Dermal miconazole nitrate nanocrystals – formulation development, increased antifungal efficacy &amp; skin penetration

Superficial fungal infection in immunocompromised patients can lead to many disorders and complications. Currently, new topical treatment options are critically needed to treat these fungal infections. Luliconazole (LZL) is a topical antifungal medicine used for fungal infection treatment. The purpose of this paper was to develop a new topical luliconazole nanocrystal (LNC) incorporated hydrogel. This study suggested the potential benefits of LNC embedded in a gel as a drug delivery system for topical antifungal treatments. Preliminary experiments were therefore carried out to characterize the LNC in comparison with raw drug. Prepared gel was homogeneous for human use with about 88 percent trapping, non-irritant and safe. Nano-systems showed an overall 5 fold enhancement in solubility, 4 fold increase in dissolution velocity, higher skin retention and better antifungal activity. Drugs retained from LNC hydrogel (N-GEL) in different skin layers within 8 h were the highest, i.e. 62.17% compared to coarse suspension (41.87%), nanosuspension (49.77%), D-GEL (55.76%). In addition, LNC and N-GEL had higher ZOI (41.20 ± 0.61mm and 44.25 ± 0.57mm respectively) than LZL and D-GEL (35.98 ± 0.81mm and 36.83 ± 0.83mm respectively). Therefore, it was observed that LNC loaded hydrogel was more effective in killing the fungus. Consequently, hydrogel incorporated with LNC could be a new approach with improved activity and increased dermal delivery for drugs with poor aqueous solubility rather than coarse drug containing gel.

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“…All plates were incubated for 72 h at 30 °C. The inhibition zone assay samples were examined in triplicate [30].…”

Section: Methodsmentioning

confidence: 99%

Preparation of luliconazole nanocrystals loaded hydrogel for improvement of dissolution and antifungal activity

Kumar

Nithya²,

Mahato³

et al. 2019

Heliyon

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“…82 The most important mechanism of nanocrystals skin penetration enhancement is the increment of saturation solubility and, therefore, increase in concentration gradient leading to higher passive diffusion of active pharmaceuticals through skin layers. 77 , 83 Some advantages and disadvantages of nanocrystals as nanocarriers in topical drug delivery systems are listed in Table 6 .…”

Section: Nanocarriers and Nanoparticlesmentioning

confidence: 99%

<p>Potential of Nanoparticles as Permeation Enhancers and Targeted Delivery Options for Skin: Advantages and Disadvantages</p>

Ghasemiyeh

Mohammadi-Samani

2020

DDDT

188

113

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The topical route of administration has many advantages for the treatment of various skin disorders as well as cosmeceutical purposes. This route bypasses hepatic firstpass effect and systemic availability of many pharmaceuticals is limited to skin organelles such as hair follicles and so could avoid unwanted adverse reactions and increase the localized therapeutic effect. Despite such attributed advantages of the topical route, the most important challenge is skin barrier characteristics that should be overcome to obtain dermal or trans-dermal drug delivery. Different approaches have been recruited to overcome this barrier. In this review, different types of nanoparticles for skin permeation enhancement and targeted delivery to skin organelles are discussed. The potential mechanisms of each nanocarrier in permeation enhancement and dermal delivery are considered and finally, the most important advantages and disadvantages of each group are summarized.

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“…Research has shown that dexamethasone nanocrystals significantly improved skin penetration compared to traditional dexamethasone creams and dexamethasone-loaded ethyl cellulose nanocarriers. These findings also showed that much of the medication was deposited in the dermis layer in nanocrystal formulations relative to traditional nanocarriers in which much of the drug stayed in the epidermis and rapid skin permeation was observed for nanocrystal (Pyo et al, 2017).…”

Section: Nanocrystalsmentioning

confidence: 82%

Enhancing Permeation of Drug Molecules Across the Skin via Delivery in Nanocarriers: Novel Strategies for Effective Transdermal Applications

Yang

et al. 2021

Front. Bioeng. Biotechnol.

182

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The transdermal route of administration provides numerous advantages over conventional routes i.e., oral or injectable for the treatment of different diseases and cosmetics applications. The skin also works as a reservoir, thus deliver the penetrated drug for more extended periods in a sustained manner. It reduces toxicity and local irritation due to multiple sites for absorption and owes the option of avoiding systemic side effects. However, the transdermal route of delivery for many drugs is limited since very few drugs can be delivered at a viable rate using this route. The stratum corneum of skin works as an effective barrier, limiting most drugs’ penetration posing difficulty to cross through the skin. Fortunately, some non-invasive methods can significantly enhance the penetration of drugs through this barrier. The use of nanocarriers for increasing the range of available drugs for the transdermal delivery has emerged as a valuable and exciting alternative. Both the lipophilic and hydrophilic drugs can be delivered via a range of nanocarriers through the stratum corneum with the possibility of having local or systemic effects to treat various diseases. In this review, the skin structure and major obstacle for transdermal drug delivery, different nanocarriers used for transdermal delivery, i.e., nanoparticles, ethosomes, dendrimers, liposomes, etc., have been discussed. Some recent examples of the combination of nanocarrier and physical methods, including iontophoresis, ultrasound, laser, and microneedles, have also been discussed for improving the therapeutic efficacy of transdermal drugs. Limitations and future perspectives of nanocarriers for transdermal drug delivery have been summarized at the end of this manuscript.

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Dermal miconazole nitrate nanocrystals – formulation development, increased antifungal efficacy & skin penetration

Cited by 38 publications

References 18 publications

Preparation of luliconazole nanocrystals loaded hydrogel for improvement of dissolution and antifungal activity

Preparation of luliconazole nanocrystals loaded hydrogel for improvement of dissolution and antifungal activity

<p>Potential of Nanoparticles as Permeation Enhancers and Targeted Delivery Options for Skin: Advantages and Disadvantages</p>

Enhancing Permeation of Drug Molecules Across the Skin via Delivery in Nanocarriers: Novel Strategies for Effective Transdermal Applications

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