Structural changes of biocompatible neutral microemulsions stabilized by mixed surfactant containing soya phosphatidylcholine and their relationship with doxorubicin release

Formariz, Thalita Pedroni; Chiavacci, Leila Aparecida; Sarmento, Víctor Hugo Vitorino; Franzini, Cristina Maria; Silva, A. A.; Scarpa, Maria Virgínia; Santilli, Celso Valentim; Egito, Eryvaldo Sócrates Tabosa do; Oliveira, Anselmo Gomes de

doi:10.1016/j.colsurfb.2007.12.021

Cited by 49 publications

(33 citation statements)

References 16 publications

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“…Depending on the spontaneous curvature and flexibility of the surfactant monolayer, bicontinuous microemulsion and liquid crystals appear during formation of a microemulsion. 23 In our research, in order to achieve the optimal water content, formulations with higher viscosity and electrical conductivity were selected, which could be near to the structure of bicontinuous microemulsion. The size and zeta potential of the diluted microemulsion were determined to characterize its properties after entering the gastrointestinal tract via oral administration.…”

Section: Discussionmentioning

confidence: 99%

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

Zhuang²,

Wu³

et al. 2011

IJN

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Background: A microemulsion is an effective formulation for improving the oral bioavailability of poorly soluble drugs. In this paper, a water-in-oil (w/o) microemulsion was investigated as a system for enhancing the oral bioavailability of Biopharmaceutic Classification System (BCS) III drugs. Methods: The microemulsion formulation was optimized using a pseudoternary phase diagram, comprising propylene glycol dicaprylocaprate (PG), Cremophor ® RH40, and water (30/46/24 w/w). Results: The microemulsion increased the oral bioavailability of hydroxysafflor yellow A which was highly water-soluble but very poorly permeable. The relative bioavailability of hydroxysafflor yellow A microemulsion was about 1937% compared with a control solution in bile duct-nonligated rats. However, the microemulsion showed lower enhanced absorption ability in bile duct-ligated rats, and the relative bioavailability was only 181%. In vitro experiments were further employed to study the mechanism of the enhanced effect of the microemulsion. In vitro lipolysis showed that the microemulsion was digested very quickly by pancreatic lipase. About 60% of the microemulsion was digested within 1 hour. Furthermore, the particle size of the microemulsion after digestion was very small (53.3 nm) and the digested microemulsion had high physical stability. An everted gut sac model demonstrated that cumulative transport of the digested microemulsion was significantly higher than that of the diluted microemulsion. Conclusion: These results suggested that digestion of the microemulsion by pancreatic lipase plays an important role in enhancing oral bioavailability of water-soluble drugs.

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Section: Discussionmentioning

confidence: 99%

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

Zhuang²,

Wu³

et al. 2011

IJN

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“…This phenomenon can be explained by the fact that the soy PC proportion of the surfactant mixture can absorb small amounts of water to form viscous gels. 8 Because of the predominant lipophilic character of PC, which has a low hydrophilic lipophilic balance (HLB) value (4.0), high hydrophilic surfactants were associated with it to give an appropriated mix to stabilize the system. Thus, EU (HLB = 14) and SO (HLB = 18) were used for this purpose of allowing greater absorption of the aqueous phase by the system.…”

Section: Resultsmentioning

confidence: 99%

“…[3][4][5]9 Antitumor and antibiotic drugs have often been incorporated into oil-in-water colloidal dispersions, due to the ability of such systems to reduce toxicity and increase therapeutic efficacy. [7][8][9][10] The jasmonates belong to a group of cyclopentenone moiety that is synthesized in plants in response to injury, insect attack, and wounding. 11 Several reports have demonstrated that cyclopentenone moiety-containing molecules such as prostaglandins and clavulones induce apoptosis in different signaling mechanisms.…”

Section: Silva Et Almentioning

confidence: 99%

“…In the pharmaceutical technology field, systems based on the nanotechnology platform may increase the apparent solubility of poorly soluble drugs, improving bioavailability and providing safe administration in the body, especially nanoand microemulsion systems. [5][6][7][8][9][10] MJ derivatives follow the physicochemical characteristics of these compounds and cannot be directly administered, and it is necessary to develop systems for such administration.…”

Section: Silva Et Almentioning

confidence: 99%

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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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“…MEs have been proven a suitable vehicle for this purpose. [18][19][20] In previous work, our research team studied anionic isotropic and anisotropic oil-in-water colloidal systems stabilized with a mixture of phosphatidylcholine (PC)/glycerol (GL)/sodium oleate as surfactant and cholesterol as oil phase. This colloidal dispersion system was able to incorporate MJ and to maintain its physical stability characteristics, suitable for intravenous administration.…”

Section: Introductionmentioning

confidence: 99%

Oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate

Silva¹,

Scarpa²,

Carlos³

et al. 2015

IJN

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Methyl dihydrojasmonate (MJ) has been studied because of its application as an antitumor drug compound. However, as MJ is a poorly water-soluble compound, a suitable oil-in-water microemulsion (ME) has been studied in order to provide its solubilization in an aqueous media and to allow its administration by the parenteral route. The ME used in this work was characterized on the pseudo-ternary phase diagram by dynamic light scattering and rheological measurements. Regardless of the drug presence, the droplet size was directly dependent on the oil/surfactant (O/S) ratio. Furthermore, the drug incorporation into the ME significantly increased the ME diameter, mainly at low O/S ratios. The rheological evaluation of the systems showed that in the absence of drug a Newtonian behavior was observed. On the other hand, in the presence of MJ the ME systems revealed pseudoplastic behavior, independently of the O/S ratio. The in vivo studies demonstrated that not only was the effect on the tumor inhibition inversely dependent on the MJ-loaded ME administered dose, but also it was slightly higher than the doxorubicin alone, which was used as the positive control. Additionally, a small antiangiogenic effect for MJ-loaded ME was found at doses in which it possesses antitumor activity. MJ revealed to be nontoxic at doses higher than 350 mg/kg, which was higher than the dose that provides tumor-inhibition effect in this study. Because the MJ-loaded ME was shown to have anticancer activity comparable to doxorubicin, the ME described here may be considered a suitable vehicle for parenteral administration of MJ.

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Structural changes of biocompatible neutral microemulsions stabilized by mixed surfactant containing soya phosphatidylcholine and their relationship with doxorubicin release

Cited by 49 publications

References 16 publications

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

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

Oil-in-water biocompatible microemulsion as a carrier for the antitumor drug compound methyl dihydrojasmonate

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