• Title/Summary/Keyword: Poloxamer-407

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Effects of the Jinan Red Ginseng Extract Treatment on Poloxamer 407-induced Hyperlipidemia in Rabbits

  • Choi, Kyung-Min;Lee, Jeong Ho;Adam, Gareeballah Osman;Kim, Shang-Jin;Kang, Hyung-Sub;Yang, Yeong-Seok;Kim, Gi-Beum
    • Korean Journal of Plant Resources
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    • v.30 no.6
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    • pp.601-611
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    • 2017
  • Hyperlipidemia is an increase in one or more of the plasma lipids, including triglycerides, cholesterol. Ginseng has been used as a valuable tonic and for the treatment of various diseases. The objective of this study was to evaluate the effects of Jinan red ginseng (JRG) water extract on the blood and serum in rabbits with hyperlipidemia induced by poloxamer 407 when supplied in drinking water. JRG treatment was performed for 20 weeks. We evaluated the effects of the JRG treatment on diabetes through hematological and biochemical analysis before and after JRG treatment were performed. Our results indicate that LDL, total cholesterol, and triglycerides were significantly decreased compared prior JRG supply. CRE, BUN, CK and UA levels indicating renal functions are significantly reduced when compared to those prior to the JRG supply. In addition, AST, ALT, ALP, and LDH were significantly reduced indicating hepatoprotective effect. Blood electrolytes deteriorated in HL rabbits were improved when JRG supplied. In conclusion, Biochemical and hematological analysis demonstrate that the JRG is effective to alleviate the hyperlipidemia signs.

Size Distribution Characteristics and Entrapment Efficiency of Dried-Reconstituted Liposomes Containing Epidermal Growth Factor (상피세포성장인자를 함유한 동결건조-재분산 리포좀의 입도분포 및 봉입률)

  • Kim, Hee-Jun;Yu, Sung-Un;Choi, Young-Wook
    • YAKHAK HOEJI
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    • v.40 no.6
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    • pp.646-652
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    • 1996
  • Epidermal Growth Factor (EGF), discovered by Stanley Cohen in 1960, has a potential healing effect for wounds and bums. Considering wound care, in order to avoid physical stress at the wound surface and efficiently apply EGF, the need for viscous spraying solutions was essential. Viscous spraying solutions containing EGF were prepared by utilizing viscosity-building polymer, poloxamer 407, and by introducing liposome systems. On the other hand, EGF is purified on reverse HPLC gradient program with the mobile solvent of acetonitrile. It is necessary to observe liposomal EGF changes as the acetonitrile contents varied in order to introduce liposome systems at the step of EGF solution (at the time of EGF purifying). By evaluating the size distribution and entrapment efficiency of EGF liposome, it was possible to detemine the limit contents of acetonitrile and establish the optimal conditions for solution formulations. It has been revealed that, as the acetonitrile content increases, mean diameter of EGF liposomes increased and the width of size distribution tends to decrease. The limit contents of acetonitrile were 10%, since there was little difference to the acetonitrile free liposomes.

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Preparation and Characterization of Solid Dispersions of Eprosartan Using Spray Drying Method (분무 건조 방식으로 제조한 에프로살탄 고체분산체 제조 및 특성 분석)

  • Hwang, Jun Seok;Kim, So Hee;Cho, Sun Hang;Huh, Kang Moo
    • Polymer(Korea)
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    • v.37 no.4
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    • pp.442-448
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    • 2013
  • In this study, we developed and optimized hydrophilic polymer-based solid dispersion formulations (SDs) using a spray drying method for improving the aqueous solubility of eprosartan, one of poorly soluble drugs that has been broadly used for the treatment of high blood pressure. Hydroxylpropylcellulose (HPC) and poly(vinyl pyrrolidone) (PVP) were used as hydrophilic polymer matrices and poloxamer 407 (P407) added as a polymeric surfactant. Various kinds of solid dispersions with different drug/polymer compositions were prepared and their physico-chemical properties were compared. As the polymer content increased, the drug crystallinity in the SDs significantly decreased and the dissolution properties were enhanced. The PVP based SDs were observed to have relatively reduced crystallinity and an enhanced dissolution rate than HPC-based SDs, due to better miscibility between drug and polymer matrix. For PVP based SDs, the drug crystallinity almost disappeared and the dissolution properties significantly increased by more than 3~7 times.

Effect of Additives on the Physicochemical Properties of Acetaminophen Liquid Suppository (아세트아미노펜 액상좌제의 물리화학적 특성에 미치는 첨가제의 영향)

  • Choi, Han-Gon;Jung, Jae-Hee;Ryu, Jei-Man;Lee, Mi-Kyung;Kim, In-Sook;Lee, Beom-Jin;Kim, Chong-Kook
    • YAKHAK HOEJI
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    • v.42 no.3
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    • pp.290-295
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    • 1998
  • To optimize the formulation of acetaminophen liquid suppository, the effect of additives on the physicochemical properties of liquid suppository base was investigated. The physi cochemical properties of P 407/P 188 (15/15%) (abbreviated in 15/15) and P 407/P l88 (15/20%) (abbreviated in 15/20) were measured after the addition of following additives; 2.5% acetaminophen as an active ingredient, vehicle components (5% ethanol, 5% propylene glycol, 5% glycerin), preservatives (0.1% sodium benzoate, 0,1% methylparahydroxybenzoate, 0.1% propylparahydroxybenzoate) and 1% of sodium chloride as an ionic strength controlling agent. Poloxamer gel was prepared with three different buffer solutions (pH 1.2, 4.0 and 6.8) and the physicochemical properties, gelation temperature, gel strength and bioadhesive force, were determined. In the results, the effect of additives on the physicochemical properties was dependent on their bonding capacities including hydrogen bonding and cross-linking bonding. Because the hydrogen-bonding capacities of acetaminophen, ethanol and propylene glycol were smaller than that of poloxamer, the binding force of poloxamer gel became weak by their putting in between poloxamer gel. Therefore, the gelation temperature (15/15, $35.7^{\circ}C$ vs 37.0, 39.4 $38.2^{\circ}C$; 15/20, $29.2^{\circ}C$ vs 31.2, 32.0, $30.3^{\circ}C$) increased, and gel strength (15/15, 4.03 see vs 2.72, 2.08, 3.12sec; 15/20, 300g vs 50, 50, 200g) and bioadhesive force (15/15, $6.8{\times}10^2\;dyne/cm^2$ vs 3.2, 6.0, $6.0{\times}10^2\;dyne/cm^2$; 15/20, $97.3{\times}10^2\;dyne/cm^2$ vs 11.1, 89.5, $92.0{\times}10^2\;dyne/cm^2$) decreased. Furthermore, the binding force of poloxamer gel became strong due to the hydrogen-bonding capacities of glycerin and the cross-liking bonding of sodium salt. Then, the gelation temperature (15/15, 35.0, $32.1^{\circ}C$; 15/20, 26.0, $21.0^{\circ}C$) decreased, and gel strength (15/15, 6.51 see, 300g; 15/20, 500, 650g) and bioadhesive force (15/15, 7.2, $81.6{\times}10^2\;dyne/cm^2$; 15/20, 112.3, $309.2{\times}10^2\;dyne/cm^2$) increased. The effect of pH on the physicochemical properties of poloxamer gel was dependent on the ingredients with which the buffer solutions were prepared. Poloxamer gels prepared with pH 1.2 and 4.0 buffer solutions had the increasing gelation temperature (15/15, 37.5, $38.1^{\circ}C$; 15/20, 33.1, $34.0^{\circ}C$) and the decreasing gel strength (15/15, 2.98, 3.81sec; 15/20, 200, 200g) and bioadhesive force (15/15, $7.0{\times}10^2dyne/cm^2$; 15/20, $74.0{\sim}88.1{\times}10^2dyne/cm^2$) owing to HCl. Poloxamer gel prepared with pH 6.8 buffer solutions had the decreasing gelation temperature (15/15, $27.2^{\circ}C$; 15/20, $22.3^{\circ}C$) and the increasing gel strength (15/15, 400g; 15/20, 550g) and bioadhesive force (15/15, $207.0{\times}10^2dyne/cm^2$; 15/20, $215.0{\times}10^2dyne/cm^2$) due to the cross-linking bonding of $NaH_2PO_4\;and\;K_2HPO_4$.

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Effects of Bangpoongtongsungsan on Adipose Tissue and Hyperlipidemia of 3T3-L1 Induced Rats (3T3-L1 cell에서 방풍통성산의 지방세포 분화 억제 효과 연구)

  • Lee, Jin-Yong;Kim, Deog-Gon;Lee, Kyung-Tae;Cha, Min-Kyung
    • The Journal of Pediatrics of Korean Medicine
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    • v.20 no.2
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    • pp.177-196
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    • 2006
  • Objective : This experimental study was designed to determine the effects of BPT on obesity in vivo and in vitro. Methods : in vitro, BPTn extracts of various concentration(50, 100, 200 ${\mu}g/m{\ell}$) were added in 3T3-L1 cell. Adipocyte differentiation was measured by Oil Red O staining and Morphological examination. The expression of $C/EBP{\alpha}$ and $PPAR{\gamma}$ receptor was measured by western blot assay and RT-PCR in vivo, Rats were orally administered BPT daily for consecutive four weeks before poloxamer-407 induced hyperlipidemic state. The rats were sacrificed 24 hrs later for poloxamer-407 treated and then serum triglyceride, total cholesterol were measured ; Rats were orally administered BPT daily for consecutive four weeks before triton WR-1339 induced hyperlipidemic state. The rats were sacrificed 40 hrs later for triton WR-1339 treated and then serum triglyceride, total cholesterol were measured ; Rats with obesity were induced by the high fat-diet for six weeks and then serum triglyceride, total cholesterol, LDL-cholesterol, triglyceride, HDL-cholesterol, hydroxy radical, superoxide dismuatse activity were measured. Results : In vitro, The 3T3-L1 cells' differentiation was significantly decreased by BPT. The expression of $C/EBP{\alpha}$ and $C/EBP{\beta}$ was decreased by BPT. In vivo, BPT significantly reduced serum triglyceride, total cholesterol contents in poloxamer-407 treated rat. BPT significantly reduced serum triglyceride contents in Triton WR-1339 treated rat. Total cholesterol also reduced but did not show a significant change. BPT significantly reduced body weight gain of rat and adipose tissue mass of rats and serum triglyceride, LDL-cholesterol contents and significantly increased HDL-cholesterol, HTR(HDL-cholesterol/Total-cholesterol) in rats with obesity induced by the high fat-diet. BPT reduced blood lipid peroxide, hydroxy radical and increased superoxide dismuatse(SOD) activity.

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Study on Skin Permeation of Tocopheryl Acetate Using Swollen Micelle (Swollen Micelle을 이용한 Tocopheryl Acetate 의 피부흡수 연구)

  • Su-Bin Son;Kyung-Sup Yoon
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.49 no.1
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    • pp.17-27
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    • 2023
  • A study was performed to increase skin permeation of tocopheryl acetate, an oil-soluble component among tocopheryl acetate, salicylic acid, and niacinamide, which are the active ingredients of the anti-hair loss toner. As a method of transparently solubilizing tocopheryl acetate while containing salicyl acid and niacinamide, we used a swollen micelle structure that increased the size of the micelle formed by the aggregation of surfactants. The prepared swollen micelle solution contains three kinds of active ingredients, and poloxamer 407 and octyldodeceth-16 were used as surfactants to increase transparent properties and stability. In addition, isostearic acid was used as a co-surfactant to increase the size of micelles. To evaluate the physical properties of the prepared swollen micelles, turbidity at room temperature (25 ℃) was measured. The Franz diffusion cell method was used to evaluate the skin permeation rate of tocopheryl acetate among the hair-loss prevention components contained in swollen micelles. After 24 h, tocopheryl acetate showed a 6-fold improvement in skin permeation compared to the control group. Therefore, it can be seen that the swollen micelles developed in this study can be applied to hair-loss prevention products or solubilized formulations of various functional cosmetics.

Formulation Design and Evaluation of Ketorolac Tromethamine Hydrogel for Transdermal Delivery System (경피흡수를 위한 케토롤락 하이드로겔의 제제설계 및 평가)

  • Cho, In-Sook;Lee, Gye-Won;Lee, Jong-Hwa;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.33 no.1
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    • pp.21-28
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    • 2003
  • Ketorolac tromethamine(KT) is a nonsteroidal agent with potent analgesic and moderate anti-inflammatory activity. The lipid-water partition coefficient of KT was evaluated and KT gel was formulated as a gel containing different pH, different concentrations of polymer (poloxamer 407, carbopol 941), propylene glycol, ethanol and various enhancers. The resulting KT gels were evaluated with respect to their viscosity, in vitro drug permeation rate through hairless mouse skin and stability. In n-octanol and chloroform, the lipid-water partition coefficient of KT was the highest at pH 4 phosphate buffer. The apparent viscosity of KT gel increased with an increase in gel pH, polymer and enhancer concentration. But the apparent viscosity of KT gel decreased with an increase in ethanol concentration. The permeation rate of KT through hairless mouse skin from gels different pH was maximum at pH 4 which is close to KT $pK_{a}$ 3.54. The permeation rate decreased with an increase in polymer, propylene glycol concentration. But the permeation rate increased with an increase in ethanol. The increase of drug concentration from 1 to 3% induced linear increase in permeation rate. The best enhancer was the combination of $Labrasol^{\circledR},\;Transcutol^{\circledR}$, oleic acid and l-menthol. In the accelerated stability test(25, 40 and $50{\circ}C$), pH 5 gel was most stable and pH 4 gel was most unstable for 90 days.

Anti-hyperlipidemic Effect of Shiitake Mushroom Extract in Hyperlipidemic Rats Induced by Poloxamer-407 (고지혈증 동물모델에서 표고버섯 추출물의 항고지혈증 효과)

  • Kim, Gye Yeop;Jung, Hun Woo;Kim, Eun Jung
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.27 no.4
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    • pp.409-415
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    • 2013
  • We attempted to determine the action target of Shiitake mushroom extract with a known anti-hyperlipidemic effect in poloxamer(P) 407-induced hyperlipidemia model. We investigated the anti-hyperlipidemic effects of the water extract from Shiitake mushroom on the progress of high fat diet for 4 weeks. Experimental rats were divided into 5 different experimental groups including an normal group (normal diet; n=10), control group (hyperlipidemia; n=10), Experimental group I (hyperlipidemic rats treated with Shiitake mushroom extract (100 mg/kg, PO), n=10), Experimental group II (hyperlipidemic rats treated with Shiitake mushroom extract (300 mg/kg, PO), n=10), and Experimental group III (hyperlipidemic rats treated with Shiitake mushroom extract (500 mg/kg, PO), n=10). It is to analysis changes in body weight, visceral fat weight, blood lipid profiles, HMG-CoA reductase and histological findings. Body weight and epididymal fat weight was not significantly change in experimental groups (p>0.05). The level of total cholesterol, TG, arthrogenic index, and HMG-CoA reductase were significantly lower in experimental groups than control group (p<0.05). These results suggested that the Shiitake mushroom extract administration may act by inhibitory the release of cholesterol related factors and HMG-CoA from the hepatocyte without liver and kidney cell damage in hyperlipidemia rats.

Formulation Design and Evaluation of Ursolic Acid Microemulsion Delivery System for Topical Formulation (마이크로에멀젼을 이용한 우르솔릭산 피부 적용제제의 설계 및 평가)

  • Park, Jong-Hee;Kyong, Kee-Yeol;Lee, Gye-Won;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.35 no.4
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    • pp.233-241
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    • 2005
  • Ursolic acid (UA), a bioactive triterpene acid, has been known to increase collagen content in human skin in addition to other actions such as anti-inflammatory, skin-tumor prevention and anti-invasion. However, it is poorly soluble in water. Therefore, we firstly prepared microemulsion system with benzyl alcohol, ethanol and Cremophor EL, RH 40 and Brij 35 as surfactant in order to increase solubility of UA and then prepared microemulsion was dispersed in o/w cream base for the topical delivery of UA in an effort to improve anti-wrinkle effect. The pseudo-ternary phase diagrams were developed and various microemulsion formulations were prepared using benzyl alcohol as an oil, Cremophor EL, RH 40 and Brij 35 as a surfactant. The droplet size of microemulsions was characterized by dynamic light scattering. The accumulation of VA in the skin from topical cream was evaluated in vitro using hairless mouse skins. The mean droplet size was $26.8{\pm}6.6$ nm for microemulsions II with Cremophor EL. All UA creams showed pseudoplastic flow and hysterisis loop in their rheogram, depending on the type of materials added in topical creams. The in vitro accumulation data demonstrated the UA topical cream prepared with the combination of Poloxamer 407 and Xanthan gum as a copolymer showed higher accumulation percentage than those prepared with either Poloxamer 407 or Xanthan gum. These results suggest that UA topical cream using microemulsion systems may be promising for the topical delivery of UA.

Anti-obestic Effects of Bangpoongtongsungcankamibang(BTSK) in 3%3-L1 preadipocyte cells and the Lipid Metabolism of Obesity induced Rats (방풍통성산가미방(防風通聖散加味方)이 비만유도(肥滿誘導) 백풍(白嵐)와 지방세포(脂肪細胞) 분화(分化)에 미치는 영향(影響))

  • Lee, Jin-Yong;Kim, Deog-Gon;Ahn, Hong-Sik
    • The Journal of Pediatrics of Korean Medicine
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    • v.20 no.1
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    • pp.219-240
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    • 2006
  • Objective : This experimental study was designed to determine the anti-obestic effects of Bangpoongtongsungcankamibang(BTSK). Method : In vitro, BTSK extracts of various concentration (50,100, 200 $200{\mu}g/ml$)were added examination. The protein and mRNA expression of $C/EBP{\alpha}$ and $PPAR{\gamma}$ receptor was measured by western blot assay and RT-PCR. In vivo, BTSK extracts of various concentration (100, $200{\mu}g/ml$) were orally administered to induced hyperlipidemic rats by poloxamer-407 for consecutive four weeks and serum triglyceride, total cholesterol were measured. This method applied to induced hyperlipidemic rats by triton WR-1339, too. Obesity induced rats by the high fat-diet for six weeks were orally administered BTSK extracts of various concentration (100, $200{\mu}g/ml$) and serum triglyceride, total cholesterol, LDL-cholesterol, triglyceride, LDL-cholesterol, triglyceride, HDL-cholesterol, hydroxy radical, superoxide dismuatse activity were measured. Results : I. In vitro 1. The 3T3-L1 cells' differentiation was significantly decreased by BTSK. 2. expression of $C/EBP{\alpha}$ and $PPAR{\gamma}$ was was significantly decreased by BTSK. II. In vitro 1. BTSK significantly reduced serum triglyceride, total cholesterol, contents in poloxamer-407 treated rat. 2. BTSK significantly reduced serum triglyceride, contents in Triton WR-1339 treated rat. But Total cholesterol did not show a significant change. 3. BTSK significantly reduced body weight gain of rat and adipose tissue mass of rats and serum triglyceride, LDL-cholesterol, contents and significantly increased HDL-cholesterol, HTR(HDL-cholesterol/Total-cholesterol) in rats with obesity induced by the high fat-diet. 4. BTSK reduced blood lipid peroxide, hydroxy radical and increased superoxied dismuatse(SOD) activity.

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