01762nas a2200277   4500000000100000008004100001653002300042653001600065653002000081653002700101653001200128653002900140100001300169700001200182700001400194700001600208700001400224700001500238700001500253700001100268245013000279300001400409490000700423520104000430022001401470       2017                            d10aBox-Behnken design10aCaco-2 cell10aEudragit® L10010ain vitro release assay10aleprosy10aPlackett–Burman design1 aChaves L1 aLima SC1 aVieira AC1 aBarreiros L1 aSegundo M1 aFerreira D1 aSarmento B1 aReis S00apH-sensitive nanoparticles for improved oral delivery of dapsone: risk assessment, design, optimization and characterization.  a1975-19900 v123 a<p><strong>AIM: </strong>To optimize the production of pH-sensitive dapsone (DAP) nanoparticles based on Eugradit L100 (NPs-EL100-DAP) for oral delivery.</p>

<p><strong>MATERIALS &amp; METHODS: </strong>NPs-EL100-DAP were optimized using a Plackett-Burman design and a Box-Behnken design. The physicochemical properties of the obtained nanoparticles were monitored by microscopy, dynamic light scattering, Fourier transform infrared spectroscopy, differential scanning calorimetry, in vitro release assays, and examined for cytotoxicity and permeation across intestinal barrier.</p>

<p><strong>RESULTS: </strong>The in vitro release assay of NPs-EL100-DAP confirmed the nanoparticles' pH sensitivity and the ability to deliver DAP at intestinal environment. NPs-EL100-DAP demonstrated enhanced intestinal interactions in comparison to free DAP, across Caco-2 monolayers.</p>

<p><strong>CONCLUSION: </strong>These studies demonstrate the potential of NPs-EL100-DAP as a therapeutic platform for oral treatment of leprosy.</p>
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