Mixed Polymeric Micelles for Rapamycin Skin Delivery

Guyader, Guillaume Le; Do, Bernard; Rietveld, Ivo B.; Coric, Pascale; Bouaziz, Serge; Secrétan, Philippe-Henri; Andrieux, Karine; Paul, Muriel

doi:10.3390/pharmaceutics14030569

Cited by 12 publications

(5 citation statements)

References 46 publications

(59 reference statements)

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“…The results showed no trace amount of rapamycin in the rapamycin‐texosomes group. In a study by Guyader et al., they evaluated rapamycin‐unloaded micelle and rapamycin‐loaded micelle by FTIR, and the rapamycin IR spectra were similar to our results 65 …”

Section: Discussionsupporting

confidence: 86%

“…In a study by Guyader et al, they evaluated rapamycinunloaded micelle and rapamycin-loaded micelle by FTIR, and the rapamycin IR spectra were similar to our results. 65 Furthermore, the HPLC method for rapamycin and texosome groups showed that we had a symmetric peak shape with good resolution for all the designed groups. In the free rapamycin group, the obtained peak shape is typical and is similar to the study by Rao et al 66 The peak shape similarity in free exosome and texosome groups found no trace amount of rapamycin in the texosome group.…”

Section: Discussionmentioning

confidence: 87%

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Exosomes derived from rapamycin‐treated 4T1 breast cancer cells induced polarization of macrophages to M1 phenotype

Ghalavand

Moradi‐Chaleshtori

Dorostkar

et al. 2023

Biotech and App Biochem

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M2 macrophages are the most prevalent type in the tumor microenvironment and their polarization to M1 type can be used as a potential cancer immunotherapy. Here, we investigated the role of tumor microenvironment and particularly purified exosomes in M2 to M1 macrophage polarization. Rapamycin treatment on triple‐negative breast cancer cells (TNBC) was performed. Tumor cells‐derived exosomes (called texosomes) were isolated and characterized using scanning electron microscopy, transmission electron microscopy, dynamic light scattering, high‐performance liquid chromatography, Fourier transform infrared, and Western blot assays. M2 mouse peritoneal macrophages were treated with rapamycin or rapamycin‐texosome. Then, M1/M2 phenotype‐specific marker genes and proteins were measured to assess the degree of M2 to M1 polarization. Finally, nitric oxide (NO) production, phagocytosis, and efferocytosis assays were assessed to verify the functionality of the polarized macrophages. Purified rapamycin‐texosomes significantly increased the expression of the M1 markers (Irf5, Nos2, and CD86) and decreased M2 markers (Arg, Ym1, and CD206). In addition, the levels of M1‐specific cytokines tumor necrosis factor alpha and interleukin 1β (IL‐1β) were increased, whereas the levels of M2 specific cytokines IL‐10 and transforming growth factor beta were declined. Furthermore, texosome treatment increased NO concentration and phagocytosis and decreased efferocytosis indicating M1 polarization. These findings suggest rapamycin‐texosomes can induce M2 to M1 macrophages polarization as a potential immunotherapy for TNBC.

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Section: Discussionsupporting

confidence: 86%

Section: Discussionmentioning

confidence: 87%

Exosomes derived from rapamycin‐treated 4T1 breast cancer cells induced polarization of macrophages to M1 phenotype

Ghalavand

Moradi‐Chaleshtori

Dorostkar

et al. 2023

Biotech and App Biochem

View full text Add to dashboard Cite

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“…73 Guillaume et al have used cryo-TEM to determine the rapamycin-loaded spherical micelles. 74 There are different architectures and shapes of micellar structures confirmed by using TEM, as reported in the literature. 75,76…”

Section: ■ Results and Discussionmentioning

confidence: 64%

“…They have shown that with change in temperature the morphology of micelles was changed from spherical to prolate ellipsoid . Guillaume et al have used cryo-TEM to determine the rapamycin-loaded spherical micelles . There are different architectures and shapes of micellar structures confirmed by using TEM, as reported in the literature. , …”

Section: Resultsmentioning

confidence: 94%

Development of Cholinium-Based API Ionic Liquids with Enhanced Drug Solubility: Biological Evaluation and Interfacial Properties

Bhat,

Padder,

Husain

et al. 2024

Mol. Pharmaceutics

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We report an efficient sustainable two-step anion exchange synthetic procedure for the preparation of choline API ionic liquids (Cho-API-ILs) that contain active pharmaceutical ingredients (APIs) as anions combined with choline-based cations. We have evaluated the in vitro cytotoxicity for the synthesized compounds using three different cells lines, namely, HEK293 (normal kidney cell line), SW480, and HCT 116 (colon carcinoma cells). The solubility of APIs and Cho-API-ILs was evaluated in water/ buffer solutions and was found higher for Cho-API-ILs. Further, we have investigated the antimicrobial potential of the pure APIs, ILs, and Cho-API-ILs against clinically relevant microorganisms, and the results demonstrated the promise of Cho-API-ILs as potent antimicrobial agents to treat bacterial infections. Moreover, the aggregation and adsorption properties of the Cho-API-ILs were observed by using a surface tension technique. The aggregation behavior of these Cho-API-ILs was further supported by conductivity and pyrene probe fluorescence. The thermodynamics of aggregation for Cho-API-ILs has been assessed from the temperature dependence of surface tension. The micellar size and their stability have been studied by dynamic light scattering, transmission electron microscopy, and zeta potential. Therefore, the duality in the nature of Cho-API-ILs has been explored with the upgradation of their physical, chemical, and biopharmaceutical properties, which enhance the opportunities for advances in pharmaceutical sciences.

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“…The results showed that rapamycin deposition in the different skin layers ( stratum corneum , viable epidermis, upper and lower dermis) significantly increased with micelle solution 0.2% after 24 h compared with the ointment. Based on these results, Le Guyader et al 46 evaluated the different stability and skin bioavailability of rapamycin in polymeric micelles (created by combining TPGS with a poloxamer P123) and their respective hydrogel solution to define an optimized formulation to effectively treat FA.…”

Section: Resultsmentioning

confidence: 99%

Analysis of current data on the use of topical mTOR inhibitors in the treatment of facial angiofibromas in tuberous sclerosis complex—An update

Balestri¹,

Rizzoli²,

Pedrolli³

et al. 2022

Acad Dermatol Venereol

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Tuberous sclerosis complex (TSC) is an autosomal dominant neurocutaneous syndrome causing hamartomatous growths in multiple organs. Facial angiofibromas occur in up to 80% of patients and can be highly disfiguring. Treatment for these lesions is challenging. Recently, topical rapamycin has been proposed as an effective option to treat angiofibromas but a commercially available compound has not yet been developed in Europe. We conducted a retrospective review with the aim to update the current data on the use of topical rapamycin in the treatment of angiofibromas in TSC, focusing on the optimal concentration and trying to establish which vehicle should be preferred. Thirty‐nine reports describing the use of topical rapamycin in the treatment of angiofibromas in TSC were considered, involving a total of 483 patients. An improvement of the lesions has been shown in over 90% of subjects, particularly if the treatment was started at early stages. Several different formulations (ointment, gel, solution and cream) with a wide range of concentrations (0.003%–1%) were proposed, of which a pharmacological analysis has also been performed. Topical rapamycin can be considered an effective and safe option for the treatment and the prevention of facial angiofibromas in younger patients, but the best formulation has yet to be established. Our review demonstrates that ointment and gel should be preferred, but it is not clear which concentration is optimal. However, according to this study, the 0.1% concentration represents the first choice. Long‐term and comparative studies between topical rapamycin formulations are required in order to establish which treatment has a better outcome and lower recurrence rate.

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Mixed Polymeric Micelles for Rapamycin Skin Delivery

Cited by 12 publications

References 46 publications

Exosomes derived from rapamycin‐treated 4T1 breast cancer cells induced polarization of macrophages to M1 phenotype

Exosomes derived from rapamycin‐treated 4T1 breast cancer cells induced polarization of macrophages to M1 phenotype

Development of Cholinium-Based API Ionic Liquids with Enhanced Drug Solubility: Biological Evaluation and Interfacial Properties

Analysis of current data on the use of topical mTOR inhibitors in the treatment of facial angiofibromas in tuberous sclerosis complex—An update

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