Pallavi D. Vispute; Milind P. Wagh; Nazma N. Inamdar
Abstract
Iontophoresis is a convenient and suitable technique for delivering charged sumatriptan succinate (SS) across the skin. The objective of study was to examine the applicability of ion exchange resins and fibers as drug carrier to enhance the efficiency of transdermal iontophoresis. The complexes of drug ...
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Iontophoresis is a convenient and suitable technique for delivering charged sumatriptan succinate (SS) across the skin. The objective of study was to examine the applicability of ion exchange resins and fibers as drug carrier to enhance the efficiency of transdermal iontophoresis. The complexes of drug with cationic resins Indion 204 and Indion 224 (DRC-1, DRC-2) as well as with fibers Smopex 102 and Smopex 101 (DFC-1, DFC-2) were formed by batch method. These complexes were characterized by DSC and PXRD and compared for drug loading, drug release and permeation across rat skin. Effects of constant and pulsed current iontophoresis on drug permeation were also evaluated. The iontophoresis study was conducted using silver–silver chloride electrodes across rat skin. The results suggested that fibers due to their open structure showed more drug loading and release compared to resins. The transdermal flux as well as amount of drug permeated from drug-fiber complexes was higher as compared to that of drug-resin complexes and drug solution. DFC-2 assisted with pulsed iontophoresis at 50 % duty cycle significantly increased the skin permeation of SS and reduced the fluctuation in drug permeation with constant drug delivery compared with the passive controls.
Yogesh M. Choudhari; Sachin V. Detane; Sushant S. Kulthe; Chandrakant C. Godhani; Nazma N. Inamdar; Seema M. Shirolikar; Lalit C. Borde; Vishnukant K. Mourya
Abstract
Low molecular weight chitosan (LMWC) exhibits higher water solubility and produces nanoparticles of fairly low particle size. However, poor drug loading and shorter circulation time in body limits its application in preparation of nanoparticles. Acylation of LMWC ensures extended circulation of nanoparticles ...
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Low molecular weight chitosan (LMWC) exhibits higher water solubility and produces nanoparticles of fairly low particle size. However, poor drug loading and shorter circulation time in body limits its application in preparation of nanoparticles. Acylation of LMWC ensures extended circulation of nanoparticles in body and hence enhanced bioavailability of the drug. We therefore synthesized the acylated LMWC using palmitoyl chloride and confirmed its synthesis by FTIR and NMR spectroscopy. The nanoparticles of LMWC and low molecular weight palmitoyl chitosan (LMWPC) were prepared by miniemulsion and chemical crosslinking method using glutaraldehyde and 5-fluorouracil (5FU) as a model drug. The nanoparticles were evaluated for particle size, zeta potential, morphology, drug loading and drug release. TEM analysis revealed nanosize and spherical nature of the particles. The palmitoyl chain of LMWPC increased particle size from 83.2±2.5 nm to 93.4±3.2 nm whereas zeta potential of nanoparticles decreased from 12.5±2.2 mV to 4.2±1.1 mV due to diminished amino groups of LMWPC as a result of acylation. The drug loading in nanoparticles was increased from 13.8±0.95% to 30.2±1.9%. LMWC showed 80±2.08% as maximum drug released in 10 h while only 52.3±2.14% was released in 24 h for LMWPC. Hence, LMWPC nanoparticles ensure increased drug loading capacity and sustained drug release profile without significant change in particle size.