• Title/Summary/Keyword: cosurfactants

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Development of Propofol-Ioaded Microemulsion Systems for Parenteral Delivery

  • Ryoo Hyun-Ki;Park Chun-Woong;Chi Sang-Cheol;Park Eun-Seok
    • Archives of Pharmacal Research
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    • v.28 no.12
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    • pp.1400-1404
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    • 2005
  • The aim of the present study was to develop the aqueous parenteral formulation containing propofol using o/w microemulsion systems. Propofol itself was chosen as the oil phase and its content was fixed to 1$\%$, w/w. Pseudoternary phase diagrams were constructed to obtain the concentration range of surfactant and cosurfacatnt and the optimum ratio between them for microemulsion formation. Consequently, the suitability of the chosen microemulsion system as a parenteral formulation was evaluated from the stability and hemolysis tests on that. Among the surfactants and cosurfactants screened, the mixture of Solutol HS 15-ethyl alcohol (5/1) showed the largest o/w mocroemulsion region in the phase diagram. When 1 $\%$ (w/w) of propofol was solubilized with 8$\%$ (w/w) of Solutol $HS^{circledR}$??? 15-ethyl alcohol (5/1), the average droplet size (150 nm) and the content of propofol in the systems were not significantly changed at 40$^{circ}C$ for 8 weeks. The hemolysis test showed that this formulation was nontoxic to red blood cells. In conclusion, propofol was successfully solubilized with the o/w microemulsion systems.

Preparation of Solid Dosage Form containing SMEDDS of Simvastatin by Microencapsulation (심바스타틴 자가유화약물전달시스템의 마이크로캡슐화를 통한 고형제제의 개발)

  • Kang, Bok-Ki;Yoon, Bok-Young;Seo, Kwang-Su;Jeung, Sang-Young;Kil, Hee-Joo;Khang, Gil-Son;Lee, Hai-Bang;Cho, Sun-Hang
    • Journal of Pharmaceutical Investigation
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    • v.33 no.2
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    • pp.121-127
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    • 2003
  • The objective of this study was to solidify the simvastatin self-microemulsifying drug delivery system (SMEDDS) and to improve the encapsulation efficiency of solidified alginate beads using sodium alginate. Typical simvastatin SMEDDS was composed of various oils, surfactants and cosurfactants. Also solidified-alginate beads was prepared by crosslinking liquid emulsion mixtures containing sodium alginate and other excipients (cetylpyridinum chloride (CP-Cl), hydroxypropyl methylcellulose, starch and so on). in $CaCl_2$ solution, it has been investigated that the drug release pattern and encapsulation efficiency were varied with the ratio of cationic lipid (CP-Cl). Solidified sodium alginate beads containing simvastatin SMEDDS were redispersed into media without re-aggregation. Oil droplet size of redispersed solidified-beads in media produced smaller than the initial size. The density of beads and drug loading amount were increased with increasing cationic lipid content. These systems have advantages of storage stability and predictability of drug release rate.

Enhanced Biodegradation of Lindane Using Oil-in-Water Bio-Microemulsion Stabilized by Biosurfactant Produced by a New Yeast Strain, Pseudozyma VITJzN01

  • Abdul Salam, Jaseetha;Das, Nilanjana
    • Journal of Microbiology and Biotechnology
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    • v.23 no.11
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    • pp.1598-1609
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    • 2013
  • Organochlorine pesticide residues continue to remain as a major environmental threat worldwide. Lindane is an organochlorine pesticide widely used as an acaricide in medicine and agriculture. In the present study, a new lindane-degrading yeast strain, Pseudozyma VITJzN01, was identified as a copious producer of glycolipid biosurfactant. The glycolipid structure and type were elucidated by FTIR, NMR spectroscopy, and GC-MS analysis. The surface activity and stability of the glycolipid was analyzed. The glycolipids, characterized as mannosylerythritol lipids (MELs), exhibited excellent surface active properties and the surface tension of water was reduced to 29 mN/m. The glycolipid was stable over a wide range of pH, temperature, and salinity, showing a very low CMC of 25 mg/l. Bio-microemulsion of olive oil-in-water (O/W) was prepared using the purified biosurfactant without addition of any synthetic cosurfactants, for lindane solubilization and enhanced degradation assay in liquid and soil slurry. The O/W bio-microemulsions enhanced the solubility of lindane up to 40-folds. Degradation of lindane (700 mg/l) by VITJzN01 in liquid medium amended with bio-microemulsions was found to be enhanced by 36% in 2 days, compared with degradation in 12 days in the absence of bio-microemulsions. Lindane-spiked soil slurry incubated with bio-microemulsions also showed 20-40% enhanced degradation compared with the treatment with glycolipids or yeast alone. This is the first report on lindane degradation by Pseudozyma sp., and application of bio-microemulsions for enhanced lindane degradation. MEL-stabilized bio-microemulsions can serve as a potential tool for enhanced remediation of diverse lindane-contaminated environments.

Improvement of Solubility of Atorvastatin Calcium Using Self-Microemulsion Drug Delivery System(SMEDDS) (자가미세유화를 통한 아토르바스타틴 칼슘의 난용성 개선)

  • Lee, Jun-Hee;Choi, Myoung-Kyu;Kim, Yun-Tae;Kim, Myoung-Jin;Oh, Jae-Min;Park, Jung-Soo;Mo, Jong-Hyun;Kim, Moon-Suk;Khang, Gil-Son;Lee, Hai-Bang
    • Journal of Pharmaceutical Investigation
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    • v.37 no.6
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    • pp.339-347
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    • 2007
  • SMEDDS is mixture of oils, surfactants, and cosurfactants, which are emulsified in aqueous media under conditions of gentle agitation and digestive motility that would be encountered in the gastro-intestinal(GI) tract. The main purpose of this work is to prepare self-microemulsifying drug delivery system(SMEDDS) for oral bioavailability enhancement of a poorly water soluble drug, atorvastatin calcium. Solubility of atorvastatin calcium was determined in various vehicles. Pseudo-ternary phase diagrams were constructed to identity the efficient self-emulsification region and particle size distributions of the resultant micro emulsions were determined using a laser diffraction sizer. Optimized formulations for in vitro dissolution and bioavailability assessment were $Capryol^{(R)}$ 90(50%), Tetraglycol(16%), and $Cremophor^{(R)}$ EL(32%). The release rate of atorvastatin from SMEDDS was significantly higher than the conventional tablet ($Lipitor^{(R)}$), 2-fold. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin calcium by the oral route.

Effect of Cosurfactant on Phase Equilibrium and Dynamic Behavior in Ternary Systems Containing Nonylphenol Ethoxylate Surfactant, Water and Hydrocarbon Oil (보조계면활성제가 노닐페놀 에톡실레이트 계면활성제, 탄화수소 오일, 물로 이루어진 삼성분계의 상평형 및 동적거동에 미치는 영향)

  • Lim, HeungKyoon;Lee, Seul;Mo, DaHee;Lim, JongChoo
    • Korean Chemical Engineering Research
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    • v.50 no.6
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    • pp.969-979
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    • 2012
  • In this study, the effects of cosurfactant on phase equilibrium and dynamic behavior were studied in systems containing nonylphenol ethoxylate (NP) surfactant solutions and nonpolar hydrocarbon oils. All the cosurfactants used during this study such as n-pentanol, n-octanol and n-decanol acted as a hydrophobic additive and the hydrophobic effect was found to increase with both increases in chain length and amount of addition of a cosurfactant. Dynamic behavior studies under hydrophilic conditions showed that the solubilization of hydrocarbon oil by NP micellar solution is controlled by an interface-controlled mechanism rather than a diffusion-controlled mechanism. Both spontaneous emulsification of water into oil phase and expansion of oil drop were observed under lipophilic conditions because of diffusion of surfactant and water into oil phase. Under conditions of a three phase region including a middle-phase microemulsion, both rapid solubilization and emulsification of oil into aqueous solutions were found mainly due to the existence of ultralow interfacial tension.

The Flow Properties and Stability of O/W Emulsion Composed of Various Mixed Nonionic Surfactants(II) The Phase Behavior and Flow Properties of O/W Emulsion According to the Addition of the Long Chain Alcohols (혼합 비이온계면활성제의 조성에 따른 O/W 에멀젼의 유동특성 및 안정성(II) 고급 알코올의 첨가에 따른 O/W 에멀젼의 상거동 및 유동특성)

  • Lee, Ho-Sik;Kim, Jum-Sik
    • Applied Chemistry for Engineering
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    • v.4 no.2
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    • pp.423-431
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    • 1993
  • Long chain alcohols, the mixtures of 1-hexadecanol/1-octadecanol, were used as cosurfactants for O/W emulsion prepared with glycerol monostearate/POE(100) monostearate mixed nonionic surfactants, and the phase behavior and flow properties of O/W emulsions were observed. The transition temperature of long chain alcohol was varied with the composition of 1-hexadecanol/1-octadecanol and had the lowest value when the mixed ratio of 1-hexadecanol/1-octadecanol was 2/1. The liquid crystalline phase was formed as the addition of long chain alcohol and the secondry droplet, the flocculate of the emulsion particles, was made, and thus the viscosity of the emulsion was increased. When the temperature of emulsion system was under the transition temperature of long chain alcohol, the mobility of hydrocarbon group of long chain alcohol was restricted, and thus gel structure was formed and the viscosity of the the O/W emulsion was increased, but along with the time, the liquid crystalline phase was disappeared and the viscosity of emulsion was decreased. Long chain alcohol/nonionic surfactants/water formed the liquid crystalline phase when the long chain alcohol was added above the saturation point of solution(2 wt% in this experoment), and the secondry droplet didn't formed when the long chain alcohol was added more than a certain amount (10 wt% in this experiment).

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Effect of Cosurfactant on Microemulsion Phase Behavior in NP7 Surfactant System (보조계면활성제가 NP7 계면활성제 시스템의 마이크로에멀젼 형성에 미치는 영향에 관한 연구)

  • Lim, HeungKyoon;Lee, Seul;Mo, DaHee;Lim, JongChoo
    • Applied Chemistry for Engineering
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    • v.22 no.4
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    • pp.416-422
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    • 2011
  • In this study, the effect of cosurfactant on the phase equilibrium and dynamic behavior was studied in systems containing NP7 nonionic surfactant solutions and nonpolar hydrocarbon oils. All cosurfactants used during this study such as n-pentanol, n-octanol and n-decanol acted as a hydrophobic additive and thus promoted the transition from an oil in water (O/W) microemulsion (${\mu}E$) in equilibrium with an excess oil phase to a three-phase region containing excess water, excess oil, and a middle-phase microemulsion and further to a water in oil (W/O) ${\mu}E$ in equilibrium with the excess water phase. The transition temperature was found to decrease with both increases in the chain length and amount of addition of a cosurfactant. Dynamic behavior studies under O/W ${\mu}E$ conditions showed that an oil drop size decreased with time due to the solubilization into micelles. On the other hand, both the spontaneous emulsification of water into the oil phase and the expansion of oil drop were observed under W/O ${\mu}E$ conditions because of the diffusion of surfactant and water into the oil phase. Under conditions of a three-phase region including a middle-phase ${\mu}E$, both the rapid solubilization and emulsification of the oil into aqueous solutions were found mainly due to the existence of ultra-low interfacial tension. Dynamic interfacial tension measurements have been found to be in a good agreement with dynamic behavior results.