Porous microneedle arrays as promising tools for the quantification of drugs in the skin: a proof of concept study.

This study aimed to demonstrate the potential of using porous microneedles (PMNs) as a promising tool for the noninvasive quantification of topically applied pharmaceutical products. We fabricated a porous microneedle (PMN) from a blend of cellulose acetate and dimethyl sulfoxide by casting and phase separation; it was characterized using scanning electron microscopy, Raman spectroscopy, differential scanning calorimetry, and a Texture Analyzer. An ex vivo study was conducted as a proof-of-concept study to assess whether this PMN could be used to quantify drug absorption through the skin after the topical administration of two nonequivalent products of sodium ibuprofen (gel and dissolving microneedles). Three cellulose acetate formulations (PMN1: 37.5%, PMN-2: 44.4%, and PMN-3: 50%) were used to prepare PMN patches; subsequently, these were evaluated for their morphological and insertion properties. Only PMN-2 microneedle patches were chosen to continue with the ex vivo study. The ex vivo study results demonstrated that PMNs could absorb and release sodium ibuprofen (SDIB) and differentiate between two different SDIB topical products. This can be attributed to the porous and interconnected architecture of these microneedles. This developmental study highlights the potential success of such a tool for the quantification of dermal drug concentration and supports moving to in vivo tests.

Development of polymeric nanoparticle gel prepared with the combination of ionic pre-gelation and polyelectrolyte complexation as a novel drug delivery of timolol maleate.

OBJECTIVE: The purpose of this study was to overcome the undesired systemic absorption of skin topical administration of timolol maleate (TM) by developing the TM nanoparticle gel. METHODS: TM-loaded nanoparticle (TMNP) was prepared by ionic pre-gelation of pectin (PCN) and calcium ions (CI) followed with polyelectrolyte complex using chitosan (CHI). TMNP was characterized by measuring the particle size, polydispersity index, zeta potential, encapsulation efficiency (EE), and the interaction between formula constituents. TM-loaded nanoparticle gel (TMNG) was prepared by using hydroxypropyl methylcellulose (HPMC) and was characterized by measuring the spreadability, pH, viscosity, and drug content. The drug release kinetics were analyzed using DDSolver add-in program. RESULTS: TMNP possessed particle size of 175.2 ± 19.7 nm, polydispersity index of 0.528 ± 0.113, zeta potential of -10.86 ± 0.87 mV, and EE of 27.45 ± 2.34%. The electrostatic interactions between PCN, CI, and CHI that formed the nanoparticles were confirmed by the result of vibrational spectroscopy analysis. TMNG possessed spreadability of 60.80 ± 1.38 cm2, pH of 5.154 ± 0.004, viscosity of 269.07 ± 5.83 cP, and drug content of 107.38 ± 1.77%. TM showed a sustained release manner within 24 h by following Korsmeyer-Peppas kinetical model with non-Fickian release mechanism. CONCLUSION: The prepared nanoparticle gel can be an effective controlled release system of TM that administered topically on the skin surface.