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15 records – page 1 of 2.

Development and evaluation of microbicidal hydrogels containing monoglyceride as the active ingredient.

https://arctichealth.org/en/permalink/ahliterature7572
Source
J Pharm Sci. 1999 Oct;88(10):1011-5
Publication Type
Article
Date
Oct-1999
Author
T. Kristmundsdóttir
S G Arnadóttir
G. Bergsson
H. Thormar
Author Affiliation
Department of Pharmacy and Institute of Biology, University of Iceland, Reykjavik, Iceland. thordisk@hi.is
Source
J Pharm Sci. 1999 Oct;88(10):1011-5
Date
Oct-1999
Language
English
Publication Type
Article
Keywords
Animals
Anti-Bacterial Agents
Anti-Infective Agents - chemical synthesis - pharmacology - toxicity
Antiviral Agents - chemical synthesis - pharmacology
Cell Survival - drug effects
Cells, Cultured
Chlamydia trachomatis - drug effects
Chromatography, High Pressure Liquid
Fatty Acids - pharmacology
Glycerides - analysis - chemical synthesis - pharmacology - toxicity
Herpesvirus 1, Human - drug effects
Hydrogels - chemical synthesis - pharmacology - toxicity
Neisseria gonorrhoeae - drug effects
Research Support, Non-U.S. Gov't
Sexually Transmitted Diseases, Bacterial - prevention & control
Solubility
Vehicles
Abstract
A number of medium-chain saturated and long-chain unsaturated fatty acids and their monoglycerides were tested against herpes simplex virus (HSV-1) to determine which lipids were most active during a short incubation time. The aim was to find which lipid would be preferable as the active ingredient in a virucidal hydrogel formulation for the purpose of preventing transmission of pathogens to mucosal membranes, particularly sexually transmitted viruses, such as herpes simplex virus and human immunodeficiency virus (HIV), and bacteria, such as Chlamydia trachomatis and Neisseria gonorrheae. The main strategy was that the formulations would be fast-acting, killing large numbers of virus or bacteria on contact in a short time, preferably causing at least a 10000-fold reduction in virus/bacteria titer in 1-5 min. Monocaprin, the 1-monoglyceride of capric acid, and lauric acid were found to be most active of all the lipids tested, causing a greater than 100000-fold reduction in virus titer in 1 min at a concentration of 20 mM. When tested at a concentration of 10 mM for 1 min, monocaprin was still fully active whereas lauric acid had no or negligible activity. It was concluded that monocaprin was most suitable as the active ingredient in a fast-acting virucidal gel formulation, and several hydrogel formulations containing monocaprin were tested. Formulations where the monoglyceride was dissolved in glycofurol were found to be active against HSV-1. The hydrogel formulations containing 20 mM monocaprin were highly virucidal in vitro and caused a greater than 100000-fold (HSV-1) inactivation of virus in human semen in 1 min. Formulations in dilution 1:10 were cytotoxic in monolayers of CV-1 cells, but they were 10-100 fold less cytotoxic than a commercial product which contains 2% nonoxynol-9.
Notes
Erratum In: J Pharm Sci 1999 Dec;88(12):1366
PubMed ID
10514348 View in PubMed
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Effect of buffers on the properties of microbicidal hydrogels containing monoglyceride as the active ingredient.

https://arctichealth.org/en/permalink/ahliterature7323
Source
Drug Dev Ind Pharm. 2003 Feb;29(2):121-9
Publication Type
Article
Date
Feb-2003
Author
T. Kristmundsdóttir
P. Sigurdsson
H. Thormar
Author Affiliation
Faculty of Pharmacy, University of Iceland, Hagi, Reykjavík, Iceland. thordisk@hi.is
Source
Drug Dev Ind Pharm. 2003 Feb;29(2):121-9
Date
Feb-2003
Language
English
Publication Type
Article
Keywords
Acrylic Resins - chemistry
Antiviral Agents - chemistry - pharmacology
Buffers
Carboxymethylcellulose - chemistry
Chemistry, Pharmaceutical
Chromatography, High Pressure Liquid
Drug Compounding
Excipients - chemistry
Glycerides - chemistry - pharmacology
Herpesvirus 1, Human - drug effects
Hydrogels - chemistry
Hydrogen-Ion Concentration
Methylcellulose - analogs & derivatives - chemistry
Povidone - chemistry
Research Support, Non-U.S. Gov't
Viscosity
Abstract
Hydrogel formulations containing the monoglyceride monocaprin have shown potent microbicidal activity against several sexually transmitted viruses and bacteria. It is recommended that formulations for preventing infection in the vagina have a low pH as the HIV virus is inactivated at low pH. The object of the work was to investigate how incorporation of buffers into the hydrogel formulations affects physicochemical properties and microbicidal activity of the active substance. Two series of gels were formulated using carbomer (Carbopol 934) and sodium carboxymethylcellulose (NaCMC) as gel-forming agents. The presence of buffers in the gels caused a lowering in gel viscosity, with carbomer gels being more sensitive to buffer presence than NaCMC gels. To obtain viscosity similar to that of a gel without buffer, the amount of polymer needs to be increased. An increase in the amount of NaCMC by 60-70% is needed to obtain the same viscosity as in gel without buffers; but for carbomer, the amount of polymer needs to be doubled. It appears that the effect of maleate buffer on NaCMC gel formation is greater than that of the citrate/lactate buffer; but for carbopol gels, the effects of the buffer systems tested on gel viscosity were equal. The virucidal activity of NaCMC gel buffered with citrate/lactate buffer against herpes simplex virus type 1 and HIV was not reduced by the presence of buffer. The results show that the presence of buffers in the hydrogel formulations affects gel viscosity, but the virucidal effect of the active compound, monocaprin, is not diminished.
PubMed ID
12648008 View in PubMed
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Effects of polysorbates on antiviral and antibacterial activity of monoglyceride in pharmaceutical formulations.

https://arctichealth.org/en/permalink/ahliterature9724
Source
Pharmazie. 2003 Apr;58(4):286-7
Publication Type
Article
Date
Apr-2003
Source
Appl Biochem Biotechnol. 2004;113-116:433-45
Publication Type
Article
Date
2004
Author
Carla C B Pereira
Mônica A P da Silva
Marta A P Langone
Author Affiliation
Escola de Química, Universidade Federal do Rio de Janeiro, Centro de Tecnologia, Bloco E, Lab I 221, Cidade Universitária, Brazil.
Source
Appl Biochem Biotechnol. 2004;113-116:433-45
Date
2004
Language
English
Publication Type
Article
Keywords
Biotechnology - methods
Chromatography, Gas
Enzymes - chemistry
Enzymes, Immobilized
Esters
Glycerides - biosynthesis - chemistry
Glycerol - chemistry
Laurates - chemistry
Lauric Acids - chemistry
Lipase - chemistry
Models, Theoretical
Monoglycerides
Research Support, Non-U.S. Gov't
Temperature
Time Factors
Abstract
The aim of this study was to produce monolaurin utilizing a commercial immobilized lipase (Lipozyme IM-20; Novo Nordisk, Bagsvaerd, Denmark) through the direct esterification of lauric acid and glycerol in a solvent-free system. The influence of fatty acid/glycerol molar ratio, temperature, and Lipozyme (IM-20) concentration on the molar fraction of monolaurin were determined using an experimental design. The best conditions employed were 55 degrees C, lauric acid/glycerol molar ratio of 1.0, and 3.0% (w/w) enzyme concentration. The final product, obtained after 6 h of reaction, was 45.5% monolaurin, 26.8% dilaurin, 3.1% trilaurin, and 24.6% lauric acid. The reusability of the enzyme was also studied.
PubMed ID
15054269 View in PubMed
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Hydrogels containing monocaprin have potent microbicidal activities against sexually transmitted viruses and bacteria in vitro.

https://arctichealth.org/en/permalink/ahliterature7584
Source
Sex Transm Infect. 1999 Jun;75(3):181-5
Publication Type
Article
Date
Jun-1999
Author
H. Thormar
G. Bergsson
E. Gunnarsson
G. Georgsson
M. Witvrouw
O. Steingrímsson
E. De Clercq
T. Kristmundsdóttir
Author Affiliation
Institute of Biology, University of Iceland, Reykjavik, Iceland.
Source
Sex Transm Infect. 1999 Jun;75(3):181-5
Date
Jun-1999
Language
English
Publication Type
Article
Keywords
Animals
Anti-Bacterial Agents
Anti-Infective Agents - therapeutic use
Cells, Cultured
Chlamydia trachomatis - drug effects
Gels
Glycerides - therapeutic use
HIV-1 - drug effects
Herpesvirus 2, Human - drug effects
Humans
Microbial Sensitivity Tests
Neisseria gonorrhoeae - drug effects
Rabbits
Research Support, Non-U.S. Gov't
Semen - microbiology
Sexually Transmitted Diseases - drug therapy
Abstract
OBJECTIVE: To investigate the in vitro microbicidal and cytocidal potency of monocaprin dissolved in pharmaceutical hydrogel formulations and to evaluate their potential use as vaginal microbicides against sexually transmitted pathogens such as herpes simplex virus type 2 (HSV-2), human immunodeficiency virus type 1 (HIV-1), Chlamydia trachomatis, and Neisseria gonorrhoeae. METHODS: Gel formulations were mixed with equal volumes of virus/bacteria suspensions in culture medium and incubated for 1 and 5 minutes. The reduction in virus/bacteria titre was used as a measure of microbicidal activity. Similarly, gels were mixed with human semen to study their effect on leucocytes. The toxicity of the gels was tested in rabbits by the standard vaginal irritation test. RESULTS: Gels containing 20 mM of monocaprin caused a greater than 100,000-fold inactivation of HSV-2 and Neisseria in 1 minute and of Chlamydia in 5 minutes. Similarly, the gels caused a greater than 10,000-fold inactivation of HIV-1 in semen in 1 minute. They caused more than a 10,000-fold reduction in the number of viable leucocytes in semen in 1 minute. No toxic effect on the vaginal mucosa of rabbits was observed after daily exposure for 10 days. CONCLUSIONS: Hydrogels containing monocaprin are potent inactivators of sexually transmitted viruses and bacteria in vitro. This simple lipid seems to be a feasible choice as a mucosal microbicide for prevention of sexually transmitted infections. It is a natural compound found in certain foodstuffs such as milk and is therefore unlikely to cause harmful side effects in the concentrations used.
PubMed ID
10448397 View in PubMed
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Induction of protective and specific antibodies against cocaine by intranasal immunisation using a glyceride adjuvant.

https://arctichealth.org/en/permalink/ahliterature57375
Source
Biol Pharm Bull. 2005 Jun;28(6):1038-42
Publication Type
Article
Date
Jun-2005
Author
Kolbrun Hrafnkelsdottir
Jon Valgeirsson
Sveinbjorn Gizurarson
Author Affiliation
Lyfjathroun, Biopharmaceuticals, Reykjavik, Iceland.
Source
Biol Pharm Bull. 2005 Jun;28(6):1038-42
Date
Jun-2005
Language
English
Publication Type
Article
Keywords
Administration, Intranasal
Animals
Antibodies - metabolism
Brain - metabolism
Cocaine - administration & dosage - antagonists & inhibitors - metabolism
Comparative Study
Female
Glycerides - administration & dosage - metabolism
Immunization - methods
Mice
Mice, Inbred BALB C
Abstract
The goal of this study was to investigate an intranasal cocaine vaccine containing the mucosal adjuvant macrogol-6-glycerol capylocaprate (RhinoVax). Cocaine-KLH conjugate was prepared and administered in two formulations. Ten mice were immunised intranasally using RhinoVax as adjuvant and ten subcutaneously using aluminium hydroxide as an adjuvant. A negative control group (n=10) received unconjugated KLH with RhinoVax intranasally. Specific cocaine antibodies in serum were measured following primary and booster immunisation. Relative antibody responses in serum indicated that the immunisation was successful. Animals were then challenged with cocaine either intranasally or intraperitoneally with subsequent measurement of drug distribution into the serum, brain and olfactory bulb. The cocaine-immunised groups revealed significantly lower cocaine levels in the brain compared to the negative control group. The inhibition of cocaine distribution to the brain in the intranasal immunised group was comparable to that of the subcutaneous immunised group. This was unexpected because the cocaine specific antibody levels in serum were fivefold lower in the intranasal immunised group. However, the presence of mucosal cocaine specific antibodies after intranasal immunisation could play an important role in hindering direct access of cocaine into the brain via the olfactory bulb.
PubMed ID
15930741 View in PubMed
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THE INFLUENCE OF SEASONAL VARIATION, DIET AND PHYSICAL ACTIVITY ON SERUM LIPIDS IN YOUNG MEN IN ANTARCTICA.

https://arctichealth.org/en/permalink/ahliterature62691
Source
Am J Clin Nutr. 1965 May;16:428-35
Publication Type
Article
Date
May-1965

15 records – page 1 of 2.