Polymeric micelle mediated follicular delivery of spironolactone: Targeting the mineralocorticoid receptor to prevent glucocorticoid-induced activation and delayed cutaneous wound healing

Dahmana, Naoual; Mugnier, Thibault; Gabriel, Doris; Favez, Tatiana; Kowalczuk, Laura; Béhar-Cohen, Francine; Gurny, Robert

doi:10.1016/j.ijpharm.2021.120773

Cited by 13 publications

(7 citation statements)

References 40 publications

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“…These results further confirmed the preferential delivery of nanocarriers (and AMF, a hydrophilic molecule) into the PSU [32,35]. It was noted that the selectivity of the "tritherapy" was less pronounced compared with the results for adapalene (4.5-and 3.3-fold for micelle solution and micelle gel, respectively) [32] and spironolactone (5-fold) [45]. The hypothesis was that the available volume within the pilosebaceous unit limited the number of nanocarriers that could be accumulated in each structure.…”

Section: Targeted Delivery To the Psusupporting

confidence: 67%

Simultaneous Delivery of Econazole, Terbinafine and Amorolfine with Improved Cutaneous Bioavailability: A Novel Micelle-Based Antifungal “Tri-Therapy”

2022

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Lack of accurate diagnosis and the use of formulations designed to address the poor aqueous solubility of antifungal agents, but not optimized for delivery, contribute to unsatisfactory outcomes for topical treatment of cutaneous mycoses. The objective of this study was to develop a micelle-based antifungal formulation containing econazole (ECZ), terbinafine (TBF) and amorolfine (AMF) using D-α-tocopheryl polyethylene glycol succinate (TPGS) for simultaneous cutaneous delivery of three agents with complementary mechanisms of action. The antifungal “tri-therapy” micelle-based formulation containing 0.1% ECZ, 0.1% TBF and 0.025% AMF had a drug loading 10-fold lower than the “reference” marketed formulations (Pevaryl®, 1% ECZ; Lamisil®, 1% TBF; Loceryl®, 0.25% AMF). Finite dose application of the micelle-based formulation for 6 h resulted in a statistically equivalent deposition of ECZ (p > 0.05) and TBF (p > 0.05) from the 2 systems, and a 2-fold higher accumulation of AMF (p = 0.017). Antifungal concentrations above MIC80 against Trichophyton rubrum were achieved in each skin layer with the “tri-therapy”, which also exhibited a preferential deposition of each antifungal agent in pilosebaceous unit (PSU)-containing biopsies as compared with PSU-free biopsies (p < 0.05). A planned clinical study will test whether these promising results translate to improved therapeutic outcomes in vivo.

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Section: Targeted Delivery To the Psusupporting

confidence: 67%

Simultaneous Delivery of Econazole, Terbinafine and Amorolfine with Improved Cutaneous Bioavailability: A Novel Micelle-Based Antifungal “Tri-Therapy”

2022

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“…Glucocorticoids are well-known anti-inflammatory hormone drugs, but long-term topical therapy of long-term injuries with glucocorticoids is prohibited, as the resulting dysfunction of keratinocytes and fibroblasts may lead to thinning of the skin. [114,150] As a result, their use in the treatment of long-term inflammatory diseases is restricted due to these severe adverse effects. A. Gauthier et al [151] developed liposomes loaded with dexamethasone phosphate and surface-modified phosphatidylserine for topical delivery of dexamethasone to macrophages to promote the polarization toward M2 macrophages.…”

Section: Biomaterials Load Hormones To Regulate Macrophage Polarizationmentioning

confidence: 99%

“…Glucocorticoids are well‐known anti‐inflammatory hormone drugs, but long‐term topical therapy of long‐term injuries with glucocorticoids is prohibited, as the resulting dysfunction of keratinocytes and fibroblasts may lead to thinning of the skin. [ 114,150 ] As a result, their use in the treatment of long‐term inflammatory diseases is restricted due to these severe adverse effects. A. Gauthier et al.…”

Section: Biomaterials Regulate Macrophage Polarization and Promote Wo...mentioning

confidence: 99%

Advanced Biomaterials for Regulating Polarization of Macrophages in Wound Healing

Mao

Chen

Cai

et al. 2021

Adv Funct Materials

120

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Macrophage immunotherapy is an emerging treatment strategy that modulates the immune system to promote wound healing. The functionality and regeneration of tissue depend on spatially and temporally regulating the biophysical and biochemical microenvironmental with poorly understood mechanisms. Biomaterials are carefully crafted to display and deliver macrophage regulatory signals in a precise and near‐physiological way, serving as powerful artificial microenvironments in which to explore and direct the fate of macrophages. The review starts with discussing the classification and function of macrophages, and then introduces the polarization of macrophages in different microenvironments of conventional wounds and chronic wounds. Recent advances in biomaterials that balance the phenotypes of macrophages in wound healing are emphasized. Finally, looking ahead, the potential ability of biomaterial scaffolds to modulate immune signaling to produce an environment conducive to regeneration is discussed.

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“…The more accurate and reliable results from this system make MS technology more widely applied in cosmetic and topical drug research. Many new delivery systems such as microneedle [48], Colloidal nanodispersions [49], Polymeric micelle mediated follicular [50], Sulfhydryl modified polymers [51], and polyamidoamine dendrimers [52] have been evaluated with MS technologies. In addition, LCMS is a very quick and effective tool to determine AI for skin benefits and a great linkage between traditional raw materials from botanical and food resources and skin efficacy validation [53].…”

Section: Mass Spectrometry Technologymentioning

confidence: 99%

Mini Review: Mass Spectrometry Technology for Molecule Distribution inside Skin

Hao¹

2022

Adv Res Dermatol Cosmetics

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The functional ingredients for skin-related products have been highly recognized accompanied by the consumers’ curiosity and instrumental improvement. The targeted location of a functional active ingredient in the skin organelle could be very critical information for its product development, safety evaluation, and benefit claims. Due to those factors, mass spectrometry technology exhibited rapid growth in those research areas because it can accurately and sensitively determine the ingredient molecular weights and locations. In this min review, a summarized figure was created for mass spectrometry technology applications in skin research in the last two decades or so. Compared to other related technologies, the uniqueness and advantage of chromatographic-mass spectrometry and mass spectrometry imaging were also emphasized. Several typical examples from separation, isotopic labeling, and combination with Franz cell were discussed.

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Polymeric micelle mediated follicular delivery of spironolactone: Targeting the mineralocorticoid receptor to prevent glucocorticoid-induced activation and delayed cutaneous wound healing

Cited by 13 publications

References 40 publications

Simultaneous Delivery of Econazole, Terbinafine and Amorolfine with Improved Cutaneous Bioavailability: A Novel Micelle-Based Antifungal “Tri-Therapy”

Simultaneous Delivery of Econazole, Terbinafine and Amorolfine with Improved Cutaneous Bioavailability: A Novel Micelle-Based Antifungal “Tri-Therapy”

Advanced Biomaterials for Regulating Polarization of Macrophages in Wound Healing

Mini Review: Mass Spectrometry Technology for Molecule Distribution inside Skin

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