• Title/Summary/Keyword: Drug stability

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Nucleic Acid Aptamers: New Methods for Selection, Stabilization, and Application in Biomedical Science

  • Kong, Hoon Young;Byun, Jonghoe
    • Biomolecules & Therapeutics
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    • v.21 no.6
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    • pp.423-434
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    • 2013
  • The adoption of oligonucleotide aptamer is well on the rise, serving an ever increasing demand for versatility in biomedical field. Through the SELEX (Systematic Evolution of Ligands by EXponential enrichment), aptamer that can bind to specific target with high affinity and specificity can be obtained. Aptamers are single-stranded nucleic acid molecules that can fold into complex three-dimensional structures, forming binding pockets and clefts for the specific recognition and tight binding of any given molecular target. Recently, aptamers have attracted much attention because they not only have all of the advantages of antibodies, but also have unique merits such as thermal stability, ease of synthesis, reversibility, and little immunogenicity. The advent of novel technologies is revolutionizing aptamer applications. Aptamers can be easily modified by various chemical reactions to introduce functional groups and/or nucleotide extensions. They can also be conjugated to therapeutic molecules such as drugs, drug containing carriers, toxins, or photosensitizers. Here, we discuss new SELEX strategies and stabilization methods as well as applications in drug delivery and molecular imaging.

The Inhibitory effect of omeprazole-cholestyramine resin in gastric secretion of rat (Omeprazole-cholestyramine resin 제제의 위산분비에 대한 억제효과)

  • 이영욱;김일웅;정지훈;라현오;최경범;이남인;손의동;허인회
    • Biomolecules & Therapeutics
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    • v.8 no.4
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    • pp.318-324
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    • 2000
  • We have examined inhibitory erects on gasritis using omeprazole-cholestyramine resinate, which has been developed to increase the stability of omeprazole, the well-known proton pump inhibitor, in an acidic condition. To test the pharmacological action of this, we investigated the effect of omeprazole-cholestyramine resinate on indomethacin-induced gastritis in rats. Omeprazole was used as a reference drug. Orally administered omeprazole-cholestyramine resinate inhibited the indomethacin-induced gastritis in a dose-dependent manner. The inhibitory effect of omeprazole-cholestyramine resinate on the gastritis was similar to that of reference drug. In addition, rectal adminstration of the omeprazole-cholestyramine resinate inhibited the indomethacin-induced gastritis in a dose-dependent manner. The inhibitory effect of omeprazole-cholestyramine resinate was equipotent to reference drug. The basal gastric acid secretion was decreased when it was administered either orally or rectally. This inhibition of omfprazole-cholestyramine resinate was similar to that of omeprazole. These data suggest that omeprazole-cholestyramine resinate inhibit the gastritis in rats, and are comparable to omeprazole available in market.

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Biocompatible Nanoparticles with Well-defined Surface Chemistry for Smart Drug Delivery

  • Min, Dal-Hee
    • Proceedings of the Korean Vacuum Society Conference
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    • 2013.02a
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    • pp.107-107
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    • 2013
  • Many nanomaterials are being harnessed as critical components in various systems for biomedical applications including diagnosis, imaging, and drug delivery. Those systems necessitate biocompatibility and low toxcity within effective dose range while achieving enough efficacy. Even though many nanomaterials enjoy successful demonstrations in bioapplications, lack of biocompatibility and high cytotoxicity often become hurdles for practical bioapplications. On the other hand, it is important to achieve enough efficiency based on chemically well-defined systems with efforts to understand mechanism at molecular level. Here, we developvarious biocompatible nanomaterials based on simple procedure using dextran as both reducing agent and surface coating. Dextran is one of the popular biocompatible polymers that have been used for drug delivery and biosensors. Dextran coated nanomaterials showed excellent colloidal stability, flexible surface chemistry for conjugation of bioactive molecules and low cytotoxicity with successful demonstrations in various bioapplications.

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Antiapoptotic Fusion Protein Delivery Systems

  • Tan, Cheau Yih;Kim, Yong-Hee
    • Macromolecular Research
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    • v.16 no.6
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    • pp.481-488
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    • 2008
  • Apoptosis is a natural cell suicide mechanism to maintain homeostasis. However, many of the diseases encountered today are caused by aberrant apoptosis where excessive apoptosis leads to neurodegenerative disorders, ischemic heart disease, autoimmune disorders, infectious diseases, etc. A variety of antiapoptotic agents have been reported to interfere with the apoptosis pathway. These agents can be potential drug candidates for the treatment or prevention of diseases caused by dysregulated apoptosis. Obviously, world-wide pharmaceutical and biotechnology companies are gearing up to develop antiapoptotic drugs with some products being commercially available. Polymeric drug delivery systems are essential to their success. Recent R&D efforts have focused on the chemical or bioconjugation of antiapoptotic proteins with the protein transduction domain (PTD) for higher cellular uptake with antibodies for specific targeting as well as with polymers to enhance the protein stability and prolonged effect with success observed both in vivo and in vitro. All these different fusion antiapoptotic proteins provide promising results for the treatment of dysregulated apoptosis diseases.

Treatment of an Atrophic Scar with Fractional Carbon Dioxide Laser-assisted Poly-L-lactic Acid Delivery

  • Kim, Wan Jin;Jung, Ha Rin;Lee, Sang Ju;Cho, Han Kyoung
    • Medical Lasers
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    • v.10 no.3
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    • pp.181-184
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    • 2021
  • Scars can cause great psychological stress among patients. Currently, there are numerous topical agents, laser and surgical treatments available for skin rejuvenation and scar minimization. Laser-assisted drug delivery (LADD) is a treatment method that increases drug delivery by stimulating the skin physically and chemically to enhance the penetration of topical agents. This is one of the areas of great interest in the treatment of various skin diseases in addition to its use for cosmetic purposes. In particular, LADD is relatively non-invasive and has advantages in terms of accessibility and stability. Poly-L-lactic acid (PLLA) is a collagen stimulator known to gradually restore skin volume by inducing inflammation and fibroplasia. Herein, we report a case of treatment of an atrophic scar with fractional carbon dioxide laser-assisted PLLA delivery.

Identification of inhibitors against ROS1 targeting NSCLC by In- Silico approach

  • Bavya, Chandrasekhar
    • Journal of Integrative Natural Science
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    • v.15 no.4
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    • pp.171-177
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    • 2022
  • ROS1 (c-ros oncogene) is one of the gene with mutation in NSCLC (non-small cell lung cancer). The increased expression of ROS1 is leading to the increase proliferation of cell, cell migration and survival. Crizotinib and Entrectinib are the drugs that have been approved by FDA against ROS1 protein, but recently patients started to develop resistance against Crizotinib and there is a need of new drug that could act as an effective drug against ROS1 for NSCLC. In this study, we have performed virtual screening, where compounds are taken from Zinc 15 dataset and molecular docking was performed. The top compounds were taken based upon their binding affinity and their interactions with the residues. The compounds stability and chemical reactivity was also studied through Density Functional theory and their properties. Further study of these compounds could reveal the required information of ROS1-inhibitor complex and in the discovery of potent inhibitors.

Detection of phenobarbital adulteration in dietary supplements: simultaneous analysis of 16 sedative-hypnotics and sleep-inducers by ultra-high-performance liquid chromatography with UV detection (UPLC-UV) and quadruple Orbitrap mass spectrometry (Q-Orbitrap-MS)

  • Lee, Ji Hyun;Choi, Ji Yeon;Park, Hanna;Min, Ah Young;Kim, Nam Sook;Park, Seong Soo;Park, Sung-Kwan;Kang, Ho-il
    • Analytical Science and Technology
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    • v.32 no.1
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    • pp.24-34
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    • 2019
  • The safety of food is occasionally questionable, as there have been some reports of products contaminated with illegal adulterants. In this study, the presence of 16 sedative-hypnotics and sleep inducers in dietary supplements was determined by ultra-high-performance liquid chromatography with UV detection (UPLC-UV) and quadruple Orbitrap mass spectrometry (Q-Orbitrap-MS). The UPLC method was validated, providing a linearity (R2) of more than 0.999, and LODs and LOQs that ranged from 0.2 to 0.5 and 0.6 to $1.5{\mu}g\;mL^{-1}$, respectively. The repeatabilities were 0.2-8.4 % (intra-day) and 0.3-4.5 % (inter-day), and the accuracies were 89.0-117.0 % (intra-day) and 87.8-111.9 % (inter-day). The mean recoveries of the spiked samples ranged from 98.7 to 107.3 %. The relative standard deviation (%RSD) of the stability was less than 2.4 %. Using the developed method, one sedative-hypnotic compound, phenobarbital, was detected in one of the nineteen samples tested. In addition, the major characteristic fragment ions of each target compound were confirmed using Q-Orbitrap-MS for higher accuracy. Monitoring the presence of these 16 sedative-hypnotics and sleep inducers in dietary supplements should be pursued in the interest of human health, and the results of this study confirmed that the developed method has value for this application.

Stability of 0ndansetron and Fluconazole in 5% Dextrose Injection and Normal Saline during Y-Site Administration

  • Burm, Jin-Pil
    • Archives of Pharmacal Research
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    • v.20 no.2
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    • pp.171-175
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    • 1997
  • The stability of ondansetron and fluconazole in 5% dextrose injection and normal saline during simulated Y-site injection at room temperature was studied. Ondansetron 0.03, 0.1 and 0.3 mg/ml were admixed 1:1 with fluconazole 2 mg/ml. The solutions were stored at room temperature and samples were retrieved at time 0, 1, 2, 4 and 12 hr for immediate assay. At the time of the assay and before any dilution, each sample was visually inspected for clarity, color, precipitation, and the pH was determined. Drug concentrations were measured by a stability-indicating high performance liquid chromatograph. Ondansetron 0.03, 0.1 and 0.3 mg/ml were stable when mixed with concentration of fluconazole 2 mg/ml. There were no change in clarity and color and no precipitates in any admixture for 12 hr of inspection. The pH measurements did not have a particular trend in any direction over time.

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Phamaceutical Studies on the Drug (III) -Enhancement of Dissolution and Stability of Sulfamethoxazole by ${\beta}-Cyclodextrin$ Complexation- (약물의 약제학적 연구(제 3보) -${\beta}-$시클로덱스트린과의 복합체 형성에 의한 설파메톡사졸의 용출 및 안정성 향상-)

  • Lee, Hyeon-Jong;Kim, Soo-Uck;Seo, Seong-Hoon
    • Journal of Pharmaceutical Investigation
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    • v.18 no.4
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    • pp.181-186
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    • 1988
  • Inclusion complex of sulfamethoxazole with ${\beta}-cyclodextrin$ was prepared by freeze-drying method in molar ratios of 1:1, 1:1.25, 1:1.5 and 1:1.75, and the complex formation was identified by ultraviolet and infrared spectroscopies, powder X-ray diffractometry and differential scanning calorimetry. Dissolution rate and solid state stability of the complex were investigated in comparison with those of sulfamethoxazole powder and the physical mixture of sulfamethoxazole with ${\beta}-cyclodextrin$. As a result, the dissolution rate and the stability of solid complexes in various relative humidity conditions increased more remarkably than those of sulfamethoxazole powder and physical mixture. But the difference according to molar ratio of the complex was not recognized.

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Development of trans-cinnamaldehyde self-microemulsifying drug delivery system(SMEDDS) with superior stability (안정성이 우수한 신남알데히드 자가미세유화 약물전달시스템 개발)

  • Bang, Kyu-Ho;Kim, Kyeong Soo
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.20 no.12
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    • pp.555-562
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    • 2019
  • This study was undertaken to develop a stable self-microemulsifying drug delivery system (SMEDDS) for trans-cinnamaldehyde, a known antibacterial and antifungal agent. A simultaneous analytical method was established for quantification of trans-cinnamaldehyde and its degradant, cinnamic acid. Various surfactants were applied to assess their effect on the aqueous solubility of trans-cinnamaldehyde, and pseudo-ternary phase diagrams were plotted. Of the various formulations tested, the liquid SMEDDS composed of trans-cinnamaldehyde (oil), Cremophor EL (surfactant) and Transcutol P (cosurfactant) at a volume ratio of 10/70/20, produced the smallest emulsion droplet size (around 23 nm). The stability test determined the superior stability of the trans-cinnamaldehyde SMEDDS with constant trans-cinnamaldehyde content and z-average diameter of emulsion, under accelerated and heat stressed condition. Thus, we believe that this novel trans-cinnamaldehyde SMEDDS formulation has the potential to be applied for the development of trans-cinnamaldehyde medicines in the pharmaceutical industry.