• Title/Summary/Keyword: Prolonged release

Search Result 105, Processing Time 0.026 seconds

Poly(vinyl pyrrolidone) Conjugated Lipid System for the Hydrophobic Drug Delivery

  • Lee, Hye-Yun;Yu, Seol-A;Jeong, Kwan-Ho;Kim, Young-Jin
    • Macromolecular Research
    • /
    • v.15 no.6
    • /
    • pp.547-552
    • /
    • 2007
  • Water soluble polymer, poly(vinyl pyrrolidone) was chosen to conjugate with 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine-N-(succinyl) (N-succinyl DPPE) to make a new drug delivery system. PVP with an amine group (amino-PVP) was polymerized by free radical polymerization. The amine group of amino-PVP was conjugated with the carboxylic group of N-succinyl DPPE. The resultant conjugate could form nanoparticles in the aqueous solution; these nanoparticles were termed a lipid-polymer system. The critical aggregation concentration was measured with pyrene to give a value of $1{\times}10^{-3}g/L$. The particle size of the lipid-polymer system, as measured by DLS, AFM and TEM, was about 70 nm. Lipophilic component in the inner part of the lipid-polymer system could derive the physical interaction with hydrophobic drugs. Griseofulvin was used as a model drug in this study. The loading efficiency and release profile of the drug were measured by HPLC. The loading efficiency was about 54%. The release behavior was sustained for a prolonged time of 12 days. The proposed lipid-polymer system with biodegradable and biocompatible properties has promising potential as a passive-targeting drug delivery carrier because of its small particle size.

Experimental Studies on Activity of the Cultivated Mycelia of Phellinus linteus (상황(桑黃) 배양균사체의 활성에 관한 연구(I))

  • Kong, Young-Yun;Lee, Kwan-Ki;Nam, Sang-Yun;Hong, Nam-Doo
    • Korean Journal of Pharmacognosy
    • /
    • v.22 no.4
    • /
    • pp.233-239
    • /
    • 1991
  • Phellinus linteus was examined for its anticancer activity using an animal model. Water extract of Phellinus linteus was prepared from artificially cultivated mycelia. Neither toxicity nor abnormal changes of hematological parameters were observed in the rat given orally with high doses of drug extract for 15 days. ICR mice were transplanted with Sarcoma-180 tumor cells intraperitoneally and drug extract was daily given to the mice from 1 day after tumer transplantation for 3 weeks. Administration of drug extract significantly prolonged the survival duration of Sarcoma 180-transplanted mice. For the better understanding of the anticancer activity, we have examined the effect of the drug extract administration on various killer cell functions, such as natural killer(NK) cells, cytotoxic T-lymphocytes (CTL) and macrophages which have been known to be main effector cells in immune responses against tumors. The results from the 4 hr $^{51}Cr-release$ assay have shown that the drug extract augments mouse NK cell activity but neither CTL nor macrophages. It is possible, then, that the anticancer activity of the Phellinus linteus may be associated with augmentation of NK cell function in the cancerated hosts.

  • PDF

Electrical Stimulation Causes Endothelium-Dependent Relaxation in Isolated Aortic Vessels of the Rabbit (토끼 흉부 대동맥 절편의 전기자극에 대한 수축 및 이완반응)

  • Lee, Seok-Gi;Choe, Hyeong-Ho;Lee, Jong-Un
    • Journal of Chest Surgery
    • /
    • v.28 no.8
    • /
    • pp.742-746
    • /
    • 1995
  • The present study was aimed at investigating possible transmitter mechanisms in the endothelial cell layer in regulating the tone of the vascular smooth muscle. The thoracic aorta was isolated from the anesthetized male white rabbits and its helical strips were prepared. Electrical field stimulation was delivered to platinum wire electrodes positioned parallel to the vessel segment preconstricted with phenylephrine [3.5x10-6 mol/L at a distance of 1.5-2.0 mm. The electrical stimulation [70 V, 5 msec, 0.5-200 Hz caused either relaxation only [34% or a biphasic response [prolonged relaxation following a weak and transient contraction, 66% . The relaxation response was frequency- dependent, and at 200 Hz a complete relaxation was noted. Mechanical rubbing of the endothelial layer abolished or greatly attenuated the relaxation. The relaxation was also markedly attenuated in the presence of NG-nitro- L-arginine methyl ester [10-3mol/L or procaine hydrochloride [3.5x10-4mol/L . Tetrodotoxin,guanethidine, atropine or indomethacin failed to block or enhance the relaxation response to electrical field stimulation. It is concluded that the vascular endothelium in the aorta contains diffusible substances that regulates the function of the smooth muscle layer, in which relaxation is more prominent than contraction. Their release by the electrical stimualtion in vitro may not involve classic neuronal transmitter release mechanisms or metabolism of arachidonic acids by cyclooxygenase. The release of the relaxing agents may require an increase in cytosolic calcium level. The chemical nature of the relaxant may be, to a large extent, nitric oxide.

  • PDF

Controlled Release of Nerve Growth Factor from Sandwiched Poly(L-lactide-co-glycolide) Films for the Application in Neural Tissue Engineering

  • Gilson Khang;Jeon, Eun-Kyung;John M. Rhee;Lee, Ilwoo;Lee, Sang-Jin;Lee, Hai-Bang
    • Macromolecular Research
    • /
    • v.11 no.5
    • /
    • pp.334-340
    • /
    • 2003
  • In order to fabricate new sustained delivery device of nerve growth factor (NGF), we developed NGF-loaded biodegradable poly(L-lactide-co-glycolide) (PLGA, the mole ratio of lactide to glycolide 75:25, molecular weight: 83,000 and 43,000 g/mole, respectively) film by novel and simple sandwich solvent casting method for the possibility of the application of neural tissue engineering. PLGA was copolymerized by direct condensation reaction and the molecular weight was controlled by reaction time. Released behavior of NGF from NGF-loaded films was characterized by enzyme linked immunosorbent assay (ELISA) and degradation characteristics were observed by scanning electron microscopy (SEM) and gel permeation chromatography (GPC). The bioactivity of released NGF was identified using a rat pheochromocytoma (PC-12) cell based bioassay. The release of NGF from the NGF-loaded PLGA films was prolonged over 35 days with zero-order rate of 0.5-0.8 ng NGF/day without initial burst and could be controlled by the variations of molecular weight and NGF loading amount. After 7 days NGF released in phosphate buffered saline and PC-12 cell cultured on the NGF-loaded PLGA film for 3 days. The released NGF stimulated neurite sprouting in cultured PC-12 cells, that is to say, the remained NGF in the NGF/PLGA film at 37 $^{\circ}C$ for 7 days was still bioactive. This study suggested that NGF-loaded PLGA sandwich film is released the desired period in delivery system and useful neuronal growth culture as nerve contact guidance tube for the application of neural tissue engineering.

Swelling and Drug Release Characteristics of PVP Hydrogel Polymerized by $\gamma$-Irradiation Method (김마선 조사법으로 합성한 PVP하이드로겔의 팽윤과 약물방출특성)

  • 심창구;오정숙;신병철
    • YAKHAK HOEJI
    • /
    • v.37 no.5
    • /
    • pp.511-519
    • /
    • 1993
  • The short and variabke transit of drug throught GI tracj and the inter-and intra-subject variations of the transit restrict the sustained drug absorption after oral adminstration. These restrictions may be solved by retaining the dosage forms in the stomach. Then the dosage form will act as a platform which releases the drug slowly and makes the GI absorption occur for a long time. In this study, as the platforms, PVP hydrogels were synthesized by chemical and y-irradiation method in the cylindrical test tube. The chemical method means the synthesis of the hydrogel by heating the mixed solution of N-vinyl-2-pyrrolidone [monomer], acrylated albumin [crosslinking agent], 2, 2'-agobis(2-methylpropionitrile) [initiator] and proxyphylline [drug] at $65^{\circ}C$ for 5 hr. The $\gamma$-irradiation method means the synthesis of the hydrogel by irradiation with $^{60}$ Co $\gamma$-ray of the mixed solution of the monomer, acrylated albumin, and flurbiprofen [drug] at room temperature with total 0.2 Mrad for 3 hr. Our intention is to design the hydrogel tablet (diameter : 1.20 cm, thickness : 0.60 cm) which swells in the gastric fluid after oral administration to such a size that passing through the pylorus could be inhibited during the period of drug release. After releasing drug, the hydrogel should be degraded by the enzymeatic digestion in the stomach, or by hydrolysis and eventually solubilized. Thus, in votro tests were performed to examine the factors that affect swelling and drug release from the PVP hydrogels. Experimental results show that the hydrogels swell to a size larger than the diameter of the pylorus(l.3$\pm$0.7 cm) and the hydrogel prepared by the chemical method is digested by pepsin. But the hydrogel prepared by the $\gamma$-irradiation method was not digested by the pepsin and just collapsed with time. Thus, the swelling of the hydrogel synthesized by $\gamma$-irradiation was independent albumin acrylation time and pepsin concentration. But drug content and radiation dose affected the swelling and drug release kinetics of the hydrogel. Drug release from the hydrigels was prolonged up to about 24 hr. Therefore, it was concluded that by adjusting these factors, the albumin-crosslinked PVP hydrogel synthesized by $\gamma$-irradiation method is expected to be retained in the stomach for up to 60hr and be a potential platform of drugs for long-term GI absorption.

  • PDF

Effects of Shear Strains on the Developement of Texture and Microstructure of $90\%$ Drawn Copper Wire during Annealing ($90\%$ 단면감소율로 인발된 전해동의 어닐링시 집합조직과 미세조직 발달에 미치는 전단 변형의 영향)

  • Park, Hyun;Lee, Dong-Nyung
    • Proceedings of the Korean Society for Technology of Plasticity Conference
    • /
    • 2001.11a
    • /
    • pp.55-62
    • /
    • 2001
  • An electrolytic copper rod was drawn up to $90\%$ in area reduction and annealed under various conditions. The EBSD measurement of the drawn wire showed that in the center region the <111> + <100> fiber duplex texture was dominant, while in the middle and surface regions relatively defused textures developed with a little higher density in <11w>//wire axis. The inhomogeneous texture in the deformed wire gave rise to the inhomogeneous microstructure and texture after annealing. The annealing texture could be classified into the recrystallization texture developed during low temperatures and at the early stage at a high temperature and the growth texture developed after a prolonged annealing at the high temperature. The recrystallization temperature could be explained by the strain energy release maximization model and the growth texture was discussed based on the grain boundary mobility anisotropy.

  • PDF

New Method of Injectable Hydrogels by Novel Photo-polymerization

  • Lee, Seung-Young;Tae, Gi-Yoong
    • Proceedings of the Polymer Society of Korea Conference
    • /
    • 2006.10a
    • /
    • pp.252-252
    • /
    • 2006
  • Utilizing the existence of the induction period in photo-polymerization, we propose a new injection method of photo-polymerizable, thermocrosslinking hydrogels made of di-acrylated Pluronic F127 (DA-PF127). This method can solve the problem of fast dissolution of thermal gelation as a scaffold and the disadvantages of the existing injection method that photo-polymerize di-acrylated Pluronic polymer after injection using optical fiber. Injectable gelation of DA-PF127 by the proposed method was demonstrated both in vitro and in vivo. The enhanced stability by this novel photo-polymerization strategy was confirmed by the more sustained release of loaded protein as well as the prolonged degradation time of the hydrogels.

  • PDF

Improvement of Haemostasis Mediated by Anti-Platelet Activities by Plant Vinegar (목초액의 혈소판 응집억제를 통한 혈행개선 작용에 관한 연구)

  • 김영대;배옥남;정승민;정진호
    • Toxicological Research
    • /
    • v.20 no.2
    • /
    • pp.137-142
    • /
    • 2004
  • We investigated the effects of plant vinegar on platelets and blood coagulation system. Plant vinegar inhibited in vitro platelet aggregation in a concentration dependent manner, when platelets were activated by thrombin and collagen. In addition, plant vinegar showed inhibitory effects on the serotonin secretion induced by thrombin in a concentration dependent manner. However, treatment with plant vinegar to platelets did not induce any cytotoxicity, as determined by the release of lactate dehydrogenase. Plant vinegar did not change the coagulation parameters such as activated partial thromboplastin time (aPTT) and prothrombin time (PT) using rat citrated plasma. In vivo study revealed that, treatment with plant vinegar prolonged the bleeding time from mouse tail. All these results suggest that plant vinegar might improve blood hemostasis mediated via anti platelet activities.

Theoretical Study for the Characteristics of Melatonin (멜라토닌의 특성에 대한 이론적 연구)

  • Kim, Dong-Yeub;Jung, Maeng-Joon;Lee, Chul-Jae
    • Journal of the Korean Society of Industry Convergence
    • /
    • v.15 no.2
    • /
    • pp.59-63
    • /
    • 2012
  • Melatonin has been studied as a potential treatment of cancer, immune disorders, cardiovascular diseases, depression, seasonal affective disorder (SAD), circadian rhythm sleep disorders, sexual dysfunction and some forms of insomnia. Prolonged release melatonin has shown good results in treating insomnia in older adults. It may ameliorate circadian misalignment and SAD. Basic research indicates that melatonin may play a significant role in modulating the effects of drugs of abuse such as cocaine. A 2004 review found that melatonin significantly increased total sleep time in people suffering from sleep restriction. Therefore, in this study, in order to explain characteristics of melatonin, total energy, net charge, vibrational mode of melatonin are calculated by PM3 methods of HyperCam 6.0.

Posttraumatic Stiffness (외상 후 동결견)

  • Choi, Chang-Hyeok
    • Clinics in Shoulder and Elbow
    • /
    • v.9 no.1
    • /
    • pp.14-19
    • /
    • 2006
  • The patient with a posttraumatic stiffness frequently has a history of prolonged immobilization after a traumatic event. Adhesions in the extraarticular humeroscapular motion interface may be present independently or in combination with intraarticular capsular contractures. A through history and physical examination usually reveal the cause and anatomic location of stiffness. Passive stretching exercise program is effective as a first line treatment, but manipulation under anesthesia is usually not effective because of potential complication such as fracture, tendon rupture and neurologic injury. The humeroscapular motion interface adhesion can be released either open or arthroscopically. The combined technique coupled with an aggressive rehabilitation program can provide more effective motion restoration and pain relief.