Drug development and industrial pharmacy · 2022
Development and evaluation of a novel methotrexate-loaded electrospun patch to alleviate psoriasis plaques.
СтатьяНазвание и аннотация: Перевод в очереди
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Hashemi Shiva, Mortazavi Seyed Alireza, Moghimi Hamid Reza, Darbasizadeh Behzad
Аннотация
OBJECTIVE: To achieve an effective topical formulation of Methotrexate (MTX) as a first-line treatment of psoriasis, we formulated three MTX-loaded electrospun nanofibrous patches composed of polycaprolactone (PCL), Eudragit L100, and a mixture of them.
SIGNIFICANCE: Topical delivery of MTX provides an appropriate therapeutic performance while circumventing the life-threatening side effects of systemic administration.
METHODS: Three MTX-loaded electrospun nanofibrous patches were prepared and characterized in terms of size and morphology (using SEM), thermal behavior (by TGA and DSC), and crystalline structure (using XRD). Furthermore, the wettability and mechanical strength of samples were investigated through water contact angle and tensile strength tests. Also, the encapsulation efficiency of MTX was calculated. Subsequently, in vitro drug release profile of each formulation was obtained and different kinetic models were fitted to achieve the best-matched model. Accordingly, the ex vivo skin permeation of MTX was studied for the optimum formulation.
RESULTS: All samples showed appropriate morphology, thermal behavior, and encapsulation efficiency. Also, XRD results showed that MTX is dispersed within the polymeric matrices in the amorphous state (with no crystalline region). Release studies demonstrated that MTX-loaded Eudragit L100-PCL formulation outperformed in terms of mechanical behavior and in vitro drug release. This formulation also exhibited better skin permeation.
CONCLUSION: The obtained controlled-release MTX-loaded electrospun patches seem promising to provide a long-acting topical treatment of psoriatic plaques with minimized systemic side effects.
SIGNIFICANCE: Topical delivery of MTX provides an appropriate therapeutic performance while circumventing the life-threatening side effects of systemic administration.
METHODS: Three MTX-loaded electrospun nanofibrous patches were prepared and characterized in terms of size and morphology (using SEM), thermal behavior (by TGA and DSC), and crystalline structure (using XRD). Furthermore, the wettability and mechanical strength of samples were investigated through water contact angle and tensile strength tests. Also, the encapsulation efficiency of MTX was calculated. Subsequently, in vitro drug release profile of each formulation was obtained and different kinetic models were fitted to achieve the best-matched model. Accordingly, the ex vivo skin permeation of MTX was studied for the optimum formulation.
RESULTS: All samples showed appropriate morphology, thermal behavior, and encapsulation efficiency. Also, XRD results showed that MTX is dispersed within the polymeric matrices in the amorphous state (with no crystalline region). Release studies demonstrated that MTX-loaded Eudragit L100-PCL formulation outperformed in terms of mechanical behavior and in vitro drug release. This formulation also exhibited better skin permeation.
CONCLUSION: The obtained controlled-release MTX-loaded electrospun patches seem promising to provide a long-acting topical treatment of psoriatic plaques with minimized systemic side effects.