• Korean Journal of Dental Materials
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• v.44 no.1
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• pp.33-41
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• 2017

In this study, we prepared PLA-tetracycline complexes coated gold nanoparticle-titania nanotubes and estimated their infrared LASER mediated drug release in the abdominal region of ICR mouse. The results of UV-Vis spectrophotometer showed the highest absorbance at the wavelength of 530 nm and 809 nm indicating the existence of gold nanoparticles. EDX analysis showed that the amounts of gold nanoparticle coated on titania nanotubes were approximately 3.62-36.5 wt%. In vivo test resulted that the tetracycline release value of experimental groups (6.5 ng/mL) was higher than that of control group (5.8 ng/mL) on the condition of 30 minutes of LASER irradiation. Therefore, it is expected that PLA-tetracycline complexes coated gold nanoparticle-titania nanotubes have the feasibility in the field of infrared remote controlled drug device and overcome the limitation of location and time of drug release in dental implant.

• Journal of Ginseng Research
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• v.47 no.5
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• pp.638-644
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• 2023

Background: The anti-platelet activity of the saponin fraction of Korean Red Ginseng has been widely studied. The saponin fraction consists of the panaxadiol fraction (PDF) and panaxatriol fraction (PTF); however, their anti-platelet activity is yet to be compared. Our study aimed to investigate the potency of anti-platelet activity of PDF and PTF and to elucidate how well they retain their anti-platelet activity via different administration routes. Methods: For ex vivo studies, Sprague-Dawley rats were orally administered 250 mg/kg PDF and PTF for 7 consecutive days before blood collection via cardiac puncture. Platelet aggregation was conducted after isolation of the washed platelets. For in vitro studies, washed platelets were obtained from Sprague-Dawley rats. Collagen and adenosine diphosphate (ADP) were used to induce platelet aggregation. Collagen was used as an agonist for assaying adenosine triphosphate release, thromboxane B2, serotonin, cyclic adenosine monophosphate, and cyclic guanosine monophosphate (cGMP) release. Results: When treated ex vivo, PDF not only inhibited ADP and collagen-induced platelet aggregation, but also upregulated cGMP levels and reduced platelet adhesion to fibronectin. Furthermore, it also inhibited Akt phosphorylation induced by collagen treatment. Panaxadiol fraction did not exert any antiplatelet activity in vitro, whereas PTF exhibited potent anti-platelet activity, inhibiting ADP, collagen, and thrombin-induced platelet aggregation, but significantly elevated levels of cGMP. Conclusion: Our study showed that in vitro and ex vivo PDF and PTF treatments exhibited different potency levels, indicating possible metabolic conversions of ginsenosides, which altered the content of ginsenosides capable of preventing platelet aggregation.

• Journal of Pharmaceutical Investigation
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• v.30 no.1
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• pp.27-32
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• 2000

Various release test methods have been applied for the evaluation of nicotine release in vitro from commercial patches. However, whether and how the release data reflect the permeation of nicotine across the skin, is not fully elucidated. To predict in vivo bioavailability from in vitro release tests, correlation between in vitro release and in vitro skin permeation was assessed in the present study. Release of nicotine from three commercial patches was measured for 24 hours under nine experimental conditions which were classified depending on the apparatus (i.e., paddle over disk, cylinder and reciprocating holder) and dissolution media (i.e., phosphate buffer pH 7.4, water and the 1 % phosphoric acid pH 1.5). In vitro permeation of nicotine from the patches across the human cadaver skin was also measured using a diffusion cell. The release of nicotine was better explained by the Higuchi's equation rather than by the first order rate equation. Correlation between the release rate and the in vitro skin permeation differed among the patches. However, in general, the cylinder method, in which water is used as a dissolution medium, showed the highest correlation among the nine release test conditions.

• Journal of Ginseng Research
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• v.19 no.2
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• pp.108-113
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• 1995

Effect of ginseng polysaccharide fraction was examined for $CCl_4$-induced hepatotoxicity in vitro and in vivo. In $CCl_4$-injured primary cultured rat hepatocytes, treatment of the polysaccharide fraction (0.1, 0.3, 1.0 mg/ml) significantly Inhibited the release of LDH and GOT into the culture medium in a dose-dependent manner. Oral administration of the polysaccharide fraction (100, 200 mg/kg) inhibited the decrease of body weight and the increase of the ratio of liver to body weight in $CCl_4$-intoxicated rats. Elevation of GOT, GPT and ALP activity in the serum by $CCl_4$-induced hepatotoxicity was suppressed by administration of ginseng polysaccharide fraction. MDA levels increased in the serum as well as in the liver tissue by treatment with $CCl_4$ showed a tendency to be 연w in the rats given to the polysaccharide fraction. These results suggest that the polysaccharide fraction may be active substance responsible for antihepatotoxic effect of Panax ginseng.

• Archives of Pharmacal Research
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• v.13 no.2
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• pp.151-160
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• 1990

In order to develop a controlled-release oral drug delivery system (DDS) which sustains the plasma acetaminophen (AAP) concentration for a certain period of time, microporous membrane-coated tablets were prepared and evaluated in vitro. Firstly, highly water-soluble core tablet of AAP were prepared with various formulations by wet granulation and compression technique. Then the core tablets were coated with polyvinychloride (PVC) in which micronized sucrose particles were dispersed. Effect of formula compositions of core tablets and coating suspensions on the pharmaceutical characteristics such as drug release kinetics and membrane stability of the coated tablets was investigated in vitro. AAP was released from the coated tablets as a zero-order rate in a pH-independent manner. This independency of AAP release to pH change from 1.2 to 7.2 is favorable for the controlled oral drug delivery, since it will produce a constant drug release in the stomach and intestine regardless of the pH change in the GI tract. Drug release could be extended upto 10 h according to the coating condition. The release rate could be controlled by changing the formula compositions of the core tablets and coating suspensions, coat weight per each tablet, and especially PVC/sucrose ratio and particle size of the sucrose in the coating suspension. The coated tablets prepared in this study had a fairly good pharmaceutical characteristics in vitro, however, overall evaluation of the coated tablet should await in vivo absorption study in man.

• Natural Product Sciences
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• v.7 no.4
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• pp.95-101
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• 2001

We investigated the effect of aqueous extract of Terminalia chebula (Combretaceae)(TCAE) on the immediate hypersensitivity reaction in vivo and in vivo. TCAE (0.01 to 1 g/kg) dose-dependently inhibited compound 48/80 induced systemic anaphylaxis in mice. When TCAE was pretreated at concentrations ranging from 0.01 to 1 g/kg, the plasma histamine levels were reduced in a dose-dependent manner. TCAE (0.1 and 1 g/kg) significantly inhibited local immunoglobulin E (IgE)-mediated passive cutaneous anaphylactic reaction. TCAE (0.001 to 1 mg/ml) also dose-dependently inhibited the histamine release from rat peritoneal mast cells (RPMC) activated by compound 48/80 or anti-dinitrophenyl (DNP) IgE. TCAE (0.01 to 1 mg/ml) had a significant inhibitory effect on anti-DNP IgE-induced tumor necrosis $factor-{\alpha}$ production from RPMC. These results indicate that TCAE inhibits immediate hypersensitivity reaction in vivo and in vitro.

• Biomolecules & Therapeutics
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• v.22 no.2
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• pp.161-165
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• 2014

The main purpose of this study was to develop a novel, in situ gel system for sustained delivery of ranitidine hydrochloride. Ranitidine in situ gels at 0.2%, 0.5%, and 1.0% gellan gum concentration (w/v) were prepared, respectively, and characterized in terms of preparation, viscosity and in vitro release. The viscosity of the gellan gum formulations in solution increased with increasing concentrations of gellan gum. In vitro study showed that the release of ranitidine from these gels was characterized by an initial phase of high release (burst effect) and translated to the second phase of moderate release. Single photon emission computing tomography technique was used to evaluate the stomach residence time of gel containing $^{99m}Tc$ tracer. The animal experiment suggested in situ gel had feasibility of forming gels in stomach and sustained the ranitidine release from the gels over the period of at least 8 h. In conclusion, the in situ gel system is a promising approach for the oral delivery of ranitidine for the therapeutic effects improvement.

• Archives of Pharmacal Research
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• v.29 no.7
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• pp.598-604
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• 2006

In many conventional drug delivery systems in vogue, failure to deliver efficient drug delivery at the target site/organs; is evident as a result, less efficacious pharmacological response is elicited. Microspheres can be derived a remedial measure which can improve site-specific drug delivery to a considerable extent. As an application, Lung-targeting Ofloxacin-loaded gelatin microspheres (GLOME) were prepared by water in oil emulsion method. The Central Composite Design (CCD) was used to optimize the process of preparation, the appearance and size distribution were examined by scanning electron microscopy, the aspects such as in vitro release characteristics, stability, drug loading, loading efficiency, pharmacokinetics and tissue distribution in albino mice were studied. The experimental results showed that the microspheres in the range of $0.32-22\;{\mu}m$. The drug loading and loading efficiency were 61.05 and 91.55% respectively. The in vitro release profile of the microspheres matched the korsmeyer’s peppas release pattern, and release at 1h was 42%, while for the original drug, ofloxacin under the same conditions 90.02% released in the first half an hour. After i.v. administration (15 min), the drug concentration of microspheres group in lung in albino mice was $1048\;{\mu}g/g$, while that of controlled group was $6.77\;{\mu}g/g$. GLOME found to release the drug to a maximum extent in the target tissue, lungs.

• The Korean Journal of Physiology and Pharmacology
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• v.5 no.3
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• pp.223-230
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• 2001

Melatonin, a pineal gland hormone, is believed to act as an antioxidant via the stimulation of radical detoxifying enzymes and scavenging of free radicals. In this study, effects of in vitro and in vivo treatments of melatonin on the cisplatin-induced lipid peroxidation, LDH release and plasma creatinine were determined in rabbit renal cortical cells. The level of malondialdehyde (MDA) was assayed as an index of lipid peroxidation and the level of LDH release as an indicator of cellular damage. In in vitro studies, cisplatin increased the levels of MDA and LDH release in a concentration-and time-dependent manner. Melatonin inhibited the cisplatin-induced lipid peroxidation and LDH release in a concentration-dependent manner. The minimal effective concentration of melatonin that significantly reduced the $300\;{\mu}M$ cisplatin-induced lipid peroxidation and LDH release was 1 mM. In in vivo studies, the levels of lipid peroxidation and LDH release in renal cortical cells increased significantly 24 or 48 hours after a single injection of cisplatin (6 mg/kg). When the cisplatin-injected rabbits were pretreated with 10 mg/kg of melatonin, a significant reduction in both lipid peroxidation and LDH release was observed. The plasma creatinine level increased from $0.87{\pm}0.07$ mg/dl in control to $6.33{\pm}0.54$ mg/dl in cisplatin-injected rabbits (P＜0.05). Melatonin partially prevented the increase in serum creatinine level $(1.98{\pm}0.11\;mg/dl)$ by cisplatin (P＜0.05). In the proximal tubules from cisplatin-treated group, tubular cells had microvilli of variable heights. Necrotic debris was seen in tubular lumens. In most of cells, the mitochondria and lysosomes were increased in frequency. The endocytic vacuoles were not prominent and distribution of the brush border was irregular and shortened. These cisplatin-induced morphological changes were moderate in the melatonin-pretreated group. These results suggest that the toxicity of cisplatin is associated with the generation of reactive oxygen free radicals and that melatonin is a powerful antioxidant, which prevents some of the adverse effects of cisplatin.

• Archives of Pharmacal Research
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• v.9 no.2
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• pp.87-91
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• 1986

In attempt to develop a drug delivery system using serum albumin microspheres, bovine serum albumin microspheres containing antitumar agent. Cytarabine, were prepared. The shape, surface characteristics, size distribution, behavior of in vivo distribution, drug release behavior, and degradation of albumin microsphers in animal liver issue homogenate and proteolytic enzyme were investigated. The shape of albumin microspheres was spherical and the surface was smooth and compact. The size distribution of the albumin microspheres was effected by dispertion forces during emulsification and albumin concentration. Distribution of albumin microspheres after imtravenous administration in rabbit was achieved immediately. In vitro, albumin microsphere matrix was so hard that it retained most of cytarabine except initial burst during the first 10 minutes, and the level of drug release during the initial burst was affected by heating temperature, drug/albumin microsphere matrix was so hard that it retained most of cytarabine except initial burst during the first 10 minutes, and the level of drug release during the initial burst was affected by heating temperature, drug/albumin concentration ratio and size distribution. After drug release test, the morphology of albumin microspheres was not changed. Albumin microsphere matrix was degraded by the animal liver issue homogenate and proteolytic enzyme. The degree of degradation was affected by heating temperature.