• Title/Summary/Keyword: sustained release

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Effects of Biodegradable Cephalexin Microspheres in Dry Cow Mastitis Therapy (젖소의 건유기 유방염 치료에 있어서 생분해 cephalexin microspheres의 효과)

  • Hwang, Cheol-Yang
    • Journal of Veterinary Clinics
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    • v.19 no.2
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    • pp.228-235
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    • 2002
  • Mastitis is the most costly disease results in lost milk production, decreased milk quality, milk discard, early culling of cows, drug costs and labor costs in dairy cow. Until now, a antibiotic administration at the end of lactation, dry cow therapy has been known the most effective and widely used mastitis control method. However, dry cow therapy do not control a new infection in the late dry and prepartum period because dry cow products have only persistent activity in the early dry period. Therefore, this study was conducted to evaluate clinical effect of sustained released biodegradable cephalexin microsphere using PLGA in bovine mastitis control during dry period. PLGA has been approved as controlled drug release system because of non-toxic, non-tissue reactive and bioerodible characteristics. This study revealed that cephalexin microsphere had a spherical shape with characteristic porous structure on the surface. Also, in vitro drug release studies are clearly observed that the release rate of cephalexin from PLGA microsphere decrease during the first 21 days after initial burst and then increase again between 3 and 4 weeks showing pulsatile releasing pattern. On the other hand, as tried in field the new infection rate, cure rate and mean SCC after parturition in cephalexin microsphere infused group were significantly differenced as compared to the control group. Accordingly, a sustained release of cephalexin from a biodegradable microsphere could make dry cow therapy more efficiently by preventing a new infection and decreasing the number of existing infection of mammary gland during dry period.

Fabrication of Luminescent Hydroxyapatite Microspheres for Drug Loading and Release

  • Park, So Yeon;Kwon, Seung Lee;Baek, Mi Yeon;Yoo, Jin Sun;Kim, Min-Cheol;Jung, Hyun Suk
    • Proceedings of the Korean Vacuum Society Conference
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    • 2016.02a
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    • pp.360.1-360.1
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    • 2016
  • Hydroxyapatite (Ca10(PO4)6(OH)2, HAP) particles have attracted a great deal of attention in biomedical fields due to their good biocompatibility, bioactivity and fairly broad applications as drug delivery, dental implant, bone cement, and etc. Thus, many researchers have made an effort to add new functionalities such as luminescence, drug delivery, and bone regeneration properties up to HAP powders by controlling their nanostructure as well as composition. In this research, the mesoporous strontium substituted HAP (Sr-HAP) microspheres were synthesized using a hydrothermal method. In this synthesis, aspartic acid monomers were utilized to form microsphere by controlling surface energy of HAP particles and Sr ions were substituted into Ca ion sites, which induced luminescence property in HAP powders. Moreover, the change in the amount of Sr substitution was found to influence the particle size, morphology, and concurrently surface area, which led to changing drug loading as well as drug release property. The amount of Sr influences the morphology, luminescent properties, particle size, surface area cell viability and drug loading property, which are investigated by SEM, TEM, XRD, FTIR, BET, XPS and in vitro test such as MTT assay and drug release test. In particular, the multifunctional Sr-HAP with molar ratios of 0.25 (Sr/(Ca+Sr)) possessed the strongest luminescent property as well as the superior drug loading and sustained release properties that were correspondent with large surface area and pore size. Our study indicates that the fabricated multifunctional Sr-HAP microspheres are quite useful for bone regeneration and drug delivery.

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Application of Stimuli-responsive Chitosan Micelles for Improved Therapeutic Efficiency of Anticancer Agents (항암제의 치료 효율성을 높이기 위한 다양한 자극 응답성 물질이 개질된 키토산 마이셀의 응용성 고찰)

  • Jeong, Gyeong-Won;Park, Jun-Kyu;Nah, Jae-Woon
    • Applied Chemistry for Engineering
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    • v.29 no.2
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    • pp.147-154
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    • 2018
  • Currently, to overcome low therapeutic efficiencies and side effects of anticancer agents, the study of drug carrier based on polymers have been consistently investigated. Although the traditional drug carrier based on polymers displayed an excellent result and significant progress, there has been a problem with the side effect and low therapeutic efficiency because of the premature drug release before reached to the targeted region by the low stability in blood stream and sustained drug release. In this review article, to improve the problem of inefficient drug release, methods were suggested, which can maximize the therapeutic efficiency by increasing the stability in the blood stream and triggering drug release at the target site by introducing a stimuli-responsive substance to the non-toxic and biocompatible natural polymer chitosan.

Controlled Release Behavior of Bioactive Molecules from Photo-Reactive Hyaluronic Acid-Alginate Scaffolds

  • Nam, Hye-Sung;An, Jeong-Ho;Chung, Dong-June;Kim, Ji-Heung;Chung, Chong-Pyoung
    • Macromolecular Research
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    • v.14 no.5
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    • pp.530-538
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    • 2006
  • There are three important components in tissue engineering: the cells, signaling factors (cytokines and growth factors), and scaffolds. To obtain finely engineered tissue, all three components should perform their individual functions and be fully integrated with each other. For the past few years, we have studied the characteristics of photodimerizable HA (CHA)/alginate (CA) composite materials. CHA/CA complex hydrogels, which were irradiated under UV light and, then treated with calcium ions, were found to have good biocompatibility, mechanical properties and water resistance for implantable tissue scaffolds. In this study, we introduced a cell growth factor (basic fibroblast growth factor; bFGF) into the CHA/CA scaffolds and studied its release behavior. We also introduced tetracycline hydrochloride and flurbiprofen into the same scaffolds as model activation factors and evaluated their release behaviors from the scaffolds. The drug release rate from the materials was influenced by various parameters, such as the degree of crosslinking, the cross linker type, the physico-chemical properties of the drug, and the amount of the drug in the polymer. The results indicated that the negatively charged CHA/CA composite materials showed sustained release behavior and that HA has a particularly strong negative charge, making it attractive toward tetracycline hydrochloride and bFGF, but repulsive toward flurbiprofen.

Antibiofilm activity of polyethylene glycol-quercetin nanoparticles-loaded gelatin-N,O-carboxymethyl chitosan composite nanogels against Staphylococcus epidermidis

  • Wanhe Luo;Yongtao Jiang;Jinhuan Liu;Beibei Sun;Xiuge Gao;Samah Attia Algharib;Dawei Guo;Jie Wei;Yurong Wei
    • Journal of Veterinary Science
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    • v.25 no.2
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    • pp.30.1-30.16
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    • 2024
  • Background: Biofilms, such as those from Staphylococcus epidermidis, are generally insensitive to traditional antimicrobial agents, making it difficult to inhibit their formation. Although quercetin has excellent antibiofilm effects, its clinical applications are limited by the lack of sustained and targeted release at the site of S. epidermidis infection. Objectives: Polyethylene glycol-quercetin nanoparticles (PQ-NPs)-loaded gelatin-N,O-carboxymethyl chitosan (N,O-CMCS) composite nanogels were prepared and assessed for the on-demand release potential for reducing S. epidermidis biofilm formation. Methods: The formation mechanism, physicochemical characterization, and antibiofilm activity of PQ-nanogels against S. epidermidis were studied. Results: Physicochemical characterization confirmed that PQ-nanogels had been prepared by the electrostatic interactions between gelatin and N,O-CMCS with sodium tripolyphosphate. The PQ-nanogels exhibited obvious pH and gelatinase-responsive to achieve on-demand release in the micro-environment (pH 5.5 and gelatinase) of S. epidermidis. In addition, PQ-nanogels had excellent antibiofilm activity, and the potential antibiofilm mechanism may enhance its antibiofilm activity by reducing its relative biofilm formation, surface hydrophobicity, exopolysaccharides production, and eDNA production. Conclusions: This study will guide the development of the dual responsiveness (pH and gelatinase) of nanogels to achieve on-demand release for reducing S. epidermidis biofilm formation.

Hyaluronic Acid in Drug Delivery Systems

  • Jin, Yu-Jin;Ubonvan, Termsarasab;Kim, Dae-Duk
    • Journal of Pharmaceutical Investigation
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    • v.40 no.spc
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    • pp.33-43
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    • 2010
  • Hyaluronic acid (HA) is a biodegradable, biocompatible, non-toxic, non-immunogenic and non-inflammatory linear polysaccharide, which has been used for various medical applications including arthritis treatment, wound healing, ocular surgery, and tissue augmentation. Because of its mucoadhesive property and safety, HA has received much attention as a tool for drug delivery system development. It has been used as a drug delivery carrier in both nonparenteral and parenteral routes. The nonparenteral application includes the ocular and nasal delivery systems. On the other hand, its use in parenteral systems has been considered important as in the case of sustained release formulation of protein drugs through subcutaneous injection. Particles and hydrogels by various methods using HA and HA derivatives as well as by conjugation with other polymer have been the focus of many studies. Furthermore, the affinity of HA to the CD44 receptor which is overexpressed in various tumor cells makes HA an important means of cancer targeted drug delivery. Current trends and development of HA as a tool for drug delivery will be outlined in this review.

Inhibition of Apoptosis is Responsible for the Acquired Resistance of K562 Cells to Cisplatin

  • Lee, Soo-Yong;Kim, Dong-Hyun
    • Biomolecules & Therapeutics
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    • v.12 no.2
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    • pp.85-91
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    • 2004
  • In all attempt to elucidate the role of apoptosis in drug resistance, cisplatin-resistant human chronic myelogenous leukemia (CML) K562 cells (K562/CDDP) were established and compared with drug sensitive parent cells (K562) in the induction of apoptosis. K562/CDDP cells were 5-fold more resistant to cisplatin compared to K562 cells. In addition, K562/CDDP cells were significantly more resistant to apoptois as judged by DNA fragmentation and DAPI staining. K562/CDDP cells exhibited decreased proleolytic activity of caspase-3 and this was further demonstrated by decreased cleavage of its substrate poly (ADP-ribose) polymerase (PARR- Western blot analysis showed that K562/CDDP cells had longer sustained levels of BCL-$X_L$ whereas no difference was noted in the level of Bcl-2. the translocation of Bax to mitochondria was significantly delayed in K562/CDDP cells. These results suggest that the reduced translocation of Bax and the sustained expression of BCL-$X_L$ may cause resistance to apoptosis through prevention of mitochondria release of cytochrome c, which subsequently induces reduction of caspase-3 activity and that this response is partly responsible for the acquired resistance to cisplatin ill K562 cells.

Tranilast-delivery surgical sutures to ameliorate wound healing by reducing scar formation through regulation of TGF-β expression and fibroblast recruitment

  • Choi, Sung Yoon;Kim, Byung Hwi;Huh, Beom Kang;Jeong, Woong;Park, Min;Park, Hyo Jin;Park, Ji-Ho;Heo, Chan Yeong;Choy, Young Bin
    • Journal of Industrial and Engineering Chemistry
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    • v.67
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    • pp.469-477
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    • 2018
  • We describe surgical sutures enabled with the local, sustained delivery of a TGF-${\beta}$ inhibitory drug, tranilast. To fabricate drug-delivery sutures, we separately prepared a tranilast-loaded strand using poly (lactic-co-glycolic acid), which was then physically braided with a surgical suture already in clinical use. By this method, the drug-delivery sutures maintained the mechanical strength and allowed the modulation of drug release profiles by simply altering the tranilast-loaded strand. The drug-delivery sutures herein released tranilast for up to 14 days. When applied to animal models, scarring was indeed reduced with diminished TGF-${\beta}$ expression and fibroblast numbers during the entire 21 day testing period.

Update on Transarterial Chemoembolization with Drug-Eluting Microspheres for Hepatocellular Carcinoma

  • Yasir M. Nouri;Jin Hyoung Kim;Hyun-Ki Yoon;Heung-Kyu Ko;Ji Hoon Shin;Dong Il Gwon
    • Korean Journal of Radiology
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    • v.20 no.1
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    • pp.34-49
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    • 2019
  • Conventional transcatheter arterial chemoembolization (c-TACE) is a widely used first-line palliative treatment for patients with unresectable hepatocellular carcinoma (HCC). Despite the effectiveness of c-TACE, to date, technique and procedure scheduling has not yet been standardized. Drug-eluting microspheres (DEMs) were therefore introduced to ensure more sustained and tumor-selective drug delivery for permanent embolization. These DEMs can load various drugs and release them in a sustained manner over a prolonged period. This approach ensures the delivery of high concentrations of chemotherapeutic agents to tumors, without increasing systemic concentrations, and promote tumor ischemia and necrosis. This review summarizes the recent advances in the use of DEM-TACE to treat HCC.

Controlled Release of Cefadroxil from Chitosan Beads in Dogs (개에서 키토산 비드를 이용한 cefadroxil 방출제어)

  • Kim Dae-Keun;Park Seung-Chun;Kim Tae-Wan;Lee Keun-Woo;Oh Tae-Ho
    • Journal of Veterinary Clinics
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    • v.22 no.3
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    • pp.175-180
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    • 2005
  • The purpose of this study is to investigate the effects of formulation variables on the release of cefadroxil form chitosan beads, to optimize the preparation of chitosan beads loaded with the drug for controlled release, and to evaluate the drug release form chitosan beads in dogs. Chitosan beads were prepared with tripolyphosphate (TPP) by ionic cross-linking and those sizes were less than 1 mm in diameter. The release behaviour of cefadroxil was affected various factors. As pH of TPP solutions decreased, the entrapment efficiency of cefadroxil increased, whereas the release of cefadroxil decreased. The release rate of cefadroxil form chitosan beads decreaed with the increased TPP solution concentration. When cross-linking time increased, the release of the drug from chitosan beads decreased. The cefadroxil loaded beads were implanted to 4 mixed breed dogs. The concentration of cefadroxil in sera due to chitosan beads implanted with 50 mg/kg body weight of beads was sustained more than 1 ug/ml for the whole 7 days period. Therefore, the cefadroxil loaded beads can be used successfully in pyoderma of dogs. These results indicate that chitosan beads may become a potential delivery system to control the release of drug.