Systematic optimization, characterization of Mycophenolic acid loaded nanostructured lipid carrier embedd ed nanogel for improved permeation and in vivo antipsoriatic activity

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY(2023)

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摘要
The current study focused on developing Mycophenolic acid (MPA) - loaded nanostructured lipid carriers (NLCs), enhancing skin penetration and efficacy for psoriasis. MPA-loaded NLCs (MPA-NLCs) were prepared using a hot homogenization process incorporating glyceryl behenate, oleic acid, and span 80. Pareto and Box Behnken designs were used in the experiment's strategy to optimize NLCs and determine how the amount of lipid, homogenization speed, and surfactant concentration affect particle size, zeta potential, and entrapment effectiveness. The optimized formulation showed 161.8 nm particle size,-53 mV zeta potential, and 88.92 % entrapment efficiency. It was characterized for XRD, DSC, FTIR, morphological (SEM, TEM, AFM), and in-vitro studies. The in-vitro study demonstrated the formulation's initial burst release followed by sustained release, showing a maximum release of 67.87 % through MPA-NLC compared to MPA-nano gel at 43.61 %. Excellent stability was observed at room temperature. The MPA-NLC was incorporated in Carbopol 940 to form MPA-nano gel and evaluated for pH, spreadability, viscosity, drug content, and texture analysis compared with MPA-gel. The ex-vivo permeation exhibited prolonged release of MPA from MPA-nano gel (415.36 mu g/cm2) versus MPA-gel (212.3 mu g/cm2) up to 24 h showing its effectivity in delivering MPA to a deeper layer.Furthermore, it effectively attenuated the PASI score showing excellent recovery in mice skin while MPA-NLC exhibited psoriasis. The dermatokinetic parameters revealed that MPA-nano gel had the potential to avoid systemic uptake and its related side effects. Moreover, good skin tolerability and safety were obtained through MPA-nano gel which was confirmed through histopathological and biochemical studies. Given the results, MPA-nano gel has been designed with promising potential and is scalable for delivering MPA through topical administration and treating psoriasis.
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关键词
Nanostructured lipid carrier,Anti-inflammatory,Psoriasis,MPA,Histopathological,Penetration,Sustained release
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