Ethosomes as Vesicles for Effective Transdermal Delivery: From Bench to Clinical Implementation

Akhtar, Nida; Varma, Anurag; Pathak, Kamla

doi:10.2174/1574884711666160813231352

Cited by 18 publications

(8 citation statements)

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“…Up to a concentration of 40%(v/v), the %EE increased which can be attributed to the increased uidity of the ethosomal membrane and also due to increased solubility of the lipophilic drug in the inner polar ethosomal core. But when ethanol concentration was above 40%(v/v), the %EE decreased due to increased solubilisation of the drug in ethanol causing disruptions in the vesicular membrane (27,28), This was a contradicting the effect from the normal, which can be reasoned to increase in the uidity of the membranes thereby the entrapped drug leaching out (29).…”

Section: Discussionmentioning

confidence: 99%

Enhancement and Extended Release of the Anti-hypertensive Drug Carvedilol using Optimized Ethosomal Gel via Transdermal Route

Amarachinta¹,

Samed²,

Kumar³

et al. 2020

Preprint

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BackgroundCarvedilol, a popular anti-hypertensive drug, when orally administered has very poor bioavailability on the account of undergoing hepatic metabolism and therefore it becomes primal to explore an alternative drug delivery route for carvedilol. For a drug to be delivered by undergoing the least number of stages of metabolism and achieve high target specificity, transdermal delivery is the most preferred route. Hence, a study was conducted to test the potential of ethosomes as a candidate for transdermal delivery of carvedilol. A statistical study by using Central Composite Design (CCD) was also conducted for optimizing the quantity of the primary constituents present in the ethosomes. The optimized ethosomal formulation was then incorporated into a hydrogel to prepare the ethosomal gel.ResultsThe optimized formulated ethosomal suspension and the ethosomal gel were undergone physicochemical, compatibility and in-vitro drug release studies along with characterization studies. The incorporation of the ethosomes into the hydrogel proved to be effective for skin application thereby ensuring better transdermal delivery. The optimized ethosomal gel has showed credible physical appearance, spreadability, viscosity and in-vitro drug release. The pharmacodynamic studies conducted on Wister rats revealed that the anti-hypertensive action was gradual and sustained lasting up to a period of 24 hours. The stability studies conducted also showed that prepared formulations maintained its consistency within the range for the measured parameters of physical appearance, rheological properties and entrapment efficiency for a period of 3 months.Conclusions The incorporation of the drug loaded into hydrogel and its effect on regulating systolic blood pressure in a sustained way lasting 24 hours proved to be better than the present available marketed formulation which has a rapid action with the anti-hypertensive effect lasting only for 10 hours. The chosen route for delivering the drug transdermally hence proved to be effective with better enhancement and permeation capability and shows the high potential of ethosomes to be considered for novel delivery of other anti-hypertensive drugs.

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Section: Discussionmentioning

confidence: 99%

Enhancement and Extended Release of the Anti-hypertensive Drug Carvedilol using Optimized Ethosomal Gel via Transdermal Route

Amarachinta¹,

Samed²,

Kumar³

et al. 2020

Preprint

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“…In addition, they have superior pharmaceutical properties, including stability at room temperature, high entrapment efficiency, and improved compatibility with the stratum corneum, thus promoting the effective penetration of lipophilic drugs into the skin. [12][13][14] In our preliminary study, we have proven that ethosomes can promote transdermal permeation of lipophilic drugs, such as lidocaine, with a shorter onset time and a longer duration in vivo than lidocaine-based liposomes or lidocaine delivered in a hydroethanolic solution. 15 Subsequently, ethosomes have been used in photodynamic therapy, 16,17 cosmeceuticals, 18 and a vaccine.…”

Section: Introductionmentioning

confidence: 93%

“…[29][30][31] In terms of possible mechanisms for ethosomes to promote percutaneous permeation of drugs, two viewpoints have been presented: the first one is that ethanol is a known penetration enhancer, which can disturb the multilamellar and ordered lipid domain, lower the structure density, and enhance the fluidity of the stratum corneum, thus providing the vesicles with flexible characteristics that allow them to penetrate easily into deeper layers of the skin; 32,33 the second one is that phospholipids between the stratum corneum and ethosomal vesicle fuse easily, thus changing the transition temperature, leading to enhanced drug penetration. 34 In our research, we interestingly found that even though the lipid content in the liposomes and the ethanol content in the hydroethanolic solution were equal with those in the ethosomes, after percutaneous penetration, a greater fluorescence intensity in the skin of the ethosomal system was observed, compared with that in the hydroethanolic solution and liposomes (P,0.05; Figure 2B).…”

mentioning

confidence: 99%

Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes

Yang

et al. 2017

IJN

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Ethosomes can promote the penetration of lipophilic drugs into the skin, but the underlying mechanism is still unknown. The purpose of this study was to investigate the mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes. The formulation of ethosomes was optimized using the Box–Behnken experimental design, in which Rhodamine B and 1-palmitoyl-2-{12-[(7-nitro-2-1,3-benzoxadiazol-4-yl)amino]dodecanoyl}- sn -glycero-3-phosphocholine were used to simulate a model lipophilic drug and act as a fluorescent tracer of ethosomal phospholipids, respectively. Liposomes with the same phospholipid concentration and a hydroethanolic solution with the same ethanol concentration were also prepared as controls. The percutaneous progression of the above fluorescent preparations was observed by confocal laser scanning microscopy, and the fluorescence intensity of the images was analyzed. The optimized ethosome formulation consisted of 2.45% yolk phospholipids, 30% ethanol, and 67.55% distilled water. The percutaneous permeation of Rhodamine B in the optimized ethosomes was superior to that in hydroethanolic solution ( P <0.05) and liposomes ( P <0.05). The ethosomes could penetrate the skin via the percutaneous pathway of the hair follicle and stratum corneum, while during the process of penetration, the vesicles were broken and the phospholipids were retained in the upper epidermis, with the test compounds penetrating gradually. The superior percutaneous penetration of ethosomes was linked to the synergistic effects of their ingredients. The percutaneous pathways of ethosomes included open hair follicles and stratum corneum pathways. In addition, the vesicles might break up during percutaneous penetration in the superficial layer of the skin, allowing the test compounds to keep permeating into the deeper layer alone, while the phospholipid was retained in the upper epidermis.

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“…It may contain 2%-5% phospholipids and 20%-40% ethanol (Grath and Uitto, 2008). Drug penetration through the skin is higher in the case of ethosomes as compared to liposomes due to the ability of ethanol to fluidize the membrane lipids of SC (Akhtar et al, 2016;Blume et al, 1993;Romero and Morilla, 2013). The addition of ethanol increases the particle size of ethosomes, and a decrease in size was observed by maintaining a constant concentration of phospholipid (Campani et al, 2016).…”

Section: Ethosomesmentioning

confidence: 99%

Nanomaterials for skin antifungal therapy: An updated review

Nagpal¹,

Kaur²

2021

J Appl Pharm Sci

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Topical diseases are treated with oral and conventional topical formulations till date. Both oral and topical routes face many challenges such as poor absorption, high metabolism, toxicity, and drug-drug interactions. Conventional topical dosage forms like creams, lotions, and gels have failed to show controlled drug release. Literature reports indicated that more than 1.5 lakh (approximate) people lost their lives due to fungal infections and several lakhs of the population are affected. Even then, it is a neglected subject by public health authorities, and while most of the deaths from fungal diseases can be stopped. Globally, it is estimated that over 30 lakh cases of pulmonary Aspergillosis, 7 lakh cases of Candidiasis, 2.5 lakh cases of Aspergillosis, 5 lakh cases of Pneumocystis jirovecii pneumonia, and many more occur annually. Nanomedicines play a key role in reducing the number of patients coming up with fungal infections. A small-sized drug can easily penetrate the micropores of the skin and show desirable results. Nanomedicines rely on various nanomaterials (lipidic carriers, metal nanoparticles, carbon nanotubes, quantum dots, etc.) for their therapeutic efficacy. Nanomaterials can facilitate efficient topical drug delivery by increased penetration, enhanced safety and efficacy, and sustained and targeted release of drugs. The review summarizes the basics of nanomedicine with respect to topical delivery and various nanomaterials for better therapeutics of the fungal infections of the skin.

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Ethosomes as Vesicles for Effective Transdermal Delivery: From Bench to Clinical Implementation

Abstract: From various research reports, it can be concluded that ethosomes are the competent and efficient vesicles to provide better drug transport via transdermal route.

Cited by 18 publications

References 0 publications

Enhancement and Extended Release of the Anti-hypertensive Drug Carvedilol using Optimized Ethosomal Gel via Transdermal Route

Enhancement and Extended Release of the Anti-hypertensive Drug Carvedilol using Optimized Ethosomal Gel via Transdermal Route

Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes

Nanomaterials for skin antifungal therapy: An updated review

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