ABSTRACT
PURPOSE: Design imiquimod-loaded chitosan nanocapsules for transdermal delivery and evaluate the depth of imiquimod transdermal absorption as well as the kinetics of this absorption using Raman Microscopy, an innovative strategy to evaluate transdermal absorption. This nanovehicle included Compritol 888ATO®, a novel excipient for formulating nanosystems whose administration through the skin has not been studied until now. METHODS: Nanocapsules were made by solvent displacement method and their physicochemical properties was measured by DLS and laser-Doppler. For transdermal experiments, newborn pig skin was used. The Raman spectra were obtained using a laser excitation source at 532 nm and a 20/50X oil immersion objective. RESULTS: The designed nanocapsules, presented nanometric size (180 nm), a polydispersity index <0.2 and a zeta potential +17. The controlled release effect of Compritol was observed, with the finding that half of the drug was released at 24 h in comparison with control (p < 0.05). It was verified through Raman microscopy that imiquimod transdermal penetration is dynamic, the nanocapsules take around 50 min to penetrate the stratum corneum and 24 h after transdermal administration, the drug was in the inner layers of the skin. CONCLUSIONS: This study demonstrated the utility of Raman Microscopy to evaluate the drugs transdermal penetration of in the different layers of the skin. Graphical Abstract New imiquimod nanocapsules: evaluation of their skin absorption by Raman Microscopy and effect of the compritol 888ATO® in the imiquimod release profile.
Subject(s)
Chitosan/pharmacokinetics , Drug Delivery Systems/methods , Fatty Acids/pharmacokinetics , Imiquimod/pharmacokinetics , Nanocapsules/administration & dosage , Skin/metabolism , Administration, Cutaneous , Animals , Chitosan/administration & dosage , Chitosan/chemistry , Fatty Acids/administration & dosage , Fatty Acids/chemistry , Imiquimod/administration & dosage , Imiquimod/chemistry , Nanocapsules/chemistry , Nonlinear Optical Microscopy/methods , Skin Absorption , SwineABSTRACT
The yields of H2 and Cl- were determined in the radiolysis of deaerated, aerated, and water mixtures of poly(vinyl chloride) (PVC) powders with gamma-rays and 5 MeV He ions. H2 yields with gamma-rays are low at about 0.25 molecule/100 eV and they double with He ion radiolysis indicating a second order formation process. The production of H2 in the gamma-radiolysis of water-PVC mixtures is much greater than expected from the weight fraction of the components and is due to acidification of the aqueous phase by the evolution of HCl from the polymer. Cl- yields in the gamma-radiolysis of PVC with number average weights of 22,000, 47,000, and 99,000 Daltons are 19.6, 33.8, and 32.5 atoms/100 eV. Cl- continuously evolves from the polymer for days following radiolysis. The extremely large yields suggest that a chain process involving radicals stabilized on the polymeric chain are responsible. Reflectance UV/vis and infrared spectroscopy show subtle changes in the PVC with radiolysis while UV/vis absorption spectra clearly indicate the formation of polyenes with 1 to 11 units. Cl- formation is probably initiated by Cl radical production followed by an electron rearrangement mechanism along the PVC chain to produce more Cl- and polyenes.
ABSTRACT
Modifications to water-zirconia nanoparticle interfaces induced by gamma irradiation have been examined using diffuse reflection infrared Fourier transform (DRIFT), Raman scattering, and electron paramagnetic resonance (EPR) techniques. Spectroscopy with in situ heating was used to probe variations in the dissociatively bound chemisorbed water on the zirconia nanoparticles following evaporation of the physisorbed water. DRIFT spectra show that the bridged Zr-OH-Zr species decreases relative to the terminal Zr-OH species upon irradiation. No variation is observed with Raman scattering, indicating that the zirconia morphology is unchanged. EPR measurements suggest the possible formation of the superoxide ion, presumably by modification of the surface OH groups. Trapped electrons and interstitial H atoms are also observed by EPR.