Development of Halobetasol-loaded nanostructured lipid carrier for dermal administration: Optimization, physicochemical and biopharmaceutical behavior, and therapeutic efficacy.
Nanomedicine, 2019/08;20:102026.
Carvajal-Vidal P[1], Fábrega MJ[2], Espina M[1], Calpena AC[1], García ML[3]
Affiliations
PMID: 31170512DOI: 10.1016/j.nano.2019.102026
Impact factor: 6.458
Abstract
Halobetasol propionate (HB) is considered a super potent drug in the group of topical corticosteroids. HB has anti-inflammatory activity, vasoconstriction properties, and due to its high skin penetration, it can cause systemic side effects. To improve its characteristics, enhance topical effectiveness and reduce penetration to systemic circulation, a study to optimize and characterize a HB-loaded lipid nanocarrier (HB-NLC) has been made by high-pressure homogenization method. The formulation is composed by HB, surfactant, glyceryl distearate and capric glycerides. The optimized HB-NLC containing 0.01% of HB and 3% of total lipid shows an average size below 200 nm with a polydispersity index ≪0.2 and an encapsulation efficiency ≫90%. The in vitro and in vivo tests indicate that the HB-NLC is not toxic, is well tolerated and has an anti-inflammatory effect because they decrease the production of Interleukins in keratinocytes and monocytes. HB-NLC is considered an alternative treatment for skin inflammatory disorders.
Keywords: Corticosteroids; Halobetasol; Inflammation; Lipid nanocarrier; Skin diseases
MeSH terms
Administration, Cutaneous; Animals; Anti-Inflammatory Agents; Cell Death; Clobetasol; Drug Carriers; Female; Humans; Lipids; Male; Nanostructures; Rabbits; THP-1 Cells; Treatment Outcome
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