Stability of drug-carrier emulsions containing phosphatidylcholine mixtures

Trotta, Michele; Pattarino, Franco; Ignoni, Terenzio

doi:10.1016/s0939-6411(01)00230-2

Cited by 64 publications

(36 citation statements)

References 13 publications

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“…lecithin likes to be at the edge of the lipid phase being its lipophilic tails directed to the lipid phase until the hydrophilic portion is directed to the water phase. Thus, the oil phase is totally recovered by the lecithin promoting long time stabilization in the interface of the emulsions (Trotta et al, 2002). From the obtained results, a correlation between the concentration of lecithin and mean particle size of the particles were found, since highest concentrations leads to a decrease in Z-Ave and PI.…”

Section: Resultsmentioning

confidence: 75%

“…Their use in the development of LN dispersions is essential to decrease the interfacial tension between the oil phase and the internal and external aqueous phase, and also to facilitate the emulsification of the lipid matrix. Lecithin is used due to its higher power of emulsification able to provide a very good stabilization of the oil-in-water interfaces and has also been reported to decrease particle size in emulsions that is mainly explained by its amphiphilic character (Trotta et al, 2002;Schubert et al, 2006;Kawaguchi et al, 2008). The lipophilic portion of lecithin dissolves the lipid phase, i.e.…”

Section: Resultsmentioning

confidence: 99%

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Design of cationic lipid nanoparticles for ocular delivery: Development, characterization and cytotoxicity

Fangueiro

Andreani

Egea

et al. 2014

International Journal of Pharmaceutics

132

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a b s t r a c tIn the present study we have developed lipid nanoparticle (LN) dispersions based on a multiple emulsion technique for encapsulation of hydrophilic drugs or/and proteins by a full factorial design. In order to increase ocular retention time and mucoadhesion by electrostatic attraction, a cationic lipid, namely cetyltrimethylammonium bromide (CTAB), was added in the lipid matrix of the optimal LN dispersion obtained from the factorial design. There are a limited number of studies reporting the ideal concentration of cationic agents in LN for drug delivery. This paper suggests that the choice of the concentration of a cationic agent is critical when formulating a safe and stable LN. CTAB was included in the lipid matrix of LN, testing four different concentrations (0.25%, 0.5%, 0.75%, or 1.0%wt) and how composition affects LN behavior regarding physical and chemical parameters, lipid crystallization and polymorphism, and stability of dispersion during storage. In order to develop a safe and compatible system for ocular delivery, CTAB-LN dispersions were exposed to Human retinoblastoma cell line Y-79. The toxicity testing of the CTAB-LN dispersions was a fundamental tool to find the best CTAB concentration for development of these cationic LN, which was found to be 0.5 wt% of CTAB.

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Section: Resultsmentioning

confidence: 75%

Section: Resultsmentioning

confidence: 99%

Design of cationic lipid nanoparticles for ocular delivery: Development, characterization and cytotoxicity

Fangueiro

Andreani

Egea

et al. 2014

International Journal of Pharmaceutics

132

View full text Add to dashboard Cite

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“…[5][6][7][8] Another main problem with nanoemulsions is their thermodynamic instability, resulting in aggregation and flocculation; furthermore, loading a drug into a nanoemulsion system can cause droplet coalescence and even phase separation. [9][10][11] Therefore, it is necessary to develop stable nanoemulsions using alternative safer surfactants.…”

Section: Introductionmentioning

confidence: 99%

Food protein-stabilized nanoemulsions as potential delivery systems for poorly water-soluble drugs: preparation, in vitro characterization, and pharmacokinetics in rats

He¹,

Tan²,

Tian³

et al. 2011

IJN

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Nanoemulsions stabilized by traditional emulsifiers raise toxicological concerns for long-term treatment. The present work investigates the potential of food proteins as safer stabilizers for nanoemulsions to deliver hydrophobic drugs. Nanoemulsions stabilized by food proteins (soybean protein isolate, whey protein isolate, β-lactoglobulin) were prepared by high-pressure homogenization. The toxicity of the nanoemulsions was tested in Caco-2 cells using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide viability assay. In vivo absorption in rats was also evaluated. Food protein-stabilized nanoemulsions, with small particle size and good size distribution, exhibited better stability and biocompatibility compared with nanoemulsions stabilized by traditional emulsifiers. Moreover, β-lactoglobulin had a better emulsifying capacity and biocompatibility than the other two food proteins. The pancreatic degradation of the proteins accelerated drug release. It is concluded that an oil/water nanoemulsion system with good biocompatibility can be prepared by using food proteins as emulsifiers, allowing better and more rapid absorption of lipophilic drugs.

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“…[23][24][25] LME compositions were selected from the respective domain region (Figure 1) for the sequence of the study. The chosen formulations were titled A, B, C, D, and E, in which the proportion of the surfactant was kept constant at 20% and the oil phase was increased from 2% to 10% in order to obtain O:S ratios of 0.1, 0.2, 0.3, 0.4, and 0.5, respectively (see Table 1 for details).…”

Section: Resultsmentioning

confidence: 99%

Development and characterization of biocompatible isotropic and anisotropic oil-in-water colloidal dispersions as a new delivery system for methyl dihydrojasmonate antitumor drug

Silva¹,

Scarpa²,

Rossanezi³

et al. 2014

IJN

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Microemulsions (MEs) are colloidal systems that can be used for drug-delivery and drug-targeting purposes. These systems are able to incorporate drugs modifying bioavailability and stability and reducing toxic effects. The jasmonate compounds belong to a group of plant stress hormones, and the jasmonic acid and its methyl ester derivative have been described as having anticancer activity. However, these compounds are very poorly water-soluble, not allowing administration by an intravenous route without an efficient nanostructured carrier system. In this work, biocompatible MEs of appropriate diameter size for intravenous route administration, loaded and unloaded with methyl dihydrojasmonate (MJ), were developed and described in a pseudo-ternary phase diagram. The compositions of the MEs were carefully selected from their own regions in the pseudo-ternary phase diagram. The formulations were analyzed by light scattering, polarized light microscopy, and X-ray diffraction. Also, a study on rheological profile was performed. The results showed that the droplet size decreased with both MJ incorporation and oil phase/surfactant ratio. All compositions of the studied MEs showed rheological behavior of pseudoplastic fluid and amorphous structures. In the absence of MJ, most of the studied MEs had thixotropic characteristics, which became antithixotropic in the presence of the drug. Almost all MJ-unloaded MEs presented anisotropic characteristics, but some formulations became isotropic, especially in the presence of MJ. The results of this study support the conclusion that the studied system represents a promising vehicle for in vivo administration of the MJ antitumor drug.

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Stability of drug-carrier emulsions containing phosphatidylcholine mixtures

Cited by 64 publications

References 13 publications

Design of cationic lipid nanoparticles for ocular delivery: Development, characterization and cytotoxicity

Design of cationic lipid nanoparticles for ocular delivery: Development, characterization and cytotoxicity

Food protein-stabilized nanoemulsions as potential delivery systems for poorly water-soluble drugs: preparation, in vitro characterization, and pharmacokinetics in rats

Development and characterization of biocompatible isotropic and anisotropic oil-in-water colloidal dispersions as a new delivery system for methyl dihydrojasmonate antitumor drug

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