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Desde a primeira publicação a respeito, em 2001, a aplicação de injeções lipolíticas para gordura localizada tornou-se um procedimento amplamente utilizado na clínica. Consiste de múltiplas injeções subcutâneas de compostos lipolíticos, que podem ter diversos mecanismos de ação. O fármaco mais utilizado atualmente, o desoxicolato de sódio, foi descoberto por acaso, em uma associação com fosfatidilcolina em que sua única função era de veículo da fórmula. Conforme estudos foram sendo realizados, concluiu-se que a ação no tecido era devido ao desoxicolato, um sal biliar que emulsiona os lipídios da membrana celular, resultando em lise do adipócito e consequente necrose do tecido adiposo. Seus principais efeitos adversos, muito frequentemente relatados, incluem dor intensa, edema e formação de nódulos fibrosos nos pontos aplicados. Em decorrência de falhas na aplicação, alguns efeitos adversos mais graves podem ocorrer, como injúria do nervo facial e infecções persistentes. Apesar destes, a utilização de desoxicolato de sódio na camada subcutânea apresenta resultados muito positivos, como publicado em diversos ensaios clínicos, inclusive com relação à satisfação do paciente perante o desfecho final, sendo, portanto, uma boa escolha de técnica para contorno corporal e diminuição de depósitos de gordura localizados. (AU)
Since the first paper, in 2001, injection lipolysis for localized fat deposits became a widely used procedure in the clinics. It consists basically of multiple subcutaneous injections of lipolytic compounds, with many different mechanisms of action. The most used drug nowadays is sodium deoxycholate, initially thought to be only the solubilizing vehicle in the phosphatidilcholine formula. As studies were performed, it was concluded that the changes seen in the tissue was due to sodium deoxycholate, a biliary salt which emulsifies membrane lipids, resulting in adipocyte lysis and consequent adipose tissue necrosis. Its main adverse events include pain, oedema and fibrous nodules. Due to poor technique, more serious adverse events may happen, such as nerve injury or persistent infection by mycobacterium. In spite of these, the use of sodium deoxycholate presents great results, as published in many clinical trials, including patient's satisfaction at the end of the treatment, which is of much value in the aesthetics field. Therefore, mesotherapy using sodium deoxycholate is a good choice for body contouring and localized fat deposits. (AU)
Subject(s)
Humans , Female , Fats , Injections , Deoxycholic Acid , Phosphatidylcholines , SodiumABSTRACT
Methylene blue (MB) is a hydrophobic drug molecule, having importance both as a staining reagent and pharmaceutical agent. MB is strongly fluorescent, with an emission peak at 686 nm (λex 665 nm). In the study, the possibility of MB as an extrinsic fluorophore to study the micellization behavior of bile salts (BSs) was carried out. Since BSs are drug delivery systems, the solubilization of hydrophobic MB drug molecule by BSs was achieved and the nature of association of MB with BS media, namely sodium cholate (NaC) and sodium deoxycholate (NaDC) was evaluated. Change in the photophysical properties of MB is monitored through fluorescence intensity and fluorescence anisotropy at emission peak, 686 nm of MB. Molecular mechanics calculations were carried out to evaluate the MB–BS association. The estimated heat of formation,ΔHf values are–625.19 kcal/mol for MB–NaC and–757.48 kcal/mol for MB–NaDC. The photophysical study also revealed that MB reports the step-wise aggregation pattern of BSs media, as an extrinsic fluorescence probe.
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INTRODUCCIÓN: en la actualidad las especies del género Aeromonas han emergido como un problema de salud pública, son ellas los agentes etiológicos de las enfermedades diarreicas con el aumento de la atención médica por años. Los procedimientos convencionales para su diagnóstico son muy engorrosos, laboriosos y duraderos. Una nueva metodología que emplea medios de cultivo cromogénicos ha permitido la simplificación y aceleración de su diagnóstico, que ofrece resultados altamente específicos. OBJETIVO: estudiar el efecto de la combinación de diferentes agentes selectivos de los microorganismos grampositivos sobre el aumento de la capacidad de recuperación, cuantificación y diferenciación de las especies de Aeromonas. MÉTODOS: se estudió el efecto inhibidor de la combinación de agentes selectivos (desoxicolato de sodio (0,05-0,2 g·L-1), sales biliares (0,65 g·L-1), verde brillante (0,025-0,03 g·L-1), cristal violeta (0,001-0,01 g·L-1) y sulfito de sodio (0,8 g·L-1) sobre los microorganismos grampositivos, así como la capacidad de recuperación, cuantificación y diferenciación de las especies de Aeromonas. Como base se utilizó la formulación de CromoCen AGN, sin el desoxicolato de sodio. RESULTADOS: los valores de las productividades de los medios CromoCen AE y CromoCen AGN a partir del inóculo 1,5 × 102 UFC·mL-1 resultaron, para: A. hydrophila 116,8 % y 23,9 %, A. caviae 100,8 % y 3,95 %, A. bestiarium 93,6 % y 28,8 %, A. culicicola 85,1 % y 66,12 %, A. veronii 116,7 % y 59,2 %, A. popoffi 86,56 % y 13,2 %, A. trota 94,8 % y 11,25 % y para A. eucrinophila 103,9 % y 2,80 %. La nueva composición cromogénica logró la diferenciación de los microorganismos por sus características culturales: color, forma, superficie, bordes en las colonias y proteólisis del medio circundante. CONCLUSIONES: la combinación de diferentes agentes selectivos para la inhibición de los microorganismos grampositivos coadyuvo el aumento de la capacidad de recuperación, cuantificación y diferenciación de las especies de Aeromonas.
INTRODUCTION: Species of the genus Aeromonas are a current public health problem, for they are the etiological agents responsible for the growing incidence of diarrheal diseases requiring medical care. Conventional procedures for their diagnosis are very complicated, laborious and time-consuming. A new methodology based on the use of chromogenic culture media allows diagnostic simplification and acceleration, yielding highly specific results. OBJECTIVE: Study the effect of combining several selective agents for gram-positive microorganisms upon an increased capacity for recovery, quantification and differentiation of Aeromonas species. METHODS: Assessment was conducted of the inhibiting effect of combined selective agents (sodium deoxycholate (0.05-0.2 g·L-1), bile salts (0.65 g·L-1), brilliant green (0.025-0.03 g·L-1), crystal violet (0.001-0.01 g·L-1) and sodium sulfite (0.8 g·L-1)) on gram-positive microorganisms, as well as their capacity for recovery, quantification and differentiation of Aeromonas species. The base used was the CromoGen AGN formulation without sodium deoxycholate. RESULTS: Productivity values for the media CromoCen AE and CromoCen AGN based on inoculation of 1.5 × 102 CFU·mL-1 were 116.8 % and 23.9 % for A. hydrophila, 100.8 % and 3.95 % for A. caviae, 93.6 % and 28.8 % for A. bestiarium, 85.1 % and 66.12 % for A. culicicola, 116.7 % and 59.2 % for A. veronii, 86.56 % and 13.2 % for A. popoffi, 94.8 % and 11.25 % for A. trota, and 103.9 % and 2.8 0% for A. eucrinophila. The new chromogenic composition enabled differentiation of microorganisms based on their cultural characteristics: color, shape, surface, colony borders and environmental proteolysis. CONCLUSIONS: Combination of various selective agents for the inhibition of grampositive microorganisms led to an increased capacity for recovery, quantification and differentiation of Aeromonas species.
Subject(s)
Humans , Chromogenic Compounds , Aeromonas/pathogenicity , Dysentery/ethnology , Sodium Sulfite/methodsABSTRACT
Objective: To establish the key conditions for the determination of percutaneous absorption of Panax notoginseng saponins (PNS) in transfersomes (TFS) by in vitro skin permeation method and clarify its percutaneous absorption characteristics. Methods: The film hydration-dispersion method was used to prepare PNS TFS and liposomes (LPS). Their physico-chemical properties were characterized. The drug content and sample volume of PNS TFS for in vitro skin permeation experiments were screened. The effects of vesicle type (TFS or LPS), size of the TFS, and formulation amount of sodium deoxycholate (DOC) on percutaneous permeation of PNS were investigated. Results: The TFS and LPS were mainly unilamellar vesicles with roundish shape and size of (121.2 ± 4.5) and (113.9 ± 2.9) nm, without gathering property. According to the cumulative permeated quantity (Qn) and steady-state percutaneous permeation rate (J) of the assayed ingredients, the appropriate PNS content in the TFS was 500 mg and sample volume was 0.5 mL. Compared with those of the LPS, the Qn values of each assayed component (ginseng saponin Rg1, ginseng saponin Rb1, ginseng saponin Re, PNS R1) in PNS of the TFS were high, and the J values of the assayed components in TFS were about 2-3 times of those in the LPS. The Qn and J values of the assayed components in the TFS with an average size of 120 nm were obviously higher than those of the assayed components in the TFS with an average size of 250 nm. The Qn and J values of the assayed components in PNS TFS with large amount of DOC were prominently higher than those containing small amount of DOC, and the increase ratios of different assayed components were different. Conclusion: In vitro skin permeation method is suitable for the determination of percutaneous absorption of PNS in TFS. The TFS promote drug percutaneous permeation stronger than the LPS and the promotion increases with an appropriate increase of the amount of DOC and decrease of vesicle size of the TFS.
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AIM@#To improve the absorption of thymopeptides (TH) by preparing sodium deoxycholate/phospholipid-mixed nanomicelles (SDC/PL-MMs).@*METHODS@#TH-SDC/PL-MMs were prepared by a film dispersion method, and then evaluated using photon correlation spectroscopy (PCS), zeta potential measurement, as well as their physical stability after storage for several days. Furthermore, in situ intestinal single-pass perfusion experiments and pharmacodynamics in immunodeficient mice were performed to make a comparison with TH powders and the control drug in absorption properties.@*RESULTS@#A narrow size distribution of nanomicelles, with a mean particle size of (149 ± 8.32) nm and a zeta potential of (-31.05 ± 2.52) mV, was obtained. The in situ intestine perfusion experiments demonstrated a significant advantage in absorption characteristics for TH compared to the other formulations, and oral administration of TH-SDC/PL-MMs potentiated an equivalent effect with i.h. TH in pharmacodynamic studies in immunodeficient mice.@*CONCLUSIONS@#TH-SDC/PL-MMs prepared by a film dispersion method are able to improve the absorption of TH. SDC/PL-MMs might be a good approach for the more effective delivery of drugs like TH.
Subject(s)
Animals , Mice , Rats , Chemistry, Pharmaceutical , Deoxycholic Acid , Chemistry , Drug Carriers , Chemistry , Drug Stability , Micelles , Particle Size , Peptides , Chemistry , Pharmacokinetics , Phospholipids , Chemistry , Rats, Wistar , Thymus Gland , ChemistryABSTRACT
Objective: To prepare and optimize the prescription of betulinic acid (BA) ethosomes modified by sodium deoxycholate (SDC) and then to investigate its transdermal penetration as carrier of BA. Methods: The BA ethosomes modified by SDC were prepared by the ethanol injection method. The encapsulation efficiency (EE) was considered as the evaluation index to optimize the prescription of the ethosomes by orthogonal design, and the shape and particle size of the optimized ethosomes were analyzed. The in vitro transdermal absorption of BA was evaluated using Franz diffusion cells. The accumulated permeation amounts and permeation rate of liposomes, ethosomes, and BA ethosomes modified by SDC were compared. Results: The best formulation consisted of soybean lecithin-SDC-BC (18:1:1) and 35% ethanol. The average EE and the particle size were (93.8 ± 1.6)% and (102.3 ± 3.6) nm, respectively. The accumulated permeation amount of BA ethosomes modified by SDC in 12 h was (99.62 ± 9.44) μg/cm2, which was 1.67, 3.85, and 8.33 times of ethosomes, liposomes, and satuated solution containing 10% isopropanol, respectively. Conclusion: The BA ethosomes, modified by SDC with high EE, obviously enhance the percutaneous absorption of BA and might be one of the most perspective percutaneous preparations.
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OBJECTIVE: To improve the oral bioavailability of glycyrrhizin by preparing glyeyrrhizin-sodium deoxycholate/phos-pholipid-mixed micelles (GL-SDC/PL-MMs). METHODS: GL-SDC/PL-MMs was prepared by a film dispersion method. In order toevaluate the property GL-SDC/PL-MMs comprehensively, physical and chemical properties determination, in situ intestinal absorption, and pharmacokinetics test were carried out. RESULTS: The average particle size of drug-loaded micelles prepared by film dispersion method was (82.99±7.5) nm and Zeta potential was (-32.23±1.05) mV. Compared with the control drug, glycyrrhizin loaded in SDC/PL-MMs significantly improved its in situ intestinal absorption. The oral bioavailability was markedly enhanced, indicated by the increase of ρmax to 77.26 μg · mL-1, which was 2.82 times of that of the control drug. CONCLUSION: SDC/PL-MMs is expected to be developed into a new drug delivery systems of GL.
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PURPOSE: Lipobean(R)s, widely used in lipodissolving techniques, contain phosphatidylcholine and sodium deoxycholate as its main substances. They have been approved only as medication for liver disease by the FDA. However, they have been used under various clinical settings without exact knowledge of its action mechanism. The authors designed an in vitro study to analyze the effects of different concentrations of phosphatidylcholine and sodium deoxycholate on adipocytes and other types of cells. METHODS: Human adipose-derived stem cell were cultured and induced to differentiate into adipocytes. Fibroblasts extracted from human inferior turbinate tissue, and MC3T3-E1 osteoblast lines were cultured. Phosphatidylcholine solution dissolved with ethanol was applied to the culture medium at differing concentrations (1, 4, 7, 10 mg/mL). The sodium deoxycholate solution dissolved in DMSO applied to the medium at differing concentrations (0.07, 0.1. 0.4. 0.7 mg/mL). Cells were dispersed at a concentration of 5 x 10(3) cells/well in 24 well plates, and surviving cells were calculated 1 day after the application using a CCK-8 kit. RESULTS: The number of surviving cells of adipocytes, fibroblasts and osteoblasts decreased as the concentration of sodium deoxycholate increased. However, all types of cells that had been processed in a phosphatidylcholine showed a cell survival rate of over 70% at all concentrations. CONCLUSION: This study shows that sodium deoxycholate is the more major factor in destroying adipocytes, and it is also toxic to the other cells. Therefore, we conclude that care must be taken when using Lipobean(R)s as a method of reducing adipose tissue, for its toxicity may destroy other nontarget cells existing in the subcutaneous tissue layer.
Subject(s)
Humans , Adipocytes , Adipose Tissue , Cell Survival , Deoxycholic Acid , Dimethyl Sulfoxide , Ethanol , Fibroblasts , Liver Diseases , Osteoblasts , Phosphatidylcholines , Sincalide , Sodium , Stem Cells , Subcutaneous Tissue , TurbinatesABSTRACT
Objective To compare the effect of 2 decellularizing methods,sodium deoxycholate plus Triton X-100 or plus DNase and Rnase,in the preparation of acelluar allograft spinal cord scaffold in order to provide an ideal natural spinal cord scaffold to bridge the nerve gap.Methods Spinal cord was removed from health rats,and then decellularized by the method of freeze thawing(immersing in 3% sodium deoxycholate followed by the mixture of 1?103 U/ml DNase and RNase),or by chemical extraction(immersing in 1% Triton X-100 and then 1% sodium deoxycholate).HE staining,myelin staining and scanning electron microscopy(SEM) were employed to evaluate the spinal cord scaffold after the 2 methods of decellularization.Results Both cells and myelin were completely decellularized with the 2 methods.In cross section,network of the extracellular matrix was presented without axon,sheath and cells nucleus being seen in the scaffold.Typical network of empty tubes were viewed in longitudinal sections.Conclusion An ideal spinal cord scaffold can be produced with these 2 decellularizing methods in tissue engineering.The scaffold made by the 2 methods have similar three dimensional structure with normal spinal cord,so can be used as a graft to bridge the nerve gap directly or as a scaffold to implant the seeding cells in spinal cord tissue engineering.
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In ultrastructural level, this paper shows that the pig bile extracts and its effective constituent, the sodium deoxycholate, could fragment the Trichomonas vaginalis in vitro, The flagellum and caudal projection were splitted up; the plasma membrane, the intracellular membrane system, such as the limiting membranes of hydrogcnosome, phagosome and nuclear envelope were injured too; and cytoplasm was condensed, even the whole body was fragmented. The mechanism of the effeces is probably due to the fact that the surface activity of the drugs accelerated degradation of lipids which are made of the biomembrane system of human trichomonas vaginalis.