• Journal of Pharmaceutical Investigation
• /
• v.35 no.6
• /
• pp.417-422
• /
• 2005

This study was aimed to design and formulate the moisture-activated patches containing ofloxacin and lidocaine for antibacterial and local anesthetic action. The solubility of lidocaine at $32^{\circ}C$ in various vehicles decreased in the rank order of PG $759.5{\pm}44.5\;mg/mL$ > PGL > IPM > PEG 300 > PEG 400 > Ethanol > PGMC > DGME > PGML > OA > $Captex^{\circledR}\;300$ > $Captex^{\circledR}\;200$ > water $(4.0{\pm}0.1\;mg/mL)$. Ofloxacin revealed very low solubility, which the highest solubility was obtained from PEG 400 $(18.7{\pm}6.3\;mg/mL)$ among the vehicles used. The addition of lactic acid increased the solubility of ofloxacin dramatically; the solubility at 5% lactic acid was $133.7{\pm}9.7\;mg/mL$. As $2-hydroxypropyl-{\beta}-cyclodextrin$ was added at the concentrations of 40, 80, 120, 160 and 200 mM, the solubilities of lidocaine and ofloxacin were enhanced up to three and two times, respectively, with concentration-dependent pattern. Gel intermediates for filmtype patches were prepared with mucoadhesive polymer, viscosity builders, lidocaine or ofloxacin at pH values from 5 to 7. Gels were cast onto a release liner and dried at room temperature. Dried patch was attached onto an adhesive backing layer, thus forming a patch system. Patches containing a single drug component were characterized by in vitro measurement of drug release rates through a cellulose barrier membrane. The release study was carried out at $37^{\circ}C$ using a Franz-type cell. Receptor solutions were isotonic phosphate buffers (pH 7.4). Samples $(100\;{\mu}L)$ were taken over 24 hours and quantitated by a verified HPLC method. The releases from all tested were proportional to the square root of time. The release rates were 0.9, 157.3 and $281.7\;{\mu}g/cm^{2}/min^{1/2}$ for the lidocaine patches and 19.8,37.2 and $50.7\;{\mu}g/cm^{2}/min^{1/2}$ for the ofloxacin patches at the concentrations of 0.3, 0.5 and 1 %, respectively. The release rates were dose dependent in both drug patches $(R^{2}\;=\;0.9077\;for\;lidocaine;\;R^{2}\;=\;0.9949\;for\;ofloxacin)$ and those were also thickness-dependent $(R^{2}\;=\;0.9246\;for\;lidocaine;\;R^{2}\;=\;0.9512\;for\;ofloxacin)$.

• Polymer(Korea)
• /
• v.37 no.1
• /
• pp.28-33
• /
• 2013

Zaltoprofen, a propionic acid derivative non-steroidal anti-inflammatory drug, was known to have powerful inhibitory effects on acute, subacute and chronic inflammation. For initial release and sustained release, the microspheres were prepared using an emulsion-solvent evaporation method like an O/W emulsion method with varying the ratio of zaltoprofen-loaded polyoxalate (POX)/PLGA micropheres. The morphology of the microspheres was confirmed by scanning electron microscopy. The crystallinity of microspheres was analyzed by X-ray diffraction and differential scanning calorimeter. Fourier transform infrared spectroscopy was used to analyze the chemical structure of microspheres. The increased ratio of POX microspheres affected the initial drug release, and the sustained release of drug was influenced by ratio of PLGA microspheres. In this study, the initial release behavior of zaltoprofen can be controlled by the ratio of POX/PLGA microspheres.

• Applied Chemistry for Engineering
• /
• v.35 no.3
• /
• pp.192-199
• /
• 2024

In this study, carbamazepine (CBZ) imprinted starch/PVA-based biomaterials were prepared by the casting method and UV irradiation, and their physicochemical properties, CBZ adsorption ability, and release properties were investigated. The surface properties of the prepared biomaterials were characterized using FE-SEM, while the stability of CBZ under UV irradiation and the functional groups of the biomaterials were characterized using FT-IR analysis. The adsorption properties of CBZ on the biomaterials were evaluated by binding isotherm and Scatchard plot. Results indicate that CBZ imprinted biomaterials possess a specific binding site of CBZ. To evaluate the applicability of the transdermal drug delivery system, the release properties of CBZ from prepared biomaterials using various pH buffers and artificial skin at 36.5 ℃ were investigated. Results indicated that the CBZ release at high pH was faster than at low pH. In addition, CBZ was released continuously for 12 h in the artificial skin test. The drug release mechanism of CBZ followed a pseudo-Fickian diffusion mechanism in buffer solution, whereas the release from artificial skin exhibited a non-Fickian diffusion mechanism.

• Bulletin of the Korean Chemical Society
• /
• v.32 no.5
• /
• pp.1587-1592
• /
• 2011

The aim of the present study was to improve the solubility and bioavailability of a poorly water-soluble drug in human body, using a solid dispersion technique (hot melt extrusion). The solid dispersion was prepared by cooling the hot melt of the drug in the carrier (Vitamin E TPGS and PVP). The dissolution rate of formulation 1 from a novel formulation prepared by solid dispersion technique was equal to release of formulation 6 (40% of eprosartan mesylate is in contrast to teveten$^{(R)}$) within 60 min (Table 1). The oral bioavailability of new eprosartan mesylate tablet having vitamin E TPGS and PVP K29 was tested on rats and dogs. Of the absorption enhancer and polymer tested, vitamin E TPGS and PVP K29, resulted in the greatest increases of AUC in animals (about 2.5-fold increase in rat and dog). When eprosartan mesylate was mixed with the absorption enhancer and polymer in a ratio of 2.94:2:1, vitamin E TPGS and PVP K29 improved eprosartan mesylate bioavailability significantly compared with the conventional immediate release (IR) tablet Teveten$^{(R)}$ (formulation 7). These results show that solid dispersion using vitamin E TPGS and PVP K29 is a promising approach for developing eprosartan mesylate drug products.

• Biomedical Science Letters
• /
• v.17 no.3
• /
• pp.211-216
• /
• 2011

The chitosan-coated liposomes (chitosomes) were designed to improve the stability in the gastrointestinal (GI) tract and to enhance the efficacy for oral drug delivery of liposomes. The phosphatic acid (PA)-incorporated anionic liposomes were surface-coated with water soluble chitosan (WSC) by electro-ionic interaction. The shape of the chitosomes observed by transmission electron microscopy (TEM) was spherical in all the formulations and the coating layer by WSC could be founded through TEM images. The mean size and the zeta potential values of the chitosomes increased significantly with depending on the content of WSC added for coating the liposomes. The stability of the chitosomes in the GI tract was confirmed through the change of relative turbidity of the liposomal suspension. The plain liposomes (plasomes) suspension without adding WSC clearly showed the change of relatively turbidity in simulated gastric fluid (SGF), while the change degree of turbidity of the chitosomes in the SGF decreased as increasing of WSC content added for coating liposome. In the 5-CF release study from the plasomes and chitosomes, the plasomes released >90% of the initial 5-CF content at 4 h of release measurement. In contrast, the chitosomes released below 40% of initial content of 5-CF. In conclusion, these results indicate that the chitosomes can be used as a potential carrier for effective oral drug delivery.

• Korean Journal of Biological Psychiatry
• /
• v.16 no.4
• /
• pp.266-270
• /
• 2009

Adverse drug reactions are very common in clinical practice, and skin is one of the most frequent organs for adverse drug reactions. We report a case of a 71-year-old male patient who developed skin eruptions after switching formulation of quetiapine immediate release(IR) to quetiapine extended release(XR). He had been taking quetiapine IR(400mg/day) for treatment of manic episode which was developed one year ago. The patient showed great improvement of symptoms after taking quetiapine IR for about one year, thus dosage of medication was reduced to 50mg/day on the average. Unfortunately dose reduction has tended to worsen symptoms, so dose of quetiapine was increased again to 200mg/day with formulation changes to XR. Two days after he took new formulation, erythematous papules were occurred over his anterior neck and ventral side of left wrist. As he stopped quetiapine XR, the skin lesions gradually subsided. And he was successfully treated with readministration of quetiapine IR without any skin lesions.

• Bulletin of the Korean Chemical Society
• /
• v.31 no.9
• /
• pp.2542-2546
• /
• 2010

The objective of this paper was to investigate the effect of dextran gel on preparation of nano-liposomes loaded with ginkgolide. During preparation, Sephadex G75, G50 and G25 were added in the aqueous phase respectively. From the experiment, nano-liposomes prepared by dextran gels were found spherical and smooth. The result indicated that aperture of dextran gels were narrower, particle size of nano-liposomes was smaller (207.13 ~ 89.16 nm) and zeta potential was greater (-36.2 ~ -29.5 mV) in more negative. The study also revealed that differences of the entrapment efficiency and drug loading among the three types of nano-liposomes were not significant. In vitro drug release test demonstrated that nano-liposomes had a better controlled release. To conclude, by using dextran gel in the preparation of nano-liposome loaded with ginkgolide, the particle size could be effectively controlled and the drug stability could be improved.

• Macromolecular Research
• /
• v.15 no.7
• /
• pp.623-632
• /
• 2007

Thermosensitive nanoparticles were prepared via the self-assembly of two different $poly({\varepsilon}-caprolactone)$-based block copolymers of poly(N-isopropylacrylamide)-b-$poly({\varepsilon}-caprolactone)$ (PNPCL) and poly(ethylene glycol)-b-$poly({\varepsilon}-caprolactone)$ (PEGCL). The self-aggregation and thermosensitive behaviors of the mixed nanoparticles were investigated using $^1H-NMR$, turbidimetry, differential scanning microcalorimetry (micro-DSC), dynamic light scattering (DLS), and fluorescence spectroscopy. The copolymer mixtures (mixed nanoparticles, M1-M5, with different PNPCL content) formed nano-sized self-aggregates in an aqueous environment via the intra- and/or intermolecular association of hydrophobic PCL chains. The microscopic investigation of the mixed nanoparticles showed that the critical aggregation concentration (cac), the partition equilibrium constants $(K_v)$ of pyrene, and the aggregation number of PCL chains per one hydrophobic microdomain varied in accordance with the compositions of the mixed nanoparticles. Furthermore, the PNPCL harboring mixed nanoparticles evidenced phase transition behavior, originated by coil to the globule transition of PNiPAAm block upon heating, thereby resulting in the turbidity change, endothermic heat exchange, and particle size reduction upon heating. The drug release tests showed that the formation of the thermosensitive hydrogel layer enhanced the sustained drug release patterns by functioning as an additional diffusion barrier.

• Archives of Pharmacal Research
• /
• v.23 no.5
• /
• pp.488-494
• /
• 2000

Cerebellar granule and glial cells prepared from 7 day-old rat pups were used to investigate the effects of sub-acute nicotine exposure on the glutamatergic nervous system. These cells were exposed to nicotine in various concentrations for 2 to 10 days in situ. Nicotine-exposure did not result in any changes in cerebellar granule and glial cell viability at concentrations of up to 500 $\mu\textrm{M}$. In cerebellar granule cells, the basal extracellular levels of glutamate, aspartate and glycine were enhanced in the nicotine-exposed granule cells. In addition, the responses of N-methyl-D-aspartate (NMDA)-induced glutamate release were enhanced at low NMDA concentrations in the nicotine-exposed granule cells. However, this decreased at higher NMDA concentrations. The glutaminase activity was increased after nicotine exposure. In cerebellar glial cells, glutamate uptake in the nicotine-exposed glial cells were either increased at low nicotine exposure levels or decreased at higher levels. The inhibition of glutamate uptake by L-trans-pyrollidine-2,4-dicarboxylic acid (PDC) was lower in glial cells exposed to 50 $\mu\textrm{M}$ nicotine. Glutamine synthetase activity was lower in glial cells exposed to 100 or 500 $\mu\textrm{M}$ of nicotine. These results indicate that the properties of cerebellar granule and glial cells may alter after subacute nicotine exposure. Furthermore, they suggest that nicotine exposure during development may modulate glutamatergic nervous activity.

• Bulletin of the Korean Chemical Society
• /
• v.33 no.12
• /
• pp.4035-4040
• /
• 2012

Presented study describes the synthesis of photo cross-linkable and water soluble hydroxyethyl starch hydroxyethyl methacrylate (HESHEMA) samples with different degree of substitution (DS) by functionalization of hydroxyethyl starch (HES) with hydroxyethyl methacrylate (HEMA) or hydroxyethyl methacrylate carbonylimidazole (HEMACI) in DMSO using two different routes. It was revealed that the reaction time for HESHEMA synthesis can be reduced from 5 days to 24 h by conducting the reaction at $80^{\circ}C$ instead of at room temperature. Solubility of HESHEMA was found to be dependent on DS which in turn was dependent on ratio between HES and HEMA or HEMACI. HESHEMA samples with DS > 0.24 depicted insoluble in water, whereas the samples with DS < 0.05 did not form appreciable gel. HESHEMA samples with appropriate DS were converted into hydrogels by cross-linking polymer chains under UV radiations and resulting HESHEMA hydrogels showed swelling up to 1200%. Application of HESHEMA in controlled drug delivery was investigated by diffusion based encapsulation of Ondansetron, a serotonin 5-$HT_3$ receptor antagonist drug, mainly used for nausea and vomiting treatment.