Physicochemical screening of antimicrobial agents as potential preservatives for submicron emulsions

Sznitowska, Małgorzata; Janicki, S; Dąbrowska, E; Gajewska, M

doi:10.1016/s0928-0987(02)00034-9

Cited by 43 publications

(29 citation statements)

References 15 publications

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“…Because all the particles in the newly developed propofol microemulsion were less than 100 nm, however, the potency of embolism can be evaded. In general, lipid-based formulations are sterilized by autoclaving at 121 o C. The change in pH of the preservative-free fat formulations was observed due to hydrolysis of phospholipids and triglycerides (Sznitowska et al, 2002) during the sterilization process. Slow hydrolysis of lipids is known to occur after the initial sterilization-induced degradation (Herman and Groves, 1993;Rabinovich-Guilatt et al, 2005).…”

Section: Discussionmentioning

confidence: 99%

Formulation and evaluation of an alternative triglyceride-free propofol microemulsion

Cho

Lee

et al. 2010

Arch. Pharm. Res.

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A new triglyceride-free propofol microemulsion for intravenous injection was formulated using nonionic surfactants, poloxamers and polyethylene glycol 660 hydroxystearate. The aim of this investigation was to evaluate the formulation for storage stability, antimicrobial activity, toxicity and preclinical efficacy. The results were compared to the characteristics obtained for the most commonly used formulation of propofol (Diprivan®). The mean particle diameter of the microemulsion was less than 100 nm so that it could be readily sterilized using a 0.22 μm membrane at room temperature. The microemulsion formulation demonstrated enhanced stability compared to the marketed macroemulsion formulation. In a stress storage condition, it was physicochemically stable for at least 40 months. This new formulation showed higher antimicrobial activity, lower risk of hyperlipidemia and better tolerability than Diprivan®. In preclinical studies, the efficacy and pharmacokinetic profile of the microemulsion were similar to those of Diprivan®. Nevertheless, the administration of the microemulsion caused considerably low histamine release compared to the macroemulsion. Based on these results, the newly developed microemulsion of propofol appeared to have several advantages and, thus, could be an alternative to the fat macroemulsions of propofol.

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Section: Discussionmentioning

confidence: 99%

Formulation and evaluation of an alternative triglyceride-free propofol microemulsion

Cho

Lee

et al. 2010

Arch. Pharm. Res.

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“…The hydroxylated aromatic compound is used in the synthesis of parabens and methylparabens, which are of great interest as antimicrobial agents (23,24) and for production of liquid glass (9).…”

Section: Discussionmentioning

confidence: 99%

“…1, pathway B). By the activity of T4MO, encoded by the tmo genes, toluene is hydroxylated into p-cresol, which is further oxidized by the products of the pcu genes (28) to 4-hydroxybenzoate (4-HBA).4-HBA is an added-value compound used in the synthesis of paraben and methylparaben, which are p-hydroxybenzoic acid alkylic ester derivatives that are of great interest for the synthesis of liquid glass (9) and as antimicrobial agents (23,24). The potential to use 4-HBA as a carbon source is widespread in gram-negative soil bacteria, and it is not a unique property of species that have the T4MO pathway as the toluene catabolic pathway.…”

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confidence: 99%

Genetic Engineering of a Highly Solvent-Tolerant Pseudomonas putida Strain for Biotransformation of Toluene to p- Hydroxybenzoate

Ramos-González

Ben‐Bassat

Campos

et al. 2003

Appl Environ Microbiol

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The solvent-tolerant strain Pseudomonas putida DOT-T1E has been engineered for biotransformation of toluene into 4-hydroxybenzoate (4-HBA). P. putida DOT-T1E transforms toluene into 3-methylcatechol in a reaction catalyzed by toluene dioxygenase. The todC1C2 genes encode the ␣ and ␤ subunits of the multicomponent enzyme toluene dioxygenase, which catalyzes the first step in the Tod pathway of toluene catabolism. A DOT-T1E⌬todC mutant strain was constructed by homologous recombination and was shown to be unable to use toluene as a sole carbon source. The P. putida pobA gene, whose product is responsible for the hydroxylation of 4-HBA into 3,4-hydroxybenzoate, was cloned by complementation of a Pseudomonas mendocina pobA1 pobA2 double mutant. This pobA gene was knocked out in vitro and used to generate a double mutant, DOT-T1E⌬todCpobA, that was unable to use either toluene or 4-HBA as a carbon source. The tmo and pcu genes from P. mendocina KR1, which catalyze the transformation of toluene into 4-HBA through a combination of the toluene 4-monoxygenase pathway and oxidation of p-cresol into the hydroxylated carboxylic acid, were subcloned in mini-Tn5Tc and stably recruited in the chromosome of DOT-T1E⌬todCpobA. Expression of the tmo and pcu genes took place in a DOT-T1E background due to cross-activation of the tmo promoter by the two-component signal transduction system TodST. Several independent isolates that accumulated 4-HBA in the supernatant from toluene were analyzed. Differences were observed in these clones in the time required for detection of 4-HBA and in the amount of this compound accumulated in the supernatant. The fastest and most noticeable accumulation of 4-HBA (12 mM) was found with a clone designated DOT-T1E-24.Pseudomonas putida DOT-T1E, a rifampin-resistant derivative of strain DOT-T1, is highly resistant to solvents, with the logarithm of the partition coefficient in a mixture of octanol and water (log P ow ) being higher than 2.5. This strain is able to thrive in the presence of supersaturating concentrations of toluene. This aromatic compound serves as a carbon and energy source for the bacteria (17). The metabolic route for the mineralization of toluene by DOT-T1E is the Tod pathway, in which toluene is oxidized to 3-methylcathecol, which in turn is channeled to Krebs cycle intermediates via a meta-cleavage pathway (13) (Fig. 1, pathway A).In Pseudomonas mendocina KR1, toluene 4-monooxygenase (T4MO) is responsible for the first step of toluene catabolism (26) (Fig. 1, pathway B). By the activity of T4MO, encoded by the tmo genes, toluene is hydroxylated into p-cresol, which is further oxidized by the products of the pcu genes (28) to 4-hydroxybenzoate (4-HBA).4-HBA is an added-value compound used in the synthesis of paraben and methylparaben, which are p-hydroxybenzoic acid alkylic ester derivatives that are of great interest for the synthesis of liquid glass (9) and as antimicrobial agents (23,24). The potential to use 4-HBA as a carbon source is widespread in gram-negative soil bacteria,...

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“…Therefore, several techniques were performed to improve the transdermal transport of ibuprofen, such as complexation with cyclodextrin, 11 supersaturation, 12,13 preparation of colloidal microstructures with lysinate and lecithin, 14 eutectic systems produced by melting-point depression, 15,16 iontophoresis, 17 and the usage of surfactants and various vehicles. 18,19 Nanoscaled emulsion and microemulsion possess very small droplets size, [20][21][22][23] which makes them quite appealing for the topical delivery of various drugs. They have the ability to accommodate large amounts of drug due to the increased solubilization capacity, thereby enhancing the thermodynamic activity towards the skin.…”

Section: Introductionmentioning

confidence: 99%

In vitro permeation and in vivo anti-inflammatory and analgesic properties of nanoscaled emulsions containing ibuprofen for topical delivery

Abdullah¹,

Abdulkarim²,

Salman³

et al. 2011

IJN

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Introduction: As a topical delivery system, a nanoscaled emulsion is considered a good carrier of several active ingredients that convey several side effects upon oral administration, such as nonsteroidal anti-inflammatory drugs (NSAIDs). Objective: We investigated the in vitro permeation properties and the in vivo pharmacodynamic activities of different nanoscaled emulsions containing ibuprofen, an NSAID, as an active ingredient and newly synthesized palm olein esters (POEs) as the oil phase. Methodology: A ratio of 25:37:38 of oil phase:aqueous phase:surfactant was used, and different additives were used for the production of a range of nanoscaled emulsions. Carbopol ® 940 dispersion neutralized by triethanolamine was employed as a rheology modifier. In some circumstances, menthol and limonene were employed at different concentrations as permeation promoters. All formulae were assessed in vitro using Franz diffusion cell fitted with full-thickness rat skin. This was followed by in vivo evaluation of the anti-inflammatory and analgesic activities of the promising formulae and comparison of the effects with that of the commercially available gel. Results and discussion: Among all other formulae, formula G40 (Carbopol ® 940-free formula) had a superior ability in transferring ibuprofen topically compared with the reference. Carbopol ® 940 significantly decreased the amount of drug transferred from formula G41 through the skin as a result of swelling, gel formation, and reduction in drug thermodynamic activity. Nonetheless, the addition of 10% w/w of menthol and limonene successfully overcame this drawback since, relative to the reference, higher amount of ibuprofen was transferred through the skin. By contrast, these results were relatively comparable to that of formula G40. Pharmacodynamically, the G40, G45, and G47 formulae exhibited the highest anti-inflammatory and analgesic effects compared with other formulae. Conclusion: The ingredients and the physical properties of the nanoscaled emulsions produced by using the newly synthesized POEs succeeded to deliver ibuprofen competently.

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Physicochemical screening of antimicrobial agents as potential preservatives for submicron emulsions

Cited by 43 publications

References 15 publications

Formulation and evaluation of an alternative triglyceride-free propofol microemulsion

Formulation and evaluation of an alternative triglyceride-free propofol microemulsion

Genetic Engineering of a Highly Solvent-Tolerant Pseudomonas putida Strain for Biotransformation of Toluene to p- Hydroxybenzoate

In vitro permeation and in vivo anti-inflammatory and analgesic properties of nanoscaled emulsions containing ibuprofen for topical delivery

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