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Improved Dermal Delivery of Cyclosporine A Loaded in Solid Lipid Nanoparticles.


ABSTRACT: Cyclosporine A (CsA) is an immunosuppressant frequently used in the therapy of autoimmune disorders, including skin-related diseases. Aiming towards topical delivery, CsA was successfully incorporated into lipid nanoparticles of Lipocire DM and Pluronic F-127 using the hot homogenization method. Two different nanocarriers were optimized: solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) where oleic acid was the liquid lipid. The developed nanoparticles showed mean sizes around 200 nm, a negative surface charge, and drug entrapment efficiencies around 85% and 70% for SLNs and NLCs, respectively. The spherical CsA-loaded lipid nanoparticles were stable for 9 weeks when stored at room temperature, and exhibited in vitro pH-dependent release under skin mimetic conditions, following the Peppas-Korsmeyer model. CsA, when loaded in SLNs, was safe to be used up to 140 ?g mL-1 in fibroblasts and keratinocytes, while CsA-loaded NLCs and free drug exhibited IC50 values of 55 and 95 ?g mL-1 (fibroblasts) and 28 and 30 ?g mL-1 (keratinocytes), respectively. The developed SLNs were able to retain the drug in pork skin with a reduced permeation rate in relation to NLCs. These findings suggest that SLNs are a potential alternative to produce stable and safe CsA nanocarriers for topical administration.

SUBMITTER: Essaghraoui A 

PROVIDER: S-EPMC6780175 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature

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Improved Dermal Delivery of Cyclosporine A Loaded in Solid Lipid Nanoparticles.

Essaghraoui Abderrazzaq A   Belfkira Ahmed A   Hamdaoui Bassou B   Nunes Cláudia C   Lima Sofia A Costa SAC   Reis Salette S  

Nanomaterials (Basel, Switzerland) 20190827 9


Cyclosporine A (CsA) is an immunosuppressant frequently used in the therapy of autoimmune disorders, including skin-related diseases. Aiming towards topical delivery, CsA was successfully incorporated into lipid nanoparticles of Lipocire DM and Pluronic F-127 using the hot homogenization method. Two different nanocarriers were optimized: solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) where oleic acid was the liquid lipid. The developed nanoparticles showed mean sizes a  ...[more]

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