• 제목/요약/키워드: drug release control

검색결과 153건 처리시간 0.03초

평간개울지혈탕이 독성약물에 의한 간조직 손상에 미치는 영향 (Effect of Pyunggangaeuljihyul-tang (Pinggankaiyuzhixue-tang) on Toxic Agent Induced Liver Cell Damage)

  • 오세광;김원일;김우환
    • 대한한의학회지
    • /
    • 제24권3호
    • /
    • pp.96-107
    • /
    • 2003
  • Objective : This study was undertaken to determine if Pyunggangaeuljihyul-tang (Pinggankaiyuzhixue-tang, PG) has a protective effect against cell injury induced by various toxic agents in rabbit liver, Methods : Cell injury in vitro was estimated by measuring lactate dehydrogenase (LDH), and that in vivo was estimated by measuring alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activity in serum. Lipid peroxidation was examined by measuring malondialdehyde, a product of lipid per oxidation. Results : PG prevented the LDH release by $CCl_4$, mercury, menadione, and tert-butyl hydroperoxide treatment in vitro in liver slices. The extent of protection by 2% PG was similar to that of $10{\mu\textrm{M}}$ N,N'-diphenyl-p-phenylenedianline, a potent antioxidant, in tert-butyl hydroperoxide-induced LDH release. PG also prevented lipid peroxidation and depletion of cellular ATP induced by Hg. Hg causes motphological changes including cell necrosis and its effect was significantly prevented by PG. When rats were treated intraperitoneatly with 0.5 ml/kg of $CCl_4$, serum alanine aminotransferase and aspartate aminotransferase activities were increased compared with the control, which was significantly inhibited by pretreatment of PG. PG also prevented reduction in GSH and lipid peroxidation induced by $CCl_4$ Conclusion : These results suggest that PG exerts aprotective effect against various toxic agents by its antioxidant action in liver tissues. Thus, PG may be used in prevention and treatment of drug-induced liver cell injury. However, the precise mechanisms of PG protection remain to be determined.

  • PDF

Gentamicin/CTMA/Montmorillonite as Slow-Released Antibacterial Agent

  • Fatimah, Is;Hidayat, Habibi;Purwiandono, Gani;Husein, Saddam;Oh, Won-Chun
    • 한국재료학회지
    • /
    • 제31권6호
    • /
    • pp.367-374
    • /
    • 2021
  • This paper presents the characteristics of gentamicin-loaded into cetyl trimethyl ammonium intercalated montmorillonite (GtM/CTMA/Mt) as a hybrid composite for a slow-released antibacterial delivery systems. The work describes the successful immobilization of gentamicin into the interlayers of surfactant-modified montmorillonite. Physicochemical characterization of the material is carried out by means of X-ray diffraction, scanning electron microscopy, transmission electron microscopy, and Fourier transform infrared spectroscopy. The kinetics of the gentamicin release is investigated by in vitro study and analyzed based on UV-Vis spectrometry. In addition, antibacterial study is performed towards Klebsiella pneumoniae Staphylococcus aureus, Escherichia coli, and Streptococcus pyogenes. The results show that the gentamicin loading into CTMA/Mt increases the effectiveness of the antibacterial activity, as shown by the higher inhibition zone for all tested bacteria, compared to gentamicin as a positive control. The kinetics study suggests that the gentamicin release obeys the modified Korsmeyer-Peppas model. The physicochemical study and activity test demonstrate the feasibility of the GtM/CTMA/Mt for practical applications.

The role of necroptosis in the treatment of diseases

  • Cho, Young Sik
    • BMB Reports
    • /
    • 제51권5호
    • /
    • pp.219-224
    • /
    • 2018
  • Necroptosis is an emerging form of programmed cell death occurring via active and well-regulated necrosis, distinct from apoptosis morphologically, and biochemically. Necroptosis is mainly unmasked when apoptosis is compromised in response to tumor necrosis factor alpha. Unlike apoptotic cells, which are cleared by macrophages or neighboring cells, necrotic cells release danger signals, triggering inflammation, and exacerbating tissue damage. Evidence increasingly suggests that programmed necrosis is not only associated with pathophysiology of disease, but also induces innate immune response to viral infection. Therefore, necroptotic cell death plays both physiological and pathological roles. Physiologically, necroptosis induce an innate immune response as well as premature assembly of viral particles in cells infected with virus that abrogates host apoptotic machinery. On the other hand, necroptosis per se is detrimental, causing various diseases such as sepsis, neurodegenerative diseases and ischemic reperfusion injury. This review discusses the signaling pathways leading to necroptosis, associated necroptotic proteins with target-specific inhibitors and diseases involved. Several studies currently focus on protective approaches to inhibiting necroptotic cell death. In cancer biology, however, anticancer drug resistance severely hampers the efficacy of chemotherapy based on apoptosis. Pharmacological switch of cell death finds therapeutic application in drug- resistant cancers. Therefore, the possible clinical role of necroptosis in cancer control will be discussed in brief.

Evaluation of Physico-chemical Properties of Acrylic Resin Hydrogel and their Application to Transdermal Delivery System

  • Chung, Uoo-Tae;Choi, Seung-Man;Kang, Kee-Long;Kim, Nak-Seo;Chung, Youn-Bok
    • Archives of Pharmacal Research
    • /
    • 제18권4호
    • /
    • pp.224-230
    • /
    • 1995
  • Recently, many attempts have been made to use hydrogels of various polymers as delivery systems of various drugs and bioactive materials to prolong and control their phamacological activities. In this study, we have evaluated the physico-chemical properties of methacrylic acid-methyacrylic acid methyl ester copolymer 9Eudispert mv)m a acrylic resin hydorgel, and its application to transdermal delivery system. In the dissolution tests, the release rate of salicylic acid (SA) and sodium salicylate (SOd. SA) were faster than lidocain (LD) and lidocain-HCl(LD-HCl). As the concentration of Eudispert mv polymer increased, the extensibility of Eudispert mu hydrogel decreased, whereas the swelling ratio increased. The more NaOH and polymer concentration increased, the more osmotic pressure linearly increased. The skin permeation of Sod. SA, an acidic model drug, was remarkably enhanced by Eudispert mv hydrogel. All fatty acids, except for Sod. glycolate, dramatically increased the skin permeation flux in Eudispert mu hydrogel containing LD-Hcl, a basic model drug. Consequently, it is suggested that Eudispert mv hydrogel may be used as potential transdermal delivery vehicle.

  • PDF

실비산의 항산화 및 지방축적 억제 효과 (Anti-oxidation and Fat Accumulation Inhibitory Effects of Silbi-san)

  • 김건우;우창훈;김영준;안희덕
    • 한방재활의학과학회지
    • /
    • 제30권4호
    • /
    • pp.41-53
    • /
    • 2020
  • Objectives The purpose of this study was to investigate the effects of Silbi-san on the antioxidant and fat accumulation inhibition and to analyze the anti-obesity effect by analyzing the changes in serum lipid composition in obese mice. Methods We compared contents of phytochemicals like total polyphenols and total flavonoid and antioxidant activities such as 2,2-dipheny-1-picrylhydrazyl and 2.2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) radical scavenging activity. After Silbi-san in 3T3-L1 cells in vitro and mouse adipose tissue ex vivo, we quantified intracellular triglyceride accumulation and lipolysis. Moreover, the anti-obesity activity though inhibiting pancreatic lipase were analyzed. In 3T3-L1 cells, morphological changes showed that control cells had many lipid while cells treated with Silbi-san had less lipid accumulation. 30% EtOH Silbi-san treatment also suppressed the fat absorption by inhibiting the activity of pancreatic lipase and led to high lipolysis through promoting glycerol release. The experimental group was divided into four groups: Normal group fed normal feed, Control group fed 60% high fat diet (HFD) and distilled water, drug group fed 60% high fat diet and 200 mg/kg of Silbi-san water extract, drug group fed 60% HFD and 200 mg/kg of Silbi-san 30% ethanol extract. Results Serum total cholesterol content and serum low density lipoprotein-cholesterol content were significantly decreased in the Silbi-san extract group compared to the control group, serum high density lipoprotein-cholesterol content was significantly increased in Silbi-san extract group. Conclusions In this study, the antioxidant and fat accumulation inhibitory effects of Silbi-san were confirmed.

Effects of Lactobacillus helveticus Fermentation on the Ca2+ Release and Antioxidative Properties of Sheep Bone Hydrolysate

  • Han, Keguang;Cao, Jing;Wang, Jinghui;Chen, Jing;Yuan, Kai;Pang, Fengping;Gu, Shaopeng;Huo, Nairui
    • 한국축산식품학회지
    • /
    • 제38권6호
    • /
    • pp.1144-1154
    • /
    • 2018
  • Both the calcium and collagen in bone powder are hard to be absorbed by the body. Although enzymatic hydrolysis by protease increased the bio-availability of bone powder, it was a meaningful try to further increase $Ca^{2+}$ release, oligopeptide formation and antioxidant activity of the sheep bone hydrolysate (SBH) by lactic acid bacteria (LAB) fermentation. Lactobacillus helveticus was selected as the starter for its highest protease-producing ability among 5 tested LAB strains. The content of liberated $Ca^{2+}$ was measured as the responsive value in the response surface methodology (RSM) for optimizing the fermenting parameters. When SBH (adjusted to pH 6.1) supplemented with 1.0% glucose was inoculated 3.0% L. helveticus and incubated for 29.4 h at $36^{\circ}C$, $Ca^{2+}$ content in the fermented SBH significantly increased (p<0.01), and so did the degree of hydrolysis and the obtaining rate of oligopeptide. The viable counts of L. helveticus reached to $1.1{\times}10^{10}CFU/mL$. Results of Pearson correlation analysis demonstrated that LAB viable counts, $Ca^{2+}$ levels, obtaining rates of oligopeptide and the yield of polypeptide were positively correlated with each other (p<0.01). The abilities of SBH to scavenge the free radicals of DPPH, OH and ABTS were also markedly enhanced after fermentation. In conclusion, L. helveticus fermentation can further boost the release of free $Ca^{2+}$ and oligopeptide, enhance the antioxidant ability of SBH. The L. helveticus fermented SBH can be developed as a novel functional dietary supplement product.

Transdermal Delivery of Ethinylestradiol UsingEthylene-vinyl Acetate Membrane

  • Shin, Sang-Chul;Byun, Soo-Young
    • Journal of Pharmaceutical Investigation
    • /
    • 제25권3호spc1호
    • /
    • pp.53-59
    • /
    • 1995
  • Ethinylestradiol (EE)-containing matrix was fabricated with ethylene-vinyl acetate(EVA) copolymer to control the release of the drug, Effect of addition of PEG 400 as receptor solution, the stripping of skin and Azone pretreatment on skin on the permeation of EE through the excised mouse skin was also studied. The permeation rate of EE through the excised mouse skin was affected by the PEG 400 volume fraction. The Azone pretreatment on skin didn't affect on the steady state flux, however, the lag time was shortened. The permeation rate of EE through the stripped skin was much larger than that through the whole skin. It showed that the stratum corneum acts as a barrier of skin permeation. The fact that there is little difference in EE permeation between the intact skin and the stripped skin with EVA membrane shows the permeation of EE through the mouse skin is mainly controlled by the membrane.

  • PDF

Preparation and Swelling Behaviors of Hydrogel Composed of Alginate, Poly(N-isopropylacrylamide) and Polyaniline

  • Lee, Young Moo;Seo, Sung Mi;Lee, Sang Bong
    • Korean Membrane Journal
    • /
    • 제6권1호
    • /
    • pp.37-43
    • /
    • 2004
  • Comb-type graft hydrogels composed of alginate and poly(N-isopropylacrylamide) (PNIPAAm) were prepared to manifest rapid temperature and pH sensitivity. To appear the electro-sensitivity, the polyaniline, conducting polymer, was added into the matrix. The swelling kinetics and ratios were compared under the various compositions of polyaniline. The swelling behaviors revealed that conducting polymer/hydrogel composites could control the swelling ratio and kinetics. The addition of polyaniline in the matrix improved the thermal stability in comparison with that of the hydrogel without polyaniline. In temperature sensitivity, the adding the polyaniline into the matrix decreased the degree of change in the swelling ratio. The swelling ratios continuously increased with increasing pH values. The drug release rate from the hydrogel increased with the adding the polyaniline and the applying the direct voltage to the hydrogels.

Topological Study of the Behavior of Inorganic Fine Powers and a Nanovesicle Hybridized Coating

  • Seo, Dong-Sung;Kim, Dong-Pyo;Jin, Fan-Long;Park, Soo-Jin
    • Bulletin of the Korean Chemical Society
    • /
    • 제30권2호
    • /
    • pp.343-347
    • /
    • 2009
  • In this study, the surface of inorganic fine powders is hybridized with nanovesicles containing tocopheryl acetate prepared with hydrogenated lecithin via a coating process. From AFM and SEM analyses it is found that the surface of the nanovesicle-coated fine powders lost their traditional topology and improved in terms of their roughness, skewness, and kurtosis. In addition, TEM observations revealed the formation of a 5 nm thick coating layer on the surface of the fine powders. These hybridized powders, in which bioactive materials such as tocopheryl acetate can be embedded, can be employed as a part of a drug delivery system due to their special ability to control release rate and temperature selectivity. Physical properties of the powders, i.e., the different angle and friction coefficient, were excellent.

약물 운반체로서의 폴리머 디스크 나노 입자에 대한 평가 (Assessment of Discoidal Polymeric Nanoconstructs as a Drug Carrier)

  • 배장열;오은설;안혁주;기재홍
    • 대한의용생체공학회:의공학회지
    • /
    • 제38권1호
    • /
    • pp.43-48
    • /
    • 2017
  • 우리가 예상했던 DPNs의 지름은 약 500 nm였으며 이는 SEM과 AFM 영상, Size Distribution을 통해 기대했던 것과 유사한 크기를 가진다는 것을 확인하였다. 또한, Zeta potential은 약 $-17.8{\pm}4.4mV$으로 측정되었다. Zeta potential이 +30 mV이상이면 강한 양성을 띤다고 한다. 나노 입자의 Zeta potential이 강한 양성이면 nonspecific cellular interaction이 높아지지만 간에 의해 쉽게 제거되며, hemolytic activity가 높아지기 때문에 약물 전달을 하기에 적합하지 않은 것으로 알려져 있다. 또한 강한 음성이어도 간에 의해 제거될 확률이 높아진다. 하지만 나노 입자의 Zeta potential이 중성이거나 약한 전하를 띠면 혈액에서 제거가 잘 되지 않아 혈액에 오랫동안 남을 수 있어 약물전달에 유리하고, 약 -15 mV의 전하를 띤 입자는 tumor site에 high accumulation됨이 알려져 있다[14]. DPNs의 경우 $-17.8{\pm}4.4mV$이므로 인체에 적용하기에 적합한 것으로 판단된다. DPNs의 Encapsulation Efficiency는 약 $43.8{\pm}6.6%$로 Nano-precipitation과 같은 Bottom-up 방식보다 낮은 수치를 나타내었지만, 독성이 강한 Salinomycin을 사용함으로써 이를 해결할 수 있을 것으로 생각되며 적은 양의 약물만으로 항암효과를 나타낼 수 있을 것으로 기대된다. 암세포와 함께 배양했을 때 형광 현미경으로 확인해본 결과 암세포 주변에 나노 입자가 이동한 것으로 보아 Targeting ligand나 Peptide, Aptamer를 이용하면 더욱 정확한 암세포 표적화를 이룰 수 있을 것으로 예상된다[15]. DPNs의 Drug Carrier로서의 평가는 Loading Amount와 Drug Releasing Profile을 통해 추가로 검증을 할 예정이며, Cell viability를 실행하여 DPNs의 In vitro 항암 효과를 확인하고 In vivo 실험을 진행할 예정이다.