Corticosteroids for Skin Delivery: Challenges and New Formulation Opportunities

Şenyiğit, Taner; Özer, Özgen

doi:10.5772/53909

Cited by 16 publications

(16 citation statements)

References 79 publications

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“…In the next step, the glucocorticoid DXM was selected as a therapeutically relevant drug from daily practice, and loaded onto CMS nanocarriers. Topical corticosteroid administration is a benchmark therapy for inflammatory skin diseases such as atopic dermatitis [65]. Well in line with the NR penetration studies, the CMS nanocarriers delivered DXM significantly more efficient (~ 3-fold) into the viable epidermis of excised human skin compared to the commercially available DXM cream (Fig.…”

Section: Dermal Drug Delivery Efficiencymentioning

confidence: 91%

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Tailored dendritic core-multishell nanocarriers for efficient dermal drug delivery: A systematic top-down approach from synthesis to preclinical testing

Hönzke

Gerecke

Elpelt

et al. 2016

Journal of Controlled Release

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Section: Dermal Drug Delivery Efficiencymentioning

confidence: 91%

“…6). Furthermore, the effectiveness of corticosteroids is directly related to the composition of its formulation, and incorporation in cream is known to reduce their efficacy [65]. …”

Section: Anti-inflammatory Efficiency Of Dxm Loaded Ester-based Cms Nmentioning

confidence: 99%

Tailored dendritic core-multishell nanocarriers for efficient dermal drug delivery: A systematic top-down approach from synthesis to preclinical testing

Hönzke

Gerecke

Elpelt

et al. 2016

Journal of Controlled Release

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“…However, the use of topical glucocorticoids can result in several local and adverse systemic effects, such as epidermis, dermis, or even subcutaneous tissue atrophy, resulting in irreversible stretch marks and in disorder of the wound-healing processes. Adverse systemic effects include body weight increase, Cushing's syndrome, hypertension, diabetes mellitus, growth retardation, osteoporosis, peptic ulcer, and gastritis (Schacke, Docke, Asadullah, 2002;Senyigit, Ozer, 2012).…”

Section: Introductionmentioning

confidence: 99%

“…However, due to its high potency, it displays dose-dependent toxicity and local and systemic adverse effects. In order to reduce the drug toxicity and to improve its action, halcinonide can be encapsulated into nanostructured systems, such as nanoparticles, which promote a controlled release of the drug in specific sites (Schaffazick, Guterres, 2003;Senyigit, Ozer, 2012). Nanostructured systems, such as nanoparticles, are submicron size ranged-usually spherical-drug carriers.…”

Section: Introductionmentioning

confidence: 99%

A simple HPLC method for the determination of halcinonide in lipid nanoparticles: development, validation, encapsulation efficiency, and in vitro drug permeation

Lopes

Langoski

Klein

et al. 2017

Braz. J. Pharm. Sci.

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Halcinonide is a high-potency topical glucocorticoid used for skin inflammation treatments that presents toxic systemic effects. A simple and quick analytical method to quantify the amount of halcinonide encapsulated into lipid nanoparticles, such as polymeric lipid-core nanoparticles and solid lipid nanoparticles, was developed and validated regarding the drug's encapsulation efficiency and in vitro permeation. The development and validation of the analytical method were carried out using the high performance liquid chromatography with the UV detection at 239 nm. The validation parameters were specificity, linearity, precision and accuracy, limits of detection and quantitation, and robustness. The method presented an isocratic flow rate of 1.0 mL.min -1 , a mobile phase methanol:water (85:15 v/v), and a retention time of 4.21 min. The method was validated according to international and national regulations. The halcinonide encapsulation efficiency in nanoparticles was greater than 99% and the in vitro drug permeation study showed that less than 9% of the drug permeated through the membrane, indicating a nanoparticle reservoir effect, which can reduce the halcinonide's toxic systemic effects. These studies demonstrated the applicability of the developed and validated analytical method to quantify halcinonide in lipid nanoparticles.Uniterms: Halcinonide/encapsulation efficiency. Halcinonide/quantification. Polymeric lipid-core nanoparticles. Solid lipid nanoparticles. Topical administration. Toxicity. High performance liquid chromatography/method validation.

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“…to increase their topical bioavailability, to deliver them to the skin as target siteepidermis and/or dermis -and to reduce the dose and frequency of administration for better safety [6,7]. Apart from the development of new molecules, one of the main strategies currently studied to overcome these challenges is the use of drug delivery systems.…”

mentioning

confidence: 99%

Submicron polymeric particles prepared by vibrational spray-drying: Semisolid formulation and skin penetration/permeation studies

Beber¹,

Andrade²,

Kann³

et al. 2014

European Journal of Pharmaceutics and Biopharmaceutics

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Topical glucocorticoids (TG) such as dexamethasone (DEX) have been used for decades for the treatment of skin diseases. However, TG present welldocumented side effects and their delivery to the skin is often insufficient.Therefore, many efforts have been undergone to improve the amount of drug delivered to the skin and to reduce side effects at the same time. In this work, the feasibility of DEX-submicron polymeric particles (SP) prepared by vibrational spray-drying as an approach to overcome the challenges associated with the topical administration of this drug class was evaluated. DEX was homogeneously dispersed in the SP matrix, according to confocal Raman microscopy analysis. Drug-loaded SP were incorporated into the oil phase of oil-in-water emulsions (creams). The formulation containing polymeric submicron particles (C-SP) showed controlled drug release kinetics and a significant drug accumulation in skin compared to formulations containing nonpolymeric particles or free drug. DEX accumulation in the stratum corneum was evaluated by tape stripping and a depot effect over time was observed for C-SP, while the formulation containing the free drug showed a decrease over time.Similarly, C-SP presented higher drug retention in epidermis and dermis in skin penetration studies performed on pig skin in Franz diffusion cells, while drug permeation into the receptor compartment was negligible. It was demonstrated, for the first time, the advantageous application of submicron polymeric particles obtained by vibrational spray-drying in semisolid formulations for cutaneous administration to overcome challenges related to the therapy with TG such as DEX.

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Corticosteroids for Skin Delivery: Challenges and New Formulation Opportunities

Cited by 16 publications

References 79 publications

Tailored dendritic core-multishell nanocarriers for efficient dermal drug delivery: A systematic top-down approach from synthesis to preclinical testing

Tailored dendritic core-multishell nanocarriers for efficient dermal drug delivery: A systematic top-down approach from synthesis to preclinical testing

A simple HPLC method for the determination of halcinonide in lipid nanoparticles: development, validation, encapsulation efficiency, and in vitro drug permeation

Submicron polymeric particles prepared by vibrational spray-drying: Semisolid formulation and skin penetration/permeation studies

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