Tacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose

Yu, Kaiyue; Wang, Yixuan; Wan, Tao; Zhai, Yuanhao; Cao, Sisi; Ruan, Wenyi; Wu, Chuanbin; Xu, Yang

doi:10.2147/ijn.s150319

Cited by 53 publications

(27 citation statements)

References 72 publications

(77 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…After the sensitization, 100 μL and 10 μL of 1.0% (w/v) DNCB were repeatedly applied to the sensitized dorsal skin and the right ear, respectively, on days 4, 7, 11, 14, 17, 20, 23, 26, and 28 for challenge. The control group was treated with NS instead of DNCB 33…”

Section: Methodsmentioning

confidence: 99%

<p>Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects</p>

Wang¹,

Cao²,

Yu³

et al. 2019

IJN

Self Cite

View full text Add to dashboard Cite

Background: Topical application of tacrolimus (FK506) was effective in treating atopic dermatitis (AD); however, the therapeutic efficiency is hampered by its poor penetration into the skin and local side effects of transient irritation symptoms with a burning sensation, a feeling of warmth or heat. Menthol and camphor have been widely used in topical compound formulations for adjunctive pharmacotherapy for antipruritics and analgesics owing to their cool nature, and both present skin penetration enhancing effects. Moreover, they can form a liquid eutectic oil to solubilize hydrophobic drugs. Purpose: Taking advantages of menthol/camphor eutectic (MCE), this work aims to integrate FK506 into MCE to construct a microemulsion system, i.e., FK506 MCE ME, which simultaneously enhances the percutaneous delivery and treatment efficacy, while reduces the side effects of FK506. Methods: The formulation of FK506 MCE ME was optimized and characterized. Different formulations containing FK506 were topically administered to treat 1–chloro–2, 4–dinitrobenzene (DNCB)-induced murine AD. Results: MCE solubilized FK506. FK506 in MCE ME penetrated skin in vitro more than in the commercial ointment, and MCE predominantly exerted the enhancing effects in MCE ME. FK506 MCE ME or FK506 MCE ME gel had greater effects on clinical symptoms, histological analysis, and IgE than did commercial FK506. The anti-pruritic and down-regulation of substance P effects of MCE ME vehicle mitigated the side effects of FK506 application. Conclusion: MCE ME presented the excellent properties of simultaneously enhancing the percutaneous delivery and treatment efficacy, while reducing the side effects of FK506 for AD. Therefore, MCE ME is a promising nanoscale system for FK506 to effectively treating AD with low irritation and high medication adherence. Chemical compounds studied in this article: Tacrolimus (PubChem CID: 445643); menthol (PubChem CID: 1254); camphor (PubChem CID: 2537)

show abstract

Section: Methodsmentioning

confidence: 99%

<p>Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects</p>

Wang¹,

Cao²,

Yu³

et al. 2019

IJN

Self Cite

View full text Add to dashboard Cite

show abstract

“…Yu et al ( 56 ) explored the development of a hybrid skin-targeting nano system with nicotinamide (NIC) and chitosan NP (CS@NP) for encapsulating Tacrolimus (FK506), i.e., FK506@NIC@CSNP, for the treatment of dermatitis. Results showed that FK506 containing NIC@CSNP has significantly enhanced penetration and deposition into the skin as compared to Protopic®.…”

Section: Nanomedicines For Atopic Dermatitis—current Scenariomentioning

confidence: 99%

Emerging Nanomedicines for the Treatment of Atopic Dermatitis

et al. 2021

View full text Add to dashboard Cite

Globally, the prevalence of Atopic dermatitis (AD) is significantly increasing and affecting around 20% of population including children. Complex interactions amongst abnormality in epidermal barrier function, environment, infectious agents and immunological defects are considered as key factors in the pathogenesis of AD. Although the role of oxidative stress has been studied in some skin diseases, investigation of the same in AD is intermittent. Calcineurin inhibitors and/or topical corticosteroids are currently available; however, it causes atrophy of the skin, burning sensation, and systemic side effects which leads to poor patient compliance. These limitations provoke the strong need to develop an innovative approach in managing AD. Nanomaterials for effective drug delivery to skin conditions such as AD have attracted a lot of attention owing to its ability to encapsulate, protect, and release the cargo at the diseased skin site. However, there are lots of unmet challenges especially in terms of development of non-toxic formulations and clinical translation of established nanomedicines in the form of accessible products. Numerous formulations have emerged as carrier for poorly soluble and permeable drugs, viz., lipidic, polymeric, metal, silica, liposomes, hydrocarbon gels and this field is evolving. This review is intended to provide an insight incidences associated with pathophysiology of AD and challenges with existing treatments of AD. Focus is kept on reviewing current development and emerging nanomedicines for effective treatment of AD. The review also inculcates merits of several nanomedicines in overcoming challenges of existing products and its future implications.

show abstract

“…Chitosan nanoparticles have been proposed for the delivery of nicotinamide and tacrolimus for the treatment of AD [89], and their in vitro and in vivo permeation compared to a commercial ointment (Protopic). The authors reported that the enhanced permeation effect of NPs through, and into, the skin, contributed to increased amounts of tacrolimus in the skin.…”

Section: Nanoparticles For Atopic Dermatitismentioning

confidence: 99%

Trends in Atopic Dermatitis—From Standard Pharmacotherapy to Novel Drug Delivery Systems

Souto

Dias-Ferreira

Oliveira

et al. 2019

IJMS

View full text Add to dashboard Cite

Atopic dermatitis (AD) is a predominant and deteriorating chronic inflammation of the skin, categorized by robust burning and eczematous lacerations in diverse portions of the body. AD affects about 20% of both offspring and adults worldwide. The pathophysiology of AD combines environmental, hereditary, and immunological aspects, together with skin barrier dysfunction. The procedures used to prevent the disease are the everyday usage of creams to support the restoration of the epidermal barrier. The classical treatments include the use of topical corticosteroids as a first-line therapy, but also calcineurin inhibitors, antihistamines, antibiotics, phototherapy, and also immunosuppressant drugs in severe cases of AD. Topical drug delivery to deeper skin layers is a difficult task due to the skin anatomic barrier, which limits deeper penetration of drugs. Groundbreaking drug delivery systems, based on nanoparticles (NPs), have received much attention due to their ability to improve solubility, bioavailability, diffusion, targeting to specific types of cells, and limiting the secondary effects of the drugs employed in the treatment of AD. Even so, additional studies are still required to recognize the toxicological characteristics and long-term safety of NPs. This review discusses the current classical pharmacotherapy of AD against new nanoparticle skin delivery systems and their toxicologic risks. a prevalence of atopic conditions, as allergic rhinitis or bronchial asthma, and food allergies [2]. Topical administration of drugs is still the main therapeutic approach for AD. Despite this, several disadvantages may be cited as reduced patient compliance (a consequence of adverse effects as skin irritation or allergy), low efficiency, and specificity of these systems in delivering therapeutic drugs [3]. Innovative drug delivery systems should, therefore, exhibit the capacity to penetrate the stratum corneum (SC), which is naturally impermeable to a range of substances, in order to reduce adverse effects and increase drug targeting [3][4][5]. There is still no medication capable of reversing the pathological effects of AD. However, formulations based on nanoparticles (NPs) have been exploited for topical administration of drugs and are expected to overcome the above-mentioned limitations [6][7][8]. PathophysiologyAD, also called atopic eczema, is the most common skin disease, characterized by a pattern of pruritus, skin deterioration, and chronic inflammation [1,6,7]. This illness affects individuals in early-, mid-or late-stages of their lives and does not have a known cure so far. Over the course of the disease, the levels of IgE increase drastically leading to cutaneous signals that appear in early ages and persist until late stages of life, when they begin to disappear. Because of this, AD is also labelled as "allergic march" [2].AD results from a multiplicity of factors such as environmental injuries, impairments against the natural barrier of the skin and response of the immune system. This latter enhances the ac...

show abstract

Tacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose

Cited by 53 publications

References 72 publications

<p>Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects</p>

<p>Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects</p>

Emerging Nanomedicines for the Treatment of Atopic Dermatitis

Trends in Atopic Dermatitis—From Standard Pharmacotherapy to Novel Drug Delivery Systems

Contact Info

Product

Resources

About