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Development And Characterization Of Starch/Gelatin Microneedle Arrays Loaded With Lecithin–Gelatin Nanoparticles Of Losartan For Transdermal Delivery

Ramón Andrés Pineda-Álvarez, M. J. Bernad-Bernad, I. M. Rodríguez-Cruz, José Juan Escobar-Chávez
Published 2020 · Materials Science

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The aim of this work was to develop and characterize biodegradable polymeric microneedle arrays loaded with (i) losartan potassium powder and (ii) nanoparticles loaded with losartan potassium dispersed in polymeric matrix (starch/gelatin) as innovative pharmaceutical forms intended to be used for blood pressure control. The lecithin/gelatin nanoparticles were prepared by desolvation method. The independent variables were lecithin/gelatin amount and stirring speed while particle size, PDI (polydispersity index), and entrapment efficiency were the dependent variables studied. The optimized nanoparticle formulation was also characterized in terms of ζ potential and morphology. The mold of microneedle manufacture was created using a 3D printer by molding, and the microneedle arrays were prepared by micromolding method. The independent variables were starch/gelatin amount and drug form while fracture force, bioadhesion, and post-wetting bioadhesion were the dependent variables evaluated. The optimized microneedle array formulations were also characterized and evaluated in terms of morphology, release profiles, and in vitro losartan skin permeation studies. The optimized nanoparticle formulation was of 170.3 ± 3.1 nm of size, with 0.201 ± 0.013 of PDI, 40.45 ± 2.27% of entrapment efficiency, and − 32.9 ± 0.8 mV of ζ potential. The mold had an array of 25 microneedles with a height of 1.5 mm each. The optimized microneedle arrays were successful in terms of fracture force with a value of 408.3 ± 6.1 gf for MP and 320.2 ± 17.4 gf for MN. The results of in vitro skin permeation studies indicated that therapeutic losartan concentrations can be reached by using a microneedle array of 49 cm2 for MP and 13 cm2 for MN. The optimal formulation of the microneedle array with nanoparticles constitutes the most suitable option for skin losartan delivery.
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