as it provides net negative charge to vesicle surface reducing its size. 30-40% is optimum concentration range of ethanol for the formation of stable ethosomes. Reducing ethanol concentration to 20% may lead to increase in vesicular size. Phospholipids have an integral role in bilayer formation; consisting of hydrophilic head and hydrophobic tail15.

 

 

Figure:  Mechanism of penetration

 

Advantage of Transethosomes:

1.    The Transethosomal system is passive, non-invasive and is available for immediate commercialization16.

2.    It contains non-toxic raw materials in the formulation16.

3.    The Transethosomes drug is administered in a semisolid form16.

4.    This drug delivery system shows better stability as compared to other conventional vesicle17.

5.    Unlike deformable liposomes, Transethosomes improve medicine delivery to the skin in both occlusive and non-occlusive circumstances.

6.    This is a straightforward method of medication delivery compared to iontophoresis, laser surgery, cryosurgery, and other sophisticated procedures18.

 

Disadvantage of Transethosomes:                                   

·         Loss of product during the transfer from alcoholic and water media.

·         Skin irritation or allergic reaction on so it’s not suitable for patients with allergic dermatitis19.

·         The drug should be of a reasonable molecular size to be absorbed percutaneously20.

·         Sensitivity to light leads to degradation, so, antioxidants such as α-tocopherol are added to the formulation5.

·         The molecular size of the drug should be reasonable that it should be absorbed percutaneously5.

 

Methods of preparation of Transethosomes:

1.     Hot Method:

Phospholipid dispersed in water and heated in a water bath up to 40ºC to get a colloidal solution. Ethanol and glycol mixture maintained at temperature 40ºC. The phase that contains ethanol and glycol is added to the aqueous phase—stirring for 7–10minutes. According to the hydrophilic or hydrophobic properties, the drug can be dissolved in water/ethanol. Temperature is kept at 40ºC throughout the procedure. The size of the Transethosomes is reduced by sonication13.

 

2.     Cold Method:

Phospholipid is dissolved in ethanol as solvent system by vigorous shaking. This mixture is heated up to 30°c in a water bath. Water is heated in a separate vessel up to 30°c and added to the alcoholic mixture slowly.  During addition of aqueous solution to ethanolic solution magnetic stirrer is used for uniform mixing (700rpm). Probe sonicator can be used in order to modulate the size of vesicles21:

 

3 Mechanical Dispersion Method:

Round Bottom flask is used in this technique, Liquid and surfactant mixture is dissolved in ethanol. Efficiency of this technique can be enhanced by combination of hydrated thin film and ultrasound homogenization. Using rotary evaporator thin lipid film can be produced, the excess of organic solvent can be removed by keeping it overnight under vacuum. 10%v/v ethanol in phosphate buffer (6.5pH) atm 60rpm is used in hydration process. Sonication technique can be employed to modify the vesicular size5.

 

4 Reverse Phase Evaporation:

Lipid is dissolved in ethanol; edge activators are added to aqueous phase. Aqueous phase is added into organic phase, and ultra-sonication technique is used in separation of two phases at 0°c. Formation of gel occurs under pressure upon removal of organic solvent22.

 

Review Of literature:

List of recently reported literature for various types of Transethosomes which are used for the drug delivery of different types of diseases included anti-cancer, anti-arthritis, anti-diabetic, Gout, anti-inflammatory, NSAIDs, anti-hypertensive. 


 

S. No

Drug Utilized

Description

Outcomes

Conclusion

Ref.

1.

Propranolol hydrochloride

(B- blocker) 

Developed and Characterized Transethosomes by utilizing homogenization method using Lipoid s100 as phospholipid and oleic acid as permeation enhancers.

Transethosomes showed acceptable size, high drug entrapment, and good colloidal characteristics, and have prolonged in vitro release up to 24h.  The value of peak plasma conc. Of drug is high as compared to marketed oral tablet

Result showed that The transdermal patch of drug could better alternative to oral as it can avoid various disadvantage of drug like dose frequency first pass effect and organ toxicity

 

23

2.

Glibenclamide (Anti -diabetics)

Transethosomes patch formulated   and evaluated   by utilizing solvent evaporation technique using HPMC and PVP as matrix polymer.

Transethosomes patch showed significantly results in moisture content, drug content, and drug release

Patch showed evaluation results and show stable during its stability study

24

3.

Sinapic acid

(anti-cancer,

Antioxidants, anti- inflammatory)

Prepared and Characterized   Transethosomes by thin film hydration method

Transethosomes   surface Morphology showed smooth and spherical vesicles.it also showed enhanced antioxidant activity. greater penetration across membrane during the study.

Result showed that the prepared Transethosomes are able to penetrate the entrapped drug in higher concentration.so it is concluded that Transethosomes based approaches useful in penetrating the drug across the skin.

25

4.

Diflunisal

(NSAIDs)

Formulated   and Characterized   Diflunisal Transethosomes by varying the types and concentration of edge activators and optimized the method of preparation.

Containing Span 80 as edge activator achieved most favourable outcomes in spherical shape, vesicle size, zeta potential, entrapment efficiency and deformability index. 

Result showed that sonication Time with an amplitude is proven to produce optimum Transethosomes, in comparison to other vesicles using span80 it was able to have excellent vesicle characteristics making it promising in developed as a transdermal drug delivery

26

5.

Flurbiprof-en

(Arthritis)

Developed and Evaluated Transethosomes by thin – film hydration method using Span80 and Tween 80 as edge activators soyaphosphotidylcholi-ne and various percentage of ethanol

The formulation showed the least particle size, highest deformability index and best ex- vivo profile was optimized after optimization it was dispersed in gel and evaluated for Ph.   Drug content and compared with marketed formulation for ex- vivo permeation and skin deposition.

 Result showed that On comparison with marketed gel it was found that the optimized gel containing higher concentration of Tween80 had better ex- vivo profile and skin deposition. The formulated Transethosomes may serve as potential carrier for the effective management of arthritis.

27

6

Irbesartan

(angiotensin-in receptor blocker)

Formulated and characterized Transethosomal loaded Nanoparticle by cold method

Various parameters like vesicle shape, vesicles size, polydispersity index, Zeta potential, calibration curve, entrapment efficiency, FTIR    and in vitro release had been done to confirm Transethosomes.

Result showed that the Transethosomes shows Useful carrier for poorly soluble drug and provide a novel vehicle for the delivery of the drug

28

7.

Ginger -Extract

Ginger- extract loaded Transethosomes for effective transdermal permeation anti – inflammation in rat model. Transethosomes were prepared by cold injection using different edge activator.

In vivo studied showed that Transethosomal hydrogel exhibited significant inhibition of edema swelling compared to free hydrogel and ketoprofen gel.

Result showed that Transethosomes could be a new vehicle for the effective skin permeation and anti-inflammatory.

29

8.

5- Fluorouracil

(Anti-cancer)

Formulated   and evaluated Transethosomes by cold method by using Phospholipon 90G.

Phospholipon 90G was selected as a vesicles forming in Transethosomes for achieving high entrapment efficiency and good stability as compared to the formulation using phospholipon 90H. standard deviation suggested better poly dispersitivity

Results show that the Transethosomes were better carrier option for delivered the drug into the deeper skin layer and hence useful in the treatment of skin cancer

30

9.

Apremilast

(anti- inflammatory)

Developed   and Characterized      Transethosomal gel by rotatory vacuum evaporator. Box Behnken design was used to optimization of formulation by taking quantity of lipoid S 100, in which sodium cholate and ethanol as independent variable and vesicle size, entrapment efficiency and cumulative drug release as dependent variable.

The optimized batch of Transethosomes vesicles was incorporated in carbapol gel base. The various evaluation parameters like size, Zeta potential, surface morphology, Ph, viscosity, spreadbility, drug content, and ex- vivo permeation studies was performed.

The ex- vivo permeation studied was performed   24 hrs through the rat skin.  In which it   showed better skin permeation and sustained release. Found to be satisfactory results with respect to Ph., gel characteristics and stability. Thus, it can be effective option for the treatment of psoriasis.

31

10.

Ketoprofen

(NSAIDs)

Formulated, developed and evaluated Transethosomes gel to see the effect of lipid concentration, drug concentration, ethanol concentration and stirrer time affected the result.

Evaluation parameters were employed to characterise Transethosomes in which it showed   average vesicles size, percent EE, and zeta potential.

Result showed that Transethosomes formulation in the gel was refined and employed as topical medication for its NSAIDs effect. Thus, it is choice for the transdermal medication and give long term released.  It improve the penetration of many medication through the skin.

32

11..

Ketorolac Tromethamine

(NSAIDs)

Transethosomes and ethosomes for enhanced transdermal delivery: A comparative Assessment by Cold Method and were characterized for particle size, entrapment efficiency, Transmission electron microscopy, Zeta potential and, in – vivo drug release, ex- vivo permeation studies and in- vivo study.

Transethosomes showed higher drug entrapment as compared to ethosomes. Both the formulation showed good Zeta potential indicating good stability.

The elasticity of Transethosomal vesicles are found higher than the ethosomal vesicles   and the transdermal flux of Transethosomal gel was found to fold increase in release as compared to ethosomal gel. Result showed that Transethosomes are more effective carrier as compared to ethosomes for transdermal delivery.

33

12.

Celecoxib

(COX – 2 Inhibitor)

Transethosomal gel for the topical delivery formulated and estimated   of skin cancer progression. The prepared Nano vesicles were characterized for drug encapsulation efficiency, Vesicle size, surface charge, morphology, FT-IR and DSC were also conducted.

The optimized formulation were dispersed in various hydrogel base in – vitro release and in- vivo permeability studies were evaluated. The formulated TES-based hydrogel displayed a sustained in vitro CXB release pattern for 24 h with an enhanced flux and permeation across rat skin compared with the control. TES-based hydrogel has a lower cytotoxic effect on normal skin as compared to TES- suspension and TES- powder.

Results suggested that TES- loaded hydrogel formulation could be a promising carrier and effective chemotherapeutic agent for the management of skin carcinoma.

34

13.

Paeonal

(Anti – bacterial, anti-inflammatory and analgesic)

Evaluated of Transethosomes as transdermal delivery carrier by Ethanol injection method

Compared to Transferosomes, Transethosomes had high entrapment efficiency and showed spherical morphology with a smooth surface when viewed under a TEM.

Results showed that Transethosomes had a narrow size distribution, high encapsulation efficiency, and long residence in plasma. Hence it increases the bioavailability of the drug.

35

14.

Baicalin

(anti- arthritic)

Developed, characterized, Pharmacokinetic and Pharmacodynamic evaluation of Transethosomes by thin film hydration method and optimization was done using Box- Behnken design (BBD)

The in vivo study revealed that the drug loaded Transethosomal gel has good anti- arthritic potential in comparison with the standard diclofenac gel which was evinced by radiographic analysis and histopathological studied.

Result showed that the Skin irritation study on Wistar   albino rats confirm that the Transethosomes formulation is safer for skin application.

36

15.

Olmesartan medoxomil

(Antihypertensive)

Use of Transethosomes for enhancing the transdermal delivery of olmesartan medoxomil prepared by full factorial design by using surfactants and different phospholipid-to-SAA ratios.

Rat skin and shed snake skin was used to ex vivo permeation and Transethosomes showed higher permeability as compared to transferosomes and solution.

Result showed that the Transethosomes was used a successful carrier for transdermal delivery of drug.

37

16.

Dimethyl Fumarate

Dimethyl fumarate loaded Transethosomes: A formulative study and preliminary Ex vivo and In vivo evaluation. Formulative study was performed to investigate the effect of the composition of Transethosomes.

Transethosomal gel evaluated in vivo with a patch test. It was gained that the phosphatidylcholine concentration affected vesicle size.

Result showed that the Transethosomal gel was not irritant after cutaneous application and hence it was used in the treatment of wounds caused by diabetes mellitus or peripheral vascular diseases.

38

17.

Dexketoprofen trometamol

Transethosomes a break through tool for controlled transdermal delivery of Dexketoprofen trometamol: Designed, fabricated, statistically optimized, In vitro and In vivo characterization. Thin film method was used to prepare Transethosomes. 

Permeation study was performed on Transethosomes for this it was incorporated in carbopol gel base for the comparison with solution.

Result showed that Transethosomes enhanced skin permeation as compared to solution.

39

18.

Quercetin

Ethosomes and Transethosomes as cutaneous delivery systems for Quercetin: A preliminary study on Melanoma cells. To overcame drug bioavailability the drug was loaded in Ethosomes and Transethosomes.

 

The result proved that both phosphatidylcholine concentration and drug affect the vesicle size.

Result showed that In vitro permeation was enhanced of drug in the case of Transethosomes as compared to Ethosomes. 

40

19.

Colchicine

(Gout)

Transethosomal gels as carrier for the transdermal delivery of drug; statistical optimized, characterized and ex vivo evaluated and were prepared by cold method and optimized by three sets of factorial design. 

Drug loaded Transethosomal gel were able to enhanced the skin permeation parameters of the drug in comparison to the non-ethosomal gel.

Result showed that the Transethosomal gel were promising careered for the transdermal delivery of drug. 

41

20.

Sinomeniu-m Hydrochloride (anti-rheumatic

Enhanced Transdermal permeability and drug deposited in rheumatoid arthritis drug loaded antioxidants surface Transethosomes.  Drug loaded Transethosomes had decorated with ascorbic acid to formed antioxidant surface Transethosomes.

It had revealed that the Transethosomes and antioxidant surface Transethosomes containing sodium deoxy cholate   had effectively increase the entrapment efficiency of hydrophilic drug, and has superior deformability and higher permeation efficiency.

Result showed that the Antioxidant surface Transethosomes had enhanced transdermal permeability and drug deposited for the oxidant stressed in RA. 

Had   further research potential to served as a TDDS of RA.

42

21.

Metformin HCl.

(Antidiabetic)

Transethosomal gel: Developed, characterized and antidiabetic potential evaluated in the diabetes -induced Rat model. Transethosomes incorporated into a chitson gel to developed Transethosomal gel.

The fabricated Transethosomes had showed sustained release followed by a more pronounced effect in Transethosomal gel as compared to the plain solution and showed enhanced permeation. The In vivo assayed result showed improved antidiabetic potential of Transethosomes gel as compared to gel.

Result showed that the Transethosomes had a promising anti-diabetic candidate for transdermal delivery that can provide sustained released and enhanced antidiabetic effect.

43

22.

Erythromycin

(Antibiotic)

Developed and Optimized drug loaded Transethosomes Cinnamon Oil Based Emulgel for Antimicrobial Efficiency. Box- behnken design was used to optimized formulation.

The formulation showed greater stability and had sufficient characteristics for effective topical application.

Result showed that the Transethosomes cinnamon oil based emulgel is an alternative way to delivered drug for the treatment of topical bacterial infections.

44

23.

Ketoconazole

(Antifungal)

Studied the antifungal and ocular permeation of drug from ophthalmic formulation contained Transethosomes Nanoparticle   and the formulation were optimized.

The developed in situ gel formulations were found to be non-irritating to the cornea and were able to penetrate deeper into the posterior eye segment without caused any toxic effect.

Result showed that the drug loaded Transethosomal gel represented a promising ocular delivery system for the treatment of deep fungal eye infections.

45

24.

Voriconazole

(Antifungal)

Fabricated and evaluated of drug loaded Transethosomal gel for enhanced antifungal and ant leishmanial activity by cold method

Rat skin was used for Ex vivo permeation and showed enhanced efficiency.

Result showed that the developed Transethosomal formulation can served as an effective drug delivery system through a topical route with enhanced efficacy and better patient compliance

46

25.

Chenopodium murate

 Potential used of Transethosomes as a transdermal delivery system for metabolites in which ethosomes and Transethosomes had formulated in different ratio of Phosphatidylcholine, cholesterol and Tween 80.

Transethosomes showed best spherical morphology, average size, zeta potential and entrapment efficiency and low deformability. Transethosomes preserved the macrostructural property of extract allowed greater permeation in the skin.

Result showed that the Transethosomes are Potential Transdermal delivery system for a drug extract with possible therapeutic applications.

47

26.

Miconazole Nitrate

In vitro and in vivo characterized of Transethosomes for the treatment of cutaneous candidiasis. Thin film hydration method was used to formulate Transethosomes.

Transethosomal gel showed enhancement of fold as compared to Transethosomes. The in vitro antifungal activity of Transethosomal gel more as compared to normal gel.

Result showed that the Transethosomal gel could be a suitable drug delivery system with higher penetration and good antifungal activity.

48

27.

Fluvastatin

(antipsoratic)

Formulated   developed and evaluated Transethosomes by thin film hydration method consist of Phospholipon 90 along with Tween 80 or Tween 20 and the edge activator.

In vitro cell culture studies were conducted to evaluate the cytotoxicity and ant psoriatic activity of the Transethosomes carrier system that exhibited the highest dermal accumulation.

Results showed that the Fluvastatin have Antipsoratic activity to the affected area of the skin.

49

28.

Voriconazole

A Novel Vesicular Carrier: Transethosomes for enhanced skin delivery Characterized   and in vitro/in vivo     evaluated. Transethosomes are composed of Phospholipid, ethanol water and edge activator.

As compared to CLs and DLs the elasticities of ELs and TELs are higher. Thus, TELs enhanced the skin permeation of drug compared to the other Vesicles.

The studied   showed that the Novel Carrier Transethosomes could served   as an effective dermal delivery of drug. 

50

29

Azelaic Acid

(Antidermatophyte)

Developed, Optimized, and In Vitro/In Vivo Evaluated of Transethosomal Gel by thin film hydration method.   Two   guinea pig infection models with Trichophyton (T.) mentagrophytes and Microsporum (M.) canis were used in vivo assessment.

The ex vivo permeation study showed enhanced skin penetration with drug loaded Transethosomes compared to normal drug after 48 h.

 Results showed that the TEs could be a promising carrier for drug delivery into deeper skin layers with enhanced ant dermatophyte activity.

51

30

Hesperidin

Formulated and Characterized of Transethosomal Gel for Dermal Delivery to Enhance Antibacterial Activity: Comprehension of In Vitro, Ex Vivo, and Dermatokinetic Analysis by rotatory evaporator method and optimized using Box–Behnken design

The in vitro drug release showed that the drug loaded Transethosomes shows more release compared to drug loaded in suspension and ex vivo skin permeation increases in transethosomes gel and antioxidant activity is higher 

Results showed that the Transethosomes formulation could enhance the topical application in the management of cutaneous bacterial infections.

52

31

Tranexamic acid (Melasma)

Formulated   developed    transethosomal   patch   by cold technique using Phospholipid, ethanol water and edge activator.

The in vitro and ex vivo released   was evaluated and showed the release period of 24 h which was better than that conventional topical cream.

Results showed that the transethosomes may be a good carrier for delivering   drug into deeper layer and good treating for the treatment of Melasma.

53

32

Tramadol HCl

(Pain- Management)

Designed, Developed and Characterized   Transethosomes gel formulation   by simple cold method using different concentration of phospholipid and edge activator (Span 20 and cremophar EL 35).

Span 20 Formulation exhibited a faster drug release than the cremophar. Optimized formulations showed first order of kinetics.

The study supported the developed   of optimized transethosomes formulation into a topical gel using carbopol   934 as gelling agent. Stability studied prove that there is very less chance in the EE, hence the formulation was found to be stable.

54

33.

Vesicular Nano carriers

Vesicular Nano carriers: A Novel approached for Transdermal delivery. Novel drug delivery system delivered the drug at predetermined rate as per the requirement of body.

Vesicular Nano carrier included Liposomes, Ethosomes, Transferosomes, Transethosomes

 And Niosomes.

Study   showed Vesicular Nano carriers became   the choice for transdermal delivery of drug.

55

34

Skin delivery

Transethosomes: Novel Technology for skin delivered of drugs. Skin delivery of drugs removed many difficulties which had come from oral route.

Among vesicular system Transethosomes showed more promising group because it had both lipophilic and hydrophilic section and many therapeutic compounds with a wide range of solubility can be taken by this route.

study showed that these vesicles transport analgesic, anaesthetics, corticosteroids, sex hormone, anticancer drugs and insulin etc.

56

35

Antifungal

Transethosomes a novel transdermal drug delivery system for antifungal drugs. The Stratum corneum was considered a barrier to the entry of drugs.

Antifungal drugs was not fully effective due to many cause like poor skin penetration, inability to reach target sites, low bioavailability due to hepatic metabolism and decrease patient compliance. Transethosomes minimized this difficulty of antifungal drugs.

Study showed that the Transethosomes increased the stability and solubility of antifungal drugs and hence increased their efficacy in eliminating the infection

57

36

Transdermal drug delivery

Transethosomes and Nanoethosomes   recent approached on transdermal drug delivery system.  It delivered the drug into the deeper layer of skin.

Nanoethosomes and Transethosomes both contained same composition water, ethanol and phospholipid but Transethosomes contained edge activator additionally so it enhanced skin permeation

Study showed that the method of preparation, characterization and pharmaceutical used of Nanoethosomes and Transethosomes.

1

37

Transdermal and topical drug delivery

Transethosomes: A breakthrough system for Transdermal and topical drug delivered. Transethosomes was able to permeate from rigid network of stratum corneum.

Ethanol imparted softness and edge activator increased the permeation by providing elasticity making possible to deliver the drug molecules into the blood.

Study showed that the Non-invasive technique can be used as a carrier for NSAIDs, anticancer, antifungal and antihypertensive drugs.

58

38

Transdermal delivery

Transethosomes: A new prospect for enhanced Transdermal delivery. Transdermal delivery overcame many problems associated with oral route of administration.

Transethosomes had both lipophilic and hydrophilic region and it accommodated drug molecules with a wide range of solubility.

Study showed that these vesicles can be used for the transdermal delivery of different category of drugs like analgesics, anaesthetics, corticosteroids, sex hormones, anticancer agents’ insulin etc.

5

39

Topical administration

Transethosomes: An effective tool in bypassing barriers for topical administration of formulation composed of Phospholipid, ethanol, water and edge activator.

Various method was used in the formulation of Transethosomes included cold method, hot method, thin film hydration method, and mechanical dispersion method. 

Study showed that These vesicles was also used Transdermal delivery of various category of drugs like NSAIDS, antifungal, antibiotics, ant parkinsonism, antiviral.

59

40

Transcutaneous drug delivery

Transethosomes: A Novel carrier for Transcutaneous drug delivery an overviewed it overcame many disadvantages which are caused by oral route.

Transethosomes had a unique property for improved transdermal delivery of drugs via the skin among transferosomes and ethosomes.

Study showed that the UDV was used to administer a variety of drugs category via transdermal route included anti-arthritic, antibacterial, anticancer, antiviral and analgesic.

60

41

Topical delivery

Novel and most prominent carrier system Transethosomes for topical delivery.  Developed vesicular system gave better patience compliance.

Different Types of vesicular system was developed like Liposomes, Ethosomes, Transferosomes and Transethosomes.

Study showed that Transethosomes was ethanol based vesicular carrier may contained both advantage of Transferosomes and Ethosomes.

61

42

Transdermal route

Exploring the potential of Transethosomes in therapeutic delivery: A comprehensive review. Transethosomes had gained attention as a promising solution, offering distinct advantages over traditional formulations.

Transethosomes minimized plasma fluctuations, first‐pass metabolism, organ toxicity, and poor bioavailability.

Study showed evaluation and methods of preparation of Transethosomes.

62

43

Therapeutic drug delivery

A comprehensive review on Transethosomes as a novel approach for drug delivery through transdermal route. Formed ultra-deformable vesicles (UDVs) was a novel technique for the transdermal applications of the drugs.

Transethosomes improved drug permeation through the stratum corneum due to increased in the concentration of ethanol, phospholipids, and edge activators. 

Study showed that these vesicular was used to deliver a variety of drugs included analgesics, antibiotics, antivirals, anticancer and arthritis drugs.

63

44

Candidiasis

A review of fluconazole loaded Transethosomal gel for candidiasis.  Fluconazole was considered as most effective as compared to other antifungal drugs.

The disadvantage which was caused from conventional system   was nullified when the drug was incorporated in Transethosomes and provided stable and more effective formulation and provided high patient compliance.  

Study showed that Transethosomes contained high concentration of ethanol along with edge activator which provided high penetration to the skin and leads to better therapeutic action.

64

45

Transdermal drug delivery

Ultra-deformable Nano Transethosomes: A novel tool to intensify transdermal drug delivery a review. Transdermal delivery overcame many disadvantages which are caused when drug was taken through oral route.

 

Among Transferosomes and Ethosomes Transethosomes was novel prospect to enhanced transdermal drug delivery through the skin.

Study showed that Nano Transethosomes was prepared by different method included hot method, Cold method and Transmembrane pH gradient method, ethanol injection method and thin film hydration method.  The UDV was used to deliver various classes of drugs such as anti-arthritic, antibiotic, anticancer, antiviral and analgesic.

65

46

Transdermal drug delivery

Transethosomes: an ultra-deformable ethanolic vesicles for enhanced transdermal drug delivery. Drug delivered through the skin improved solubility, bioavailability, and unwanted side effect of drugs.

Transethosomes was novel UDV that delivered the drug into deeper tissue.

Study showed that Transethosomes was composed of Phospholipid, ethanol and surfactants and method of preparation of Transethosomes.

66


 


Patent related to Transethosomes:

Description of few patents regarding transdermal drug delivery of Transethosomes are:


Title of Patent.

Brief description

Inventor.

Patent number

Transethosomes Preparation of ketoconazole ophthalmic solution and methods of preparation.

This invention describes the Preparation technique of Transethosomes of ketoconazole ophthalmic solution used in the treatment of eye disease. 

Tarek A, Ahmed (Jeddah), Maram M, Alzahrani (Jeddah),

Nebil A, Alhakamy (Jeddah), Raed I, Felimban (Jeddah).

US11285148

Transethosomal gel preparation of Epigenin.

This invention describes the preparation of Transethosomal gel of epigenin for topical administration.

Adnan et. ol

DE202022103412U1

Transethosomal gel preparation of Neem-oil.

This invention describes the preparation of Transethosomal gel of Neem-oil.

Gupta et. ol

DE202022104296U1

 


CONCLUSION:

Transdermal drug delivery system improve the bioavailability and skin permeation of many drugs. Transethosomes are novel vesicular system which contain phospholipid, ethanol, water and edge activator has the ability to penetrate deeper layer of the skin. it has more advantage over conventional drug delivery, ethosomes and transferosomes because of ethanol and edge activator. Transethosomes deliver medication with enormous molecular weight such as peptides and protein molecules. Transethosomes are not only used in the topical treatment of local diseases but it also become a promising approach for systemic diseases and it improved high patient.

 

CONFLICT OF INTEREST:

No

 

REFERENCES:

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Received on 19.03.2024      Revised on 10.09.2024

Accepted on 14.01.2025      Published on 23.04.2025

Available online from April 26, 2025

Asian J. Pharm. Tech. 2025; 15(2):141-150.

DOI: 10.52711/2231-5713.2025.00023

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