Development of transethosomes formulation for dermal fisetin delivery: Box–Behnken design, optimization, in vitro skin penetration, vesicles–skin interaction and dermatokinetic studies

Moolakkadath, Thasleem; Aqil, Mohd.; Ahad, Abdul; Imam, Syed Sarim; Iqbal, Babar; Sultana, Yasmin; Mujeeb, Mohd; Iqbal, Zeenat

doi:10.1080/21691401.2018.1469025

Cited by 94 publications

(49 citation statements)

References 50 publications

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“…Dermatokinetic study is performed for determination of the amount of drug deposited in the skin. 68 The amount of OLM deposited from drug suspension and TE14 through rat skin at different time intervals is depicted in Figure 7. The skin treated with TE14 showed a significantly higher C max of 108.04±6.44 µg/cm 2 and an AUC 0-10 of 680.46±17.99 µg⋅h/cm 2 in the skin layers when compared to the drug suspension with a C max of 47.07±32.40 µg/cm 2 and an AUC 0-10 of 196.30±99.66 µg⋅h/cm 2 (P,0.05).…”

Section: Dermatokinetic Studymentioning

confidence: 99%

Use of transethosomes for enhancing the transdermal delivery of olmesartan medoxomil: in vitro, ex vivo, and in vivo evaluation

Albash¹,

Abdelbary²,

Refai³

et al. 2019

IJN

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Introduction and aim: Olmesartan medoxomil (OLM) is an antihypertensive drug with low oral bioavailability due to extensive first-pass metabolism. This study aimed to prepare transetho somes (TEs) for enhancing the transdermal delivery of OLM to avoid its oral problems. Methods: TE formulae were prepared utilizing 5 1 .3 1 full factorial design using various surfactants (SAAs) and different phospholipid-to-SAA ratios. The formulae were characterized regarding their entrapment efficiency percentage (EE%), particle size (PS), polydispersity index (PDI), zeta potential (ZP), and the amount of drug released after 6 hours (Q6h). Design Expert ® software was employed to select the optimum formula. Results: The optimum formula (TE14) had an EE% of 58.50%±1.30%, PS of 222.60±2.50 nm, PDI of 0.11±0.06, ZP of-20.80±0.30 mV, and Q6h of 67.40%±0.20%. In addition, TE14 was compared to transferosomes (TFs) in terms of elasticity and was found to show higher deformability index. Further, evaluation of ex vivo permeation using both rat and shed snake skin showed higher permeability of TE14 compared to TFs and OLM suspension. Confocal laser scanning microscopy confirmed the capability of the fluoro-labeled TE14 to penetrate deep within the skin, while the histopathological study confirmed its safety. TE14 successfully maintained normal blood pressure values of rats up to 24 hours. Moreover, TE14 showed superiority in dermatokinetic study when compared with drug suspension. Conclusion: Taken together, the obtained results confirmed the potential of employing TEs as a successful carrier for the transdermal delivery of OLM.

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Section: Dermatokinetic Studymentioning

confidence: 99%

Use of transethosomes for enhancing the transdermal delivery of olmesartan medoxomil: in vitro, ex vivo, and in vivo evaluation

Albash¹,

Abdelbary²,

Refai³

et al. 2019

IJN

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“…A modification of ethosomes, namely transethosome, was introduced by Song et al [114] who combined the use of phospholipids, with high amounts of ethanol and surfactant, acting as permeation enhancers, for delivery of voriconazole. This technology has been investigated for the delivery of fisetin [115], piroxicam [116], paeonol [117], epigallocatechin gallate-containing extract [118] and agomelatine [119].…”

Section: Vesicles and Analoguesmentioning

confidence: 99%

Enhancement strategies for transdermal drug delivery systems: current trends and applications

Ramadon

McCrudden

Courtenay

et al. 2021

Drug Deliv. and Transl. Res.

184

105

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Transdermal drug delivery systems have become an intriguing research topic in pharmaceutical technology area and one of the most frequently developed pharmaceutical products in global market. The use of these systems can overcome associated drawbacks of other delivery routes, such as oral and parenteral. The authors will review current trends, and future applications of transdermal technologies, with specific focus on providing a comprehensive understanding of transdermal drug delivery systems and enhancement strategies. This article will initially discuss each transdermal enhancement method used in the development of first-generation transdermal products. These methods include drug/vehicle interactions, vesicles and particles, stratum corneum modification, energy-driven methods and stratum corneum bypassing techniques. Through suitable design and implementation of active stratum corneum bypassing methods, notably microneedle technology, transdermal delivery systems have been shown to deliver both low and high molecular weight drugs. Microneedle technology platforms have proven themselves to be more versatile than other transdermal systems with opportunities for intradermal delivery of drugs/biotherapeutics and therapeutic drug monitoring. These have shown that microneedles have been a prospective strategy for improving transdermal delivery systems. Graphical abstract

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“…The sink condition is maintained and sample is analyzed using HPLC. 60 The cumulative amount of drug permeated through animal's skin is calculated by…”

Section: Ex Vivo Skin Permeation Studiesmentioning

confidence: 99%

Nano-transethosomes: A Novel Tool for Drug Delivery through Skin

Bajaj¹,

Parab²,

Shidhaye³

2021

IJPER

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Transdermal drug delivery has become a popular tool from last few years. It overcomes drawbacks which are encountered with the oral route. Though very few routes are as attractive as transdermal route, transport of drug through the skin is challenging. In order to overcome the challenges, researchers have found a system in which the drug is encapsulated into the vesicle and these vesicles can penetrate deeper into the skin to hit the target site. Hence, better skin penetration of bioactive agents can be achieved. Vesicular systems like liposomes, niosomes, ethosomes and Transferosomes tend to remain accumulated in the skin layers. Since Transethosomes have small particle size and can easily alter the shape of vesicle as compared with other vesicular systems; it can penetrate through the layers of skin. Hence, the drug encapsulated into Transethosomes can easily reach the target site. Transethosomes consist of ethanol, phospholipids along with an edge activator. Ethanol and edge activator help to enhance skin permeation of Transethosomes. Since it is a non-invasive technique, it improves patient compliance. It also increases drug entrapment efficiency. These vesicles can accommodate different variety of drugs such as anticancer, corticosteroids, proteins and peptides, analgesics.

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Development of transethosomes formulation for dermal fisetin delivery: Box–Behnken design, optimization, in vitro skin penetration, vesicles–skin interaction and dermatokinetic studies

Cited by 94 publications

References 50 publications

<p>Use of transethosomes for enhancing the transdermal delivery of olmesartan medoxomil: in vitro, ex vivo, and in vivo evaluation</p>

<p>Use of transethosomes for enhancing the transdermal delivery of olmesartan medoxomil: in vitro, ex vivo, and in vivo evaluation</p>

Enhancement strategies for transdermal drug delivery systems: current trends and applications

Nano-transethosomes: A Novel Tool for Drug Delivery through Skin

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