Tacrolimus-loaded ethosomes: Physicochemical characterization and in vivo evaluation

Li, Guiling; Fan, Yixuan; Fan, Chao; Li, Xinru; Wang, Xiaoning; Li, Mei; Liu, Yan

doi:10.1016/j.ejpb.2012.05.011

Cited by 117 publications

(55 citation statements)

References 80 publications

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“…The application was first put forward by Touitou in 1996(Touitou, 1996 and was specially tailored to efficiently deliver various molecules into deep skin layers and across the skin (Ainbinder et al, 2010). Ethosomes has been studied for delivery of various drugs ranging from low molecular weight drugs such as acyclovir , minoxidil (Jun-Bo et al, 2007), tacrolimus (Li et al, 2012), ligustrazine phosphate (Shi et al, 2012), econazole nitrate (Verma & Pathak, 2012), ibuprofen (Shumilov et al, 2010) to polypeptides and gene medicines (Godin & Touitou, 2003).…”

Section: Introductionmentioning

confidence: 99%

Penetration profile and human cadaver skin distribution of finasteride from vesicular nanocarriers

et al. 2013

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The skin accumulation of therapeutic agents affects the efficiency of topical drug delivery. In this study, in vitro distribution of finasteride of ethosomes and liposomes in human cadaver skin after percutaneous delivery were investigated. Experiments were performed using modified Franz diffusion cells. Finasteride ethosomes, liposomes or hydroethanolic solutions were used as donor medium. Drug distribution at different skin layers and depths were studied by hotplate separation and frozen horizontal slicing technique. The result showed that the accumulation of finasteride in skin ranged from 9.7-24.3 mg/cm 2 at 12 or 24 hours. The ethosomes demonstrated better enhancing ability to deliver finasteride into the dermis layer than liposomes did. The finasteride concentration in the dermis layer from ethosomes was more than sevenfold higher than from liposomes. The finasteride accumulation in ethosomes group showed a distinctive reversed distribution profile. This distinctive reversed distribution profile is meaningful for exerting a favorable pharmacological effect for finasteride. The drug distribution profile in skin layers showed no significant difference between 12 and 24 hours application (p40.05). The study demonstrated that finasteride can be accumulated at target site more effectively and maintained at higher level through the application of novel ethosomal carriers.

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Section: Introductionmentioning

confidence: 99%

Penetration profile and human cadaver skin distribution of finasteride from vesicular nanocarriers

et al. 2013

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“…120 This mouse strain is susceptible to the T lymphocyte immune response, showing strong delayed allergic reaction that affects ear thickness. Tacrolimus is a poorly hydrophilic (4 µg/mL), lipophilic (logP = 3.3) drug molecule with a 23-member macrolide lactone structure.…”

Section: Preclinical Applications As Antiscarring Anti-atopic Dermatmentioning

confidence: 99%

Highly deformable and highly fluid vesicles as potential drug delivery systems: theoretical and practical considerations

Romero¹,

Morilla²

2013

IJN

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Vesicles that are specifically designed to overcome the stratum corneum barrier in intact skin provide an efficient transdermal (systemic or local) drug delivery system. They can be classified into two main groups according to the mechanisms underlying their skin interaction. The first group comprises those possessing highly deformable bilayers, achieved by incorporating edge activators to the bilayers or by mixing with certain hydrophilic solutes. The vesicles of this group act as drug carriers that penetrate across hydrophilic pathways of the intact skin. The second group comprises those possessing highly fluid bilayers, owing to the presence of permeation enhancers. The vesicles of this group can act as carriers of drugs that permeate the skin after the barrier of the stratum corneum is altered because of synergistic action with the permeation enhancers contained in the vesicle structure. We have included a detailed overview of the different mechanisms of skin interaction and discussed the most promising preclinical applications of the last five years of Transfersomes ® (IDEA AG, Munich, Germany), ethosomes, and invasomes as carriers of antitumoral and anti-inflammatory drugs applied by the topical route.

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“…With the aim of improving percutaneous permeation, various approaches based on colloidal vesicles have been developed for FK506 dermal delivery. Microemulsion, 6 ethosomes, 8 lipid nanoparticles (NPs), 9 and modified nanolipid carrier 10 have been addressed, and they all presented enhanced FK506 percutaneous permeation. However, each of these approaches has its respective challenges in terms of safety, feasibility, or stability, for example, considerable surfactants for microemulsion, hot homogenization preparation for lipid NPs and modified nanolipid carrier, and lecithin stability for ethosomes.…”

Section: Introductionmentioning

confidence: 99%

“…8,49,50 As we described earlier, FK506-loaded ethosomes, lipid NPs, or modified lipid NPs were reported to enhance FK506 penetration, resulting in an enhanced efficacy for treating AD. 8,49,50 Therefore, the synergistically enhanced penetration of FK506 by the combination of HA-Chol-NPs with NIC also suggests that FK506-HA-Chol-NPs-NIC will exert an enhanced effect on treating skin diseases compared to FK506-HA-CholNPs, FK506-NIC complex, FK506 aqueous suspension, or commercial ointment. In clinic, FK506 has been investigated successfully in the management of AD and psoriasis.…”

mentioning

confidence: 99%

Combination of hydrotropic nicotinamide with nanoparticles for enhancing tacrolimus percutaneous delivery

Pan¹,

Qin²,

Zhang³

et al. 2016

IJN

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Tacrolimus (FK506), an effective immunosuppressant for treating inflammatory skin diseases, hardly penetrates into and through the skin owing to its high hydrophobicity and molecular weight. The aim of this study was to develop a hybrid system based on nicotinamide (NIC) and nanoparticles (NPs) encapsulating FK506, such as FK506–NPs–NIC, for facilitating percutaneous delivery, which exploited virtues of both NIC and NPs to obtain the synergetic effect. Solubility and percutaneous permeation studies were carried out. The results showed that NIC could increase the solubility and permeability of FK506 and that 20% (w/v) NIC presented higher FK506 permeability and was thus chosen as the hydrotropic solution to solubilize FK506 and prepare FK506–NPs–NIC. Hyaluronic acid (HA) was chemically conjugated with cholesterol (Chol) to obtain amphiphilic conjugate of HA–Chol, which self-assembled NPs in 20% NIC solution containing FK506. The particle size, zeta potential, and morphology of NPs were characterized. The encapsulation efficiency and in vitro percutaneous permeation of NPs were evaluated in the presence and absence of NIC. The results demonstrated that hydrotropic solubilizing FK506 was readily encapsulated into NPs with a higher encapsulation efficiency of 79.2%±4.2%, and the combination of NPs with NIC exhibited a significantly synergistic effect on FK506 deposition within the skin (2.39±0.53 μg/cm 2 ) and penetration through the skin (13.38±2.26 μg/cm 2 ). The effect of the combination of NPs with NIC on drug permeation was further visualized by confocal laser scanning microscope through in vivo permeation studies, and the results confirmed that NPs–NIC synergistically enhanced the permeation of the drug into the skin. The cellular uptake performed in HaCaT cells presented a promoting effect of NPs on cellular uptake. These overall results demonstrated that HA–Chol–NPs–NIC can synergistically improve the percutaneous delivery of FK506, and it is a novel potential strategy based on a nano-sized carrier for FK506 to treat skin diseases.

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Tacrolimus-loaded ethosomes: Physicochemical characterization and in vivo evaluation

Cited by 117 publications

References 80 publications

Penetration profile and human cadaver skin distribution of finasteride from vesicular nanocarriers

Penetration profile and human cadaver skin distribution of finasteride from vesicular nanocarriers

Highly deformable and highly fluid vesicles as potential drug delivery systems: theoretical and practical considerations

Combination of hydrotropic nicotinamide with nanoparticles for enhancing tacrolimus percutaneous delivery

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