• Title/Summary/Keyword: microemulsion stability

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Microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(S)-protopanaxadiol: in vitro and in vivo evaluation studies

  • Kim, Ki-Taek;Kim, Min-Hwan;Park, Ju-Hwan;Lee, Jae-Young;Cho, Hyun-Jong;Yoon, In-Soo;Kim, Dae-Duk
    • Journal of Ginseng Research
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    • v.42 no.4
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    • pp.512-523
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    • 2018
  • Background: 20(S)-Protopanaxadiol (20S-PPD) is a fully deglycosylated ginsenoside metabolite and has potent dermal antiaging activity. However, because of its low aqueous solubility and large molecular size, a suitable formulation strategy is required to improve its solubility and skin permeability, thereby enhancing its skin deposition. Thus, we optimized microemulsion (ME)-based hydrogel (MEH) formulations for the topical delivery of 20S-PPD. Methods: MEs and MEHs were formulated and evaluated for their particle size distribution, morphology, drug loading capacity, and stability. Then, the deposition profiles of the selected 20S-PPD-loaded MEH formulation were studied using a hairless mouse skin model and Strat-M membrane as an artificial skin model. Results: A Carbopol-based MEH system of 20S-PPD was successfully prepared with a mean droplet size of 110 nm and narrow size distribution. The formulation was stable for 56 d, and its viscosity was high enough for its topical application. It significantly enhanced the in vitro and in vivo skin deposition of 20S-PPD with no influence on its systemic absorption in hairless mice. Notably, it was found that the Strat-M membrane provided skin deposition data well correlated to those obtained from the in vitro and in vivo mouse skin studies on 20S-PPD (correlation coefficient $r^2=0.929-0.947$). Conclusion: The MEH formulation developed in this study could serve as an effective topical delivery system for poorly soluble ginsenosides and their deglycosylated metabolites, including 20S-PPD.

Preparation and Evaluation of Paclitaxel Nano-particle Delivery System for Parenteral Formulations (나노입자수송시스템을 이용한 파클리탁셀 정맥주사제의 제조 및 평가)

  • Jeon Il-Soon;Kim Jeong-Soo;Lee Gye-Won;Jee Ung-Kil
    • YAKHAK HOEJI
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    • v.49 no.4
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    • pp.268-274
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    • 2005
  • Paclitaxel is an effective antineoplastic agent against ovarian, colon and breast tumors. But there have been many difficulties to formulate this drug due to the extremely low aqueous solubility. Paclitaxel is currently formulated in a vehicle composed of Cremophor EL and absolute ethanol mixture which is $5\~20$ fold diluted in normal saline or $5\%$ dextrose solution before I.V. injection. However, this formulation has many problems such as allergic reactions and drug precipitation on aqueous dilution. To overcome these problems, we prepared the micelle and microemulsion systems for parenteral administration of paclitaxel by using glycofurol, $Soluto^{(R)}lHS$ 15 and oleic acid. Phase diagram, pH-rate stability, particle size distributions and pharmacokinetics of the systems were studied. Micelles and microemulsions formulated as nano-particle delivery system were physically and chemically stable. Therefore, these formulations might be the promising alternative candidate for the parenteral delivery of paclitaxel.

SMEDDS (Self-MicroEmulsifying Drug Delivery System) As An Intraurethral Prostaglandin E1 Delivery System

  • Lee, Sang-Kil;Jeon, Sang-Ok;Kang, Jae-Seon;Lee, Jae-Hwi;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.37 no.5
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    • pp.291-295
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    • 2007
  • Prostaglandin $E_1\;(PGE_1)$ was formulated as two self-microemulsifying drug delivery systems (SMEDDS) composed of Cremophor $EL^{(R)}$ or Cremophor $ELP^{(R)}$ as a surfactant, ethanol as a cosurfactant and Labrafac $CC^{(R)}$ as an oil to develop liquid preparation for the treatment of erectile dysfunction. In pseudo-ternary phase diagram, viscous gel area and microemulsion area were defined. In the measurement of viscosity, the viscosity of two formulations increased gradually upon the addition of water and it decreased from the water contents over 40%. With excessive water, the present systems formed a microemulsion spontaneously. From these results, rte could expect that the present liquid $PGE_1$ SMEDDS formulations might stay within the urethra in the viscous state when contacting the moisture of the urethra and can be easily eliminated by urination. In long-term stability study, we could select one formulation more stable at the shelf storage condition of $4^{\circ}C$.

Preparation and Evaluation of Microcapsule/Emulsions via the Electroatatic Interations of Polysaccharide and Protein (식물 유래 다당류/단백질 기반 마이크로캡슐/에멀젼 제조 및 평가)

  • Choi, Yu Ri;Lim, Hyung Jun;Lee, John Hwan;Oh, Seong Geun
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.41 no.4
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    • pp.295-302
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    • 2015
  • A novel microcapsule/emulsions for cosmetics was studied. Our present studies demonstrate that the biopolymer-stabilized microemulsion composed of polysaccharide and protein can encapsulate and stabilize remarkably coenzyme-Q10 (Q10). Polysaccharide and protein complex were incorporated in the microcapsule in order to reinforce the physical strength of the microspheres. We compared the long-term stability of the activity of Q10 in biopolymer-stabilized microemulsion. There was no noticeable negative effect on the activity of Q10. Optical microscope (OM) and transmission electron microscope (TEM) showed that microcapsules were spherical and had a smooth surface. Consequently, the polysaccharide/protein emulsion produced in this study may be beneficial in improving the emulsion stability and the protection capability of labile substances.

Preparation and Evaluation of Liquid Suppository Containing Prostaglandin $E_1-loaded$ Microemulsion (프로스타글란딘 $E_1$ 마이크로에멀젼이 함유된 액상좌제의 제조 및 평가)

  • Kim, Chung-Hwan;Lee, Sa-Won;Park, Kyung-Mi;Choi, Han-Gon;Kim, Chong-Kook
    • Journal of Pharmaceutical Investigation
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    • v.30 no.3
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    • pp.167-172
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    • 2000
  • The purpose of this study is to develop a transurethral liquid suppository containing prostaglandin $E_1\;(PGE_1)-loaded$ microemulsion, which undergoes a phase transition to gels at body temperature. The effects of oils, ethanol as solvent and HCl as pH-controlling agent on the physicochemical properties of liquid suppositories composed of poloxamer P 407, P 188 and carbopol was investigated. The stability of $PGE_1$ and release of $PGE_1$ from liquid suppository were evaluated. Oils such as Neobee and soybean oil significantly decreased the gelation temperature but increased the gel strength of liquid suppository due to their strongly binding with the components of liquid suppository base. However, ethanol slightly did the opposite. The pH of liquid suppositories hardly affected the gelation temperature and gel strength due to addition of very small HCl (0.005-0.01%). A liquid suppository [$PGE_1/P$ 407/P 188/carbopol/Neobee/ethanol/HCl (0.2/14/14/0.4/7/2/0.005%)], which had the gelation temperature $(34.2{\pm}0.6^{\circ}C)$ and gel strength $(31.35{\pm}4.37\;sec)$ suitable for liquid suppository system, was easily administered and not leak out from the body. About 60% of $PGE_1$ was released out within 2 h from this formulation. It was shown that the release of $PGE_1$ was proportional to the square root of time, indicating that $PGE_1$ might be released from the suppository by Fickian diffusion. It was stable at $4^{\circ}C$ for at least 2 months. The results suggest that transurethral liquid suppository containing prostaglandin $E_1-loaded$ microemulsion is thought to be a convenient, safe and effective dosage form for $PGE_1$. However, it should be further developed as a more convenient and stable dosage form for $PGE_1$.

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Preparation of AgCl/Ag3PO4/Diatomite Composite by Microemulsion Method for Rapid Photo-Degradation of Rhodamine B with Stability under Visible Light

  • Zhu, Hai-Tao;Ren, Qi-Fang;Jin, Zhen;Ding, Yi;Liu, Xin-Yu;Ni, Xi-Hui;Han, Meng-Li;Ma, Shi-Yu;Ye, Qing;Oh, Won-Chun
    • Korean Journal of Materials Research
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    • v.30 no.8
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    • pp.383-392
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    • 2020
  • In this paper, AgCl/Ag3PO4/diatomite photocatalyst is successfully synthesized by microemulsion method and anion in situ substitution method. X-ray diffraction (XRD), photoelectron spectroscopy (XPS), scanning electron microscopy (SEM), energy dispersive spectroscopy (EDS), transmission electron microscopy (TEM), and ultraviolet-visible spectroscopy (UV-Vis) are used to study the structural and physicochemical characteristics of the AgCl/Ag3PO4/diatomite composite. Using rhodamine B (RhB) as a simulated pollutant, the photocatalytic activity and stability of the AgCl/Ag3PO4/diatomite composite under visible light are evaluated. In the AgCl/Ag3PO4/diatomite visible light system, RhB is nearly 100 % degraded within 15 minutes. And, after five cycles of operation, the photocatalytic activity of AgCl/Ag3PO4/diatomite remains at 95 % of the original level, much higher than that of pure Ag3PO4 (40 %). In addition, the mechanism of enhanced catalytic performance is discussed. The high photocatalytic performance of AgCl/Ag3PO4/diatomite composites can be attributed to the synergistic effect of Ag3PO4, diatomite and AgCl nanoparticles. Free radical trapping experiments are used to show that holes and oxygen are the main active species. This material can quickly react with dye molecules adsorbed on the surface of diatomite to degrade RhB dye to CO2 and H2O. Even more remarkably, AgCl/Ag3PO4/diatomite can maintain above 95 % photo-degradation activity after five cycles.

Improved Immobilized Enzyme Systems Using Spherical Micro Silica Sol-Gel Enzyme Beads

  • Lee, Chang-Won;Yi, Song-Se;Kim, Ju-Han;Lee, Yoon-Sik;Kim, Byung-Gee
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.11 no.4
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    • pp.277-281
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    • 2006
  • Spherical micro silica sol-gel immobilized enzyme beads were prepared in an emulsion system using cyclohexanone and Triton-X 114. The beads were used for the in situ immobilization of transaminase, trypsin, and lipase. Immobilization during the sol to gel phase transition was investigated to determine the effect of the emulsifying solvents, surfactants, and mixing process on the formation of spherical micro sol-gel enzyme beads and their catalytic activity. The different combinations of sol-gel precursors affected both activity and the stability of the enzymes, which suggests that each enzyme has a unique preference for the silica gel matrix dependent upon the characteristics of the precursors. The resulting enzyme-entrapped micronsized beads were characterized and utilized for several enzyme reaction cycles. These results indicated improved stability compared to the conventional crushed form silica sol-gel immobilized enzyme systems.

Effect of Polymerization Conditions on the Size Development of Nano-sized PPy (나노 사이즈 폴리파이롤의 합성 조건에 따른 크기 변화)

  • Kim, Hyemin;Park, Chong-Rae
    • Proceedings of the Korean Fiber Society Conference
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    • 2003.10b
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    • pp.171-172
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    • 2003
  • Electrically conducting polymers have attracted a great deal of attention because of their unusual electronic Properties.1 One of them, polypyrrole has been widely studieddue to its high conductivity and good environmental stability. 2Especially polypyrrole nano-Particles and -fibers are interesting because of their unique properties and applications. Recently amorphous polypyrrole nano-particles were fabricated using microemulsion Polymerization at low temperature. (omitted)

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Process and characterization of an electrochromic film made of silica-polyaniline composite nanoparticle

  • Hwang, Tae-Jin;Lee, Heung-Yeol;Joo, Hyun-Jung;Yim, Tai-Hong
    • Proceedings of the Korean Institute of Surface Engineering Conference
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    • 2008.11a
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    • pp.6-7
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    • 2008
  • Composite nanoparticles of silica-polyaniline were synthesized and tested as an electrochromic material. For the optical application, the size of the nanoparticle was intended to be less than 100 nm in diameter. The synthesis was done by using a microemulsion synthesis method where the silica-polyaniline composite nanoparticle was obtained by dispersing two acidic aqueous phases containing aniline and polymerization agent, respectively. Microstructure analysis such as TEM and BET surface area measurement showed the possibility that polyaniline is incorporated in porous silica structure. The composite structure of the particle was proved to enhance chemical stability of the prepared electrochromic film.

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Synthesis and Characterization of Interfacial Properties of Glycerol Surfactant (글리세롤계 계면활성제 합성 및 계면 특성에 관한 연구)

  • Lim, JongChoo;Lee, Seul;Kim, ByeongJo;Lee, JongGi;Choi, KyuYong
    • Applied Chemistry for Engineering
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    • v.22 no.4
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    • pp.376-383
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    • 2011
  • The CMCs of LA and LA3 nonionic surfactants obtained from the reaction between glycidol and lauryl alcohol were found to be $0.97{\times}10^{-3}mol/L$ and $1.02{\times}10^{-3}mol/L$ respectively and the surface tensions for 1 wt% surfactant were 26.99 and 27.48 mN/m respectively. Dynamic surface tension measurements using a maximum bubble pressure tensiometer showed that the adsorption rate of surfactant molecules at the interface between the air and the surfactant solution was found to be relatively fast in both surfactant systems, presumably due to the high mobility of surfactant molecules. The contact angles of LA and LA3 nonionic surfactants were 27.8 and $20.9^{\circ}$ respectively and the dynamic interfacial tension measurement by a spinning drop tensiometer showed that interfacial tensions at equilibrium condition in both systems were almost the same. Also both surfactant systems reached equilibrium in 2~3 min. Both surfactant solutions showed high stability when evaluated by conductometric method and the LA nonionic surfactant system provided the higher foam stability than the LA3 nonionic surfactant system. The phase behavior experiments showed a lower phase or oil in water (O/W) microemulsion in equilibrium with an excess oil phase at all temperatures studied. No three-phase region was observed including a middle-phase microemulsion or a lamellar liquid crystalline phase.