• Title/Summary/Keyword: drug release rate

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Optimization of In Vivo Embryo Production and Pregnancy following Embryo Transfer in Hanwoo Cattle

  • Jeon, Soon-Hong;Jung, Kyoung Sub;Choi, Jae-Won;Heo, Young-Tae;Xu, Yong-Nan;Kim, Nam-Hyung
    • Journal of Embryo Transfer
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    • v.28 no.4
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    • pp.307-314
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    • 2013
  • Embryos formed in vivo were collected from 171 donors housed in Chung Cheong Buk-Do Institute of Livestock and Veterinary Research of the Chungbuk community during the years 2009~2012. We evaluated annual embryo collection, effect of follicle stimulating hormone (FSH), controlled internal drug release (CIDR) and prostaglandin (PG) administration to the donor for superovulation and controlling the estrus cycle, seasonal effects of embryo collection and compared the number of embryos recovered as per the collection days and pregnancy rate. In all, 1,243 embryos were collected from 118 donors with an average of $7.31{\pm}5.35$ embryos per donor, out of which 69.4% were transferable. Dosages of FSH required for inducing superovulation in various donors were compared. Average number of embryos collected from donors administered with 30 AU of FSH ($7.13{\pm}5.74$ per donor) was not significantly different from that of donors who were given an injection of 24 AU of FSH ($7.53{\pm}4.91$ per donor). However, the percentage of transferable embryos in the 30AU FSH-administered group (63.2 %, 449 of 711) was higher than that in the 24AU FSH-administered group (77.8%, 414 of 532). In the group of donors under a natural estrus cycle, the FSH dose administered did not influence the number of transferable embryos produced ($7.49{\pm}6.25$ per donor for 30 AU of FSH vs $7.49{\pm}4.92$ per donor for 24 AU of FSH). However, in donors administered with CIDR and PG for controlling the estrus cycle, the FSH dose affected the average number of transferable embryos collected ($4.25{\pm}2.87$ per donor for 30 AU of FSH vs $8.50{\pm}6.36$ per donor for 24 AU of FSH). We collected embryos from donors 6, 7 or 8 days after artificial insemination (AI). Results showed that the percentage of transferable embryos among those collected 8 days after AI was significantly higher than that among embryos collected 6 or 7 days after AI. Seasonal variations did not affect number of recovered embryos and pregnancy rates in natural estrus cycle and CIDR treatment groups (48.28% and 42.55%) but higher than pregnancy rate of frozen embryos (19.63%). These results indicated that administration of FSH beyond a threshold dose (at least 24 AU) has no beneficial effect on the production embryos and that collection of embryos 7~8 days after AI is optimal for embryo recovery. CIDR treatment induced superovulation in short term and had no influence on the natural estrus cycle. Finally, although good-quality embryos were transferred, freezing significantly reduced the pregnancy rates after transfer.

Application of Various Hydrophobic Moiety-modified Chitosan Nanoparticle as a Drug Delivery Carrier (다양한 소수성 물질이 개질된 키토산 나노입자의 약물전달체로서 응용성 고찰)

  • Jeong, Gyeong-Won;Nah, Jae-Woon;Park, Jun-Kyu
    • Applied Chemistry for Engineering
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    • v.28 no.4
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    • pp.404-409
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    • 2017
  • Natural polymer chitosan has been widely applied to medical fields due to its biochemical activities such as anticancer, antibacterial and lowering cholesterol in addition to biocompatibility and biodegradability. Currently, researches are being actively conducted to develop various drug-encapsulated chitosan nanoparticles for curing different diseases by applying chitosan to a drug delivery system. The free amine ($-NH_2$) group present in chitosan can bind to various hydrophobic groups by physical and chemical modification and the chitosan with hydrophobic groups can form shell-core nanoparticles by self-assembly when dispersed in water. In addition, an insoluble drug can increase the solubility against water when it was encapsulated in the core of chitosan nanoparticles. Also, the therapy effect can be maximized by minimizing side effects of drugs such as proteins, anticancer drugs and vaccines when they were encapsulated in the core of chitosan nanoparticles. Moreover, it is possible to control the particle size and release rate according to the hydrophobic group introduced to chitosan, so that it can be applied to a wide range of medical fields. The purpose of this review is to discuss the preparation and property of chitosan nanoparticles modified with various hydrophobic groups, and the application to drug delivery systems according to their property.

Electrospraying of Micro/Nano Particles for Protein Drug Delivery (단백질 약물 전달을 위한 마이크로/나노 입자의 전기분무 제조법)

  • Yoo, Ji-Youn;Kim, Min-Young;Lee, Jong-Hwi
    • Polymer(Korea)
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    • v.31 no.3
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    • pp.215-220
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    • 2007
  • The control of the surface energy by electrohydrodynamic force provides electrospraying with various potential advantages such as simple particle size control, mono-dispersity, high recovery, and mild processing conditions. The advantages are quite helpful to improve the stability of protein drug and control its release. Herein, the nano-encapsulation of protein drugs using electrospraying was investigated. Albumin as a model protein was processed using uniaxial and co-axial electrospraying, and chitosan, polycaporlactone (PCL), and poly (ethylene glycol) (PEG) were used as encapsulation materials. The major processing parameters such as the conductivity of spraying liquids, flow rate, the distance of electrical potential gradient, etc were measured to obtain the maximum efficiency. In the chitosan systems, mean particles size decreases as flow rate and the distance between nozzle and the collecting part decreases. In the uniaxial technique of the PCL systems, mean particles size decreases as flow rate decreases. In the coaxial technique of the PCL systems, it was found that the particles size gets larger under the application of the higher ratio of inner-to-outer liquid flow rates. The primary particles formed out of an electrospraying nozzle showed narrow particle size distribution, but once they arrived to the collecting part, aggregation behavior was observed obviously. Efficient nano-encapsulation of albumin with PCL, PEG, and chitosan was conveniently achieved using electrospraying at above 12 kV.

Sibutramine Release Behavior from Microspheres Prepared by Spray-Dry Method (분무건조 방법으로 제조된 미립구에서 Sibutramine의 방출거동)

  • Park, Jung-Soo;Oh, Jung-Soo;Oh, Jae-Min;Kim, Yun-Tae;Lee, Jun-Hee;Mo, Jong-Hyun;Lee, Hai-Bang;Khang, Gil-Son
    • Polymer(Korea)
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    • v.32 no.3
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    • pp.193-198
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    • 2008
  • Sibutramine is a highly crystalline and poorly water soluble drug as the appetite depressant for obesity treatment. In order to increase water solubility of sibutramine, microspheres including sibutramine were prepared by solid dispersion method using a spray dryer. The crystallinity and morphology of the prepared microspheres were confirmed by SEM and XRD. The morphology of micro spheres has gradually changed into spherical shape as increasing evaporation rate of solvent. According to XRD analysis, crystallinity of sibutramine in micro spheres was decreased by below 10%. Release behavior of microspheres was investiaged at pH 1.2, pH 6.8, and solubility of the sibutramine was significantly different depending on pH. The hard capsule showed fast release of sibutramine comparing with the tablet. These results demonstrated that the pharmaceutical preparation is able to control the release behaviors.

Assessment of In Vitro Assay System for Thyroid Hormone Disruptors Using Rat Pituitary GH3 Cells

  • Kim, Hee-Jin;Park, Hae-Young;Kim, Jeong-A;Kang, Il-Hyun;Kim, Tae-Sung;Han, Soon-Young;Kang, Tae-Seok;Park, Kui-Lea;Kim, Hyung-Sik
    • Toxicological Research
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    • v.22 no.4
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    • pp.307-313
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    • 2006
  • The development of in vitro assays has been recommended to screening and testing the potential endocrine disruptors (EDs). These assay systems focus only on identifying the estrogenic or antiestrogenic activity of EDs, whereas a few studies have been carried out to screen the thyroid hormone (TH) disruptors. The aim of this study was to evaluate a test system to detect TH disruptors using rat pituitary tumor $GH_3$ cells. The test system is based on the TH-dependent increase in growth rate. As expected, L-3,5,3-triiodothyronine ($(T_3)$ markedly induced a morphological change in $GH_3$ cells from flattened fibroblastic types to rounded or spindle-shaped types. $T_3$ stimulated $GH_3$ cell growth in a dose-dependent manner with the maximum growth-stimulating effect being observed at a concentration $1{\times}10^9M$. In addition, $T_3$ increased the release of growth hormone and prolactin into the medium of the $GH_3$ cells culture. Using this assay system, the TH-disrupting activities of bisphenol A (BPA) and its related compounds were examined. BPA, dimethy/bisphenol A (DMBPA), and TCI-EP significantly enhanced the growth of $GH_3$ cells in the range of $1{\times}10^{-5}M\;to\;1{\times}10^{-6}M$ concentrations. In conclusion, this in vitro assay system might be useful for identifying potential TH disruptors. However, this method will require further evaluation and standardization before it can be used as a broad-based screening tool.

Improvement of Dissolution Rate for Zaltoprofen Tablets Using CMC and HPMC (CMC와 HPMC를 이용한 잘토프로펜 정제의 용출률 개선)

  • Park, Hyun-Jin;Hong, Hee-Kyung;Song, Yi-Seul;Hong, Min-Sung;Seo, Han-Sol;Hong, Dong-Hyun;Lee, Dong-Won;Khang, Gil-Son
    • Polymer(Korea)
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    • v.34 no.4
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    • pp.300-305
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    • 2010
  • Zaltoprofen is a propionic acid derivative of non-steroidal anti-inflammatory drugs (NSAIDs) and has been widely used in the treatment of a number of arthritic conditions or lumbago. Zaltoprofen has low water solubility and low bioavailability, therefore great efforts have been devoted to enhance the extent of drug adsorption. In this study, zaltoprofen was formulated into a tablet to enhance the bioavailability and to achieve sustained-release using additives such as lactose monohydrate, carboxymethylcellulose (CMC), hydroxypropylmethylcellulose (HPMC). Fourier transform-infrared (FTIR) and differential scanning calorimeter (DSC) were employed to study the structure and crystallization of zaltoprofen in the tablet with various contents of additives. It was found that additives had interactions with zaltoprofen and inhibited the crystallization of zaltoprofen. Tablets containing low viscosity HPMC showed a higher release than those containing high viscosity HPMC. Also, as the amount of CMC increased zaltoprofen release increased.

Relationship Between Dissolution Patterns of Carbamazepine Tablet and Dissolution Medium Composition (카르바마제핀 정제 용출패턴과 용출액 조성과의 상관성)

  • Lee, Hyeon-Tae;Kim, Jeong-Ho;Kim, Hyun-Joo;Sah, Hong-Kee
    • Journal of Pharmaceutical Investigation
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    • v.34 no.3
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    • pp.185-192
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    • 2004
  • The objective of this study was to evaluate the effects of surfactant type and concentration upon dissolution rates of carbamazepine from an immediate-release tablet. The dissolution media used in this study were aqueous solutions containing 0.1-2% sodium lauryl sulfate, cetyltrimethylammonium bromide, or polysorbate 80. The solubility of carbamazepine in the dissolution media was determined at first. A dissolution study was then conducted by using the USP dissolution apparatus II (paddle method) with an agitation rate of 75 rpm. Aliquots of the dissolution media were taken at predetermined time intervals, and the amount of carbamazepine dissolved was measured spectrophotometrically at 285 nm. The dissolution data obtained were fitted into a biphasic exponential equation with four parameters. Excellent correlations were observed between the experimental data and the theoretical ones predicted by the equation. This equation permitted the calculation of $T_{50%}$ (the time required for dissolving 50% of carbamazepine) under various experimental conditions. Differentiation of the equation also led to the attainment of dissolution rates at dissolution time points. The addition of a surfactant to an aqueous solution led to increasing the solubility of carbamazepine by 3- to 12-folds, depending upon its type and concentration. This event also resulted in enhancing the magnitude of a sink condition during the dissolution study. As a result, the dissolution rate of carbamazepine was affected by the aqueous surfactant concentration in a proportional manner. Subsequently, $T_{50%}$ values declined rapidly, as the surfactant concentration increased. Such effects were observed in decreasing order of sodium lauryl sulfate, cetyltirmethylammonium bromide, and polysorbate 80. These results clearly demonstrated that it was possible to tailor a dissolution rate and $T_{50%}$ of carbamazepine by manipulating the type and concentration of a surfactant. Relevant information would be beneficial to setting up dissolution specifications for poorly water-soluble drug products.

Formulation and Characterization of Lipase Loaded Poly(D,L - lactide-co-glycolide) Nanoparticles (리파아제가 함입된 락타이드-글리콜라이드 공중합체 나노입자의 제조 및 특성)

  • Kim, Beom-Su;ZEROUAL, Y;Lee, Kang-Min
    • Polymer(Korea)
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    • v.31 no.1
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    • pp.20-24
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    • 2007
  • The preservation of biological activity of protein drugs in formulation is still a major challenge for successful drug delivery. Lipase was encapsulated in poly (D,L-lactide- co-glycolide) PLGA nano-particles using a w/o/w solvent evaporation technique. The lipase-containing PLGA/poly (vinyl alcohol) (PVA) nanoparticles were characterized with regard to morphology, size, size distribution, lipase-loading efficiency, in vitro lipase release, and stability of lipase activity. The size of nanoparticles increased as polymer concentration was increased. The size of particles was not significantly affected by the PVA concentration; on the other hand, the particle size distribution was the narrowest when 4% of PVA was used. In optimum conditions, we possessed nanoparticles that characterized 72.5% of encapsulation efficiency, $198.3{\pm}13.8 nm$ size diameter. During the initial burst phase, the in vitro release rate was very fast, reaching 83% within 12 days. Until days 6, enzyme activity increased as the amount of lipase released was increased.

Preparation and Characterization of Pioglitazone Loaded PLGA Nanospheres for the Treatment of Type 2 Diabetes (제2형 당뇨병 치료제인 Pioglitazone을 봉입하기 위한 PLGA 나노입자 제조 및 분석)

  • Woo, Hyun-Ju;Kim, Jin-Soo;Kim, Jun-Gi;Nurunnabi, Md.;Huh, Kang-Moo;Cho, Kwang-Jae;Lee, Yong-Kyu
    • Polymer(Korea)
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    • v.34 no.6
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    • pp.527-533
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    • 2010
  • The pioglitazone loaded poly(lactide-co-glycolide)(PLGA) nanospheres were prepared by emulsion-evaporation method and optimized for particle size and entrapment efficiency. The optimized particles were 125~170 nm in size with narrow size distribution and showed above 85% entrapment efficiency at 30% of pioglitazone loading when prepared with 3% w/v of poly(vinyl alcohol) (PVA) as a surfactant. These particulate carriers exhibited a controlled in vitro release of pioglitazone for 40 days at a nearly constant rate. The pioglitazone loaded PLGA nanospheres were not only effective to reduce the blood sugar level of diabetic rats but also non-toxic for the animal body, in particular for sensitive organs like kidney, liver, heart, lung and spleen. These results indicate that PLGA nanospheres have a great potential for oral delivery of pioglitazone.

Effect of an Excipient on the Formation of PLGA Particles Using Supercritical Fluid (초임계 유체를 이용한 PLGA 입자 제조에 첨가제가 미치는 영향)

  • Jung, In-Il;Haam, Seung-Joo;Lim, Gio-Bin;Ryu, Jong-Hoon
    • Polymer(Korea)
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    • v.36 no.1
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    • pp.1-8
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    • 2012
  • In this study, we employed hydroxypropyl-${\beta}$-cyclodextrin (HP-${\beta}$-CD) as an excipient to produce poly(lactic-$co$-glycolic acid) (PLGA) fine particles by a supercritical fluid process, called aerosol solvent extraction system (ASES), and investigated the effect of HP-${\beta}$-CD content on the morphology of the particles. The influence of HP-${\beta}$-CD on the drug release characteristics of paclitaxel-loaded PLGA particles was also evaluated. Fine particles were obtained when the HP-${\beta}$-CD content in PLGA/HP-${\beta}$-CD mixtures was greater than 40% and 30%, respectively, for PLGA(75:25) and PLGA(50:50), whereas a film-like precipitate was obtained for lower HP-${\beta}$-CD content. The release rate for paclitaxel loaded PLGA(75:25)/HP-${\beta}$-CD particles was found to increase with HP-${\beta}$-CD content.