• Title/Summary/Keyword: Formation of micelles

Search Result 66, Processing Time 0.025 seconds

Effect of Polysorbate 80 and Benzyl Alcohol on the Solubility of Amiodarone Hydrochloride

  • LEONTIEV, Viktor;LAZOVSKAYA, Olesya
    • The Korean Journal of Food & Health Convergence
    • /
    • v.5 no.4
    • /
    • pp.13-17
    • /
    • 2019
  • Amiodarone hydrochloride is an antiarrhythmic agent which has low aqueous solubility and presents bioavailability problem. These properties are a challenge for the pharmaceutical industry. Inclusion of lipophilic compound in the hydrophobic core of micelles, i.e. self-assembled structures based on surfactants in aqueous solution, is one way of increasing the solubility. Intravenous formulation of amiodarone hydrochloride with polysorbate 80 as a detergent and benzyl alcohol as a co-solvent is used in medical practice. This paper aimed to study the effect of polysorbate 80 and benzyl alcohol on the water solubility of amiodarone hydrochloride. Formation of mixed micelles consisting of nonionic surfactant polysorbate 80 and cationic amiodarone with chloride counterion was investigated by fluorescence spectroscopy. Benzyl alcohol was found to decrease the stability of the mixed micelles and lead to crystallization of amiodarone hydrochloride. The greatest amounts of crystals formed at 4℃ for 30 days in the model drug solutions with polysorbate 80 concentrations of 100.1 mg/mL and 97.9 mg/mL. A change of the polysorbate 80 concentration and avoidance the use of benzyl alcohol are recommended to improve the stability of the parenteral dosage form. These results can open new perspectives in the optimization of amiodarone intravenous formulations.

Absorption Spectroscopical Studies on the dye-surfactant interactions (색소-계면활성제 상호작용에 관한 흡수분장학적 연구)

  • Park, No-Youn;Lee, Hong;Pae, Huyn-Ock
    • Journal of the Society of Cosmetic Scientists of Korea
    • /
    • v.17 no.1
    • /
    • pp.18-28
    • /
    • 1991
  • Spectral behaviors of cationic dye, crystal violet(CV), in aqueous solution and with varying concentrations of Triton X-100(TX-100), sodium dodecylsulfate (SDS) and cetyl trimethyl amonium bromide(CTAB) were studied. The characteristic changes of the absorption spectra observed in the dye-SDS interacting systems with the SDS concentration are analyzed. The behaviors of both a- and J-bands of the each componet dye suggest that the following four sequential steps are occurring : the formation of dye-SDS complex, the stacking of the dye molecules arising from the association of the dye-SDS complex, breaking of the dye stacking due to the formation of micelles, redistribution of the dye molecules in the surface of micelles at high SDS concentration.

  • PDF

Effect of Surfactant Micelles on Lipid Oxidation in Oil-in-water Emulsion Containing Soybean Oil (Surfactant micelle이 수중유적형 유화계내의 대두유 산화에 미치는 영향)

  • Cho, Young-Je;Chun, Sung-Sook;Decker, Eric A.
    • Korean Journal of Food Science and Technology
    • /
    • v.34 no.5
    • /
    • pp.770-774
    • /
    • 2002
  • Effect of surfactant micelles on lipid oxidation was determined in soybean oil-in-water (O/W) emulsions. The concentration of ferric irons to continuous phase in the O/W emulsions was measured as a function of various Brij type and concentrations. The concentration of ferric iron in the continuous phase increased with increasing surfactant micelles concentration $(0.5{\sim}2.0%)$ and storage time $(1{\sim}7\;days)$. At pH 3.0, the concentration of continuous phase iron was higher than at pH 7.0. Lipid oxidation rates, as determined by the formation of lipid hydroperoxides and headspace hexanal, in the O/W emulsions containing ferric iron decreased with increasing surfactant micelle concentration $(0.5{\sim}2.0%)$. These results indicate that surfactant micelles concentration could alter the physical location and prooxidant activity of iron in soybean O/W emulsions.

Principles of Physiology of Lipid Digestion

  • Bauer, E.;Jakob, S.;Mosenthin, R.
    • Asian-Australasian Journal of Animal Sciences
    • /
    • v.18 no.2
    • /
    • pp.282-295
    • /
    • 2005
  • The processing of dietary lipids can be distinguished in several sequential steps, including their emulsification, hydrolysis and micellization, before they are absorbed by the enterocytes. Emulsification of lipids starts in the stomach and is mediated by physical forces and favoured by the partial lipolysis of the dietary lipids due to the activity of gastric lipase. The process of lipid digestion continues in the duodenum where pancreatic triacylglycerol lipase (PTL) releases 50 to 70% of dietary fatty acids. Bile salts at low concentrations stimulate PTL activity, but higher concentrations inhibit PTL activity. Pancreatic triacylglycerol lipase activity is regulated by colipase, that interacts with bile salts and PTL and can release bile salt mediated PTL inhibition. Without colipase, PTL is unable to hydrolyse fatty acids from dietary triacylglycerols, resulting in fat malabsorption with severe consequences on bioavailability of dietary lipids and fat-soluble vitamins. Furthermore, carboxyl ester lipase, a pancreatic enzyme that is bile salt-stimulated and displays wide substrate reactivities, is involved in lipid digestion. The products of lipolysis are removed from the water-oil interface by incorporation into mixed micelles that are formed spontaneously by the interaction of bile salts. Monoacylglycerols and phospholipids enhance the ability of bile salts to form mixed micelles. Formation of mixed micelles is necessary to move the non-polar lipids across the unstirred water layer adjacent to the mucosal cells, thereby facilitating absorption.

Thermosensitive Block Copolymers Consisting of Poly(N-isopropylacrylamide) and Star Shape Oligo(ethylene oxide)

  • Lee, Seung-Cheol;Chang, Ji-Young
    • Bulletin of the Korean Chemical Society
    • /
    • v.30 no.7
    • /
    • pp.1521-1525
    • /
    • 2009
  • Thermosensitive block copolymers of ethylene oxide and N-isopropylacrylamide (NIPAM) were synthesized. A five armed star shape oligo(ethylene oxide) initiator with a cyclotriphosphazene core was prepared and used for the atom transfer radical polymerization (ATRP) of NIPAM. The lower critical solution temperatures (LCSTs) of the copolymers were 36 to 46 ${^{\circ}C}$, higher than that of PNIPAM (32 ${^{\circ}C}$), depending on their molecular weights. The copolymers were soluble in water below the LCSTs but formed micelles above the LCSTs. The thermosensitive micellization behaviors of the polymers were investigated by fluorescence spectroscopy. With increasing the temperature of an aqueous solution of P2 and pyrene above the LCST, the peak of 333 nm red-shifted to appear around 339 nm and its intensity increased significantly, indicating the micelle formation. The transfer of pyrene into the micelles was also confirmed by a confocal laser scanning microscope. The fluorescence image obtained from P2 in an aqueous pyrene solution exhibited a green emission resulting from the pyrene transferred into the micelles. Salt effects on the solubility of the copolymers in an aqueous solution were investigated. The LCST of P2 decreased sharply as the concentration of sodium chloride increased, while decreased slowly with potassium chloride.

The Solubilization Behavior of DOPE-Immunoliposomes with Immunoglobulin G(IgG) by Added Bile Salts (Immunoglobulin G(IgG)를 함유한 DOPE 리포솜의 제조와 담즙산염에 의한 용해 특성)

  • Lee, Eun-Ok;Kim, Jin-Gu;Kim, Jong-Duk
    • Journal of Pharmaceutical Investigation
    • /
    • v.20 no.3
    • /
    • pp.135-144
    • /
    • 1990
  • The effects of bile salts (BS) on the stability of dioleoylphosphatidylethanolamine (DOPE) liposomes were investigated, observing apparent absorbance of vacant liposomes and calcein release from entrapped liposomes. Unilamellar liposomes were prepared by using a small quantity of palmitoly-immunoglobulin G(IgG) ($2.5{\times}10^{-4}$ mo1/lipid mol) to stabilize the bilayer phase of the unsaturated DOPE which by itself does not form stable liposomes. The destabilization of PE immunoliposomes by papain, clearly demonstrates that the IgG is essential for stabilization of PE bilayer. Approximately 4% of the entrapped calcein was released from the PE liposomes after 1 hr from liposome formation. Calcein release and absorbance of liposomes depended on the BS/lipid ratio because of the solubilization of lipid molecule in bilayer and the formation of mixed micelles. At very low BS concentrations, the incorporation of BS induced BS/lipid aggregates in the outer vesicles monolayer, while high BS concentrations, mixed micelles were formed. Chelate and its conjugates as $3{\alpha},\;7{\alpha},\;12{\alpha}-trihydroxy$ BS induce the concentration of the $3{\alpha}$, $12{\alpha}-dihydroxy$ BS at half-maximal solubilization of immunoliposomes to approximately 2.5-, or 5-fold. Conjugation of BS with glycine or taurine slightly enhanced their capacities to perturb membranes.

  • PDF

Electrochemical Studies on the Methylviologen-Sodium Dodecyl Sulfate Solution in the Presence of $MgCl_2$ (염화마그네슘 존재하의 메틸비올로겐-도데실황산나트륨 용액의 전기화학적 연구)

  • Ko, Young Chun;Chung, Keun Ho
    • Analytical Science and Technology
    • /
    • v.11 no.3
    • /
    • pp.151-155
    • /
    • 1998
  • Electrochemical behaviours on 1.0 mM methylviologen ($MV^{2+}$) in 100 mM NaCl+27 mM $MgCl_2$ solution, without and with sodium dodecyl sulfate (SDS), were studied. The intersection of two lines on ${\Delta}E_p$ (the difference between the anodic, $E_{pa}$, and the cathodic, $E_{pc}$, peak potentials) of the first and second redox waves vs. -log[SDS] plot was determined as a critical micelle concentration (CMC). When $Mg^{2+}$ was added, the effective access of $MV{\cdot}^+$ to the glassy carbon electrode surface became possible and the formation of micelles was retarded.

  • PDF

Absorption and Fluorescence Spectroscopic Behavior of Thionine in the Presence of Sodium Dodecyl Sulfate (Sodium Dodecyl Sulfate 존재하에서 Thionine의 흡수 및 형광분광학적 성질)

  • Seong Gwan Kang;Chong Hoe Park;Minjoong Yoon
    • Journal of the Korean Chemical Society
    • /
    • v.38 no.12
    • /
    • pp.857-863
    • /
    • 1994
  • The absorption and fluorescence spectroscopic studies on the interaction between thionine (TH) and sodium dodecyl sulfate (SDS) have been carried out. The absorption and fluorescence spectral changes of TH with the changes of concentration of SDS are interpreted in terms of i) the aggregation of TH-SDS complex, ii) the stacking process of dye molecules by the association of the TH-SDS complex, iii) breakdown of the stacking due to the formation of dye-rich induced micelles, iv) redistribution of dye molecules in the surface of SDS micelles.

  • PDF

Revesible Switching between Nematic Gel and Isotriopic Fluid Triggered by External Stimuli in Aqueous Self-Assembly of Supramolecular Nanocylinders

  • Ryu, Ja-Hyoung;Lee, Myong-Soo
    • Proceedings of the Polymer Society of Korea Conference
    • /
    • 2006.10a
    • /
    • pp.308-308
    • /
    • 2006
  • We have demonstrated that the cylindrical micelles self-assembled from coil-rod-coil molecules can be interconnected by addition of a small amount of rod-coil-rod molecule as a bridging agent. Subsequently, these dynamic interconnections lead to stiff bundles composed of cylindrical micelles that are responsible for the formation of a reversible nematic gel. The results described here represent a significant example that dynamic bridging of supramolecular cylinders in aqueous solution can provide a useful strategy to construct one-dimensional nematic structure with three dimensional elastic properties.

  • PDF

Self-assembled Micelle-based Fluorescence Sensor for Extremely Acidic pH Range (강산성 용액의 pH를 측정할 수 있는 미셀기반의 형광센서 개발)

  • Lee, Jeongmoo;Lee, Seoung Ho
    • Journal of Environmental Science International
    • /
    • v.29 no.8
    • /
    • pp.801-808
    • /
    • 2020
  • In this study, an effective fluorescence pH sensor based on conjugated polyelectrolyte micelles (CPMs) was devised for detecting extremely acidic conditions. An amphiphilic coumarin derivative (CC12-N), a building block, was prepared, into which an ionizable amino group, aryl amine, was incorporated as a potential hydrophilic moiety. This monomer displays self-assembled micelle formation in extremely acidic pH ranges, giving a hydrophobic π-extended conjugated system at the inner part and hydrophilic functionality at the periphery, resulting in efficient fluorescence intensity enhancement. This new micelle-based fluorescence provides an efficient sensing platform for detecting very low pH values in the presence of competing substances.