Details

Autor(en) / Beteiligte

• Zhao, Yun-Chun
• Zheng, Hai-Li
• Wang, Xiao-Rong
• Zheng, Xiao-Ling
• Chen, Yue
• Fei, Wei-Dong
• Zheng, Yong-Quan
• Wang, Wen-Xi
• Zheng, Cai-Hong

Titel

Enhanced Percutaneous Delivery of Methotrexate Using Micelles Prepared with Novel Cationic Amphipathic Material

Ist Teil von

• International journal of nanomedicine, 2020-01, Vol.15, p.3539-3550

Ort / Verlag

New Zealand: Dove Medical Press Limited

Erscheinungsjahr

2020

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• Methotrexate (MTX) is an antiproliferative drug widely used to treat inflammatory diseases and autoimmune diseases. The application of percutaneous administration is hindered due to its poor transdermal penetration. To reduce side effects and enhanced percutaneous delivery of MTX, novel methotrexate (MTX)-loaded micelles prepared with a amphiphilic cationic material, -dimethyl-( -di-stearoyl-1-ethyl)1,3-diaminopropane (DMSAP), was designed. DMSAP was synthesized via three steps using simple chemical agents. H nuclear magnetic resonance and mass spectroscopy were used to confirm the successful synthesis of DMSAP. A safe and non-toxic phosphatidylcholine, soybean phosphatidylcholine (SPC), was added to DMSAP at different ratios to form P/D-micelles. Then, MTX-entrapped micelles (M/P/D-micelles) were prepared by electrostatic adsorption. The physicochemical properties and blood stability of micelles were examined thoroughly. In addition, the transdermal potential of the micelles was evaluated by permeation experiments. In aqueous environments, DMSAP conjugates could self-assemble spontaneously into micelles with a low critical micelle concentration (CMC) of 0.056 mg/mL. Stable, spherical MTX-entrapped micelles (M/P/D-micelles) with a size of 100-120 nm and high zeta potential of +36.26 mV were prepared. In vitro permeation studies showed that M/P/D-micelles exhibited superior skin permeability and deposition of MTX in the epidermis and dermis compared with that of free MTX. These special novel cationic M/P/D-micelles can enhance the permeability of MTX and are expected to be a promising percutaneous delivery system for therapy skin diseases.