Drug solubilization and in vitro toxicity evaluation of lipoamino acid surfactants

Ménard, Nathalie; Tsapis, Nicolas; Poirier, Cécile; Arnauld, Thomas; Moine, Laurence; Lefoulon, François; Péan, Jean-Manuel

doi:10.1016/j.ijpharm.2011.11.030

Cited by 41 publications

(35 citation statements)

References 23 publications

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“…Based on the principle that pyrene emission spectra was dependent on the polarity of the microenvironment, the hydrophobic pyrene was encapsulated into the core of micelle at different concentrations resulting in the decrease of the ratio between I372 and I383 (Ménard et al, 2012). The CMC of CUR-loaded mixed micelles from the experiment was 0.0087 g/l, far lower than the CMC of SDC (3 mM) (Zhou et al, 2010).…”

Section: Discussionmentioning

confidence: 96%

Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

et al. 2014

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Although curcumin (CUR) can inhibit proliferation and induce apoptosis of tumors, the poor water solubility restricted its clinical application. The aim of this study was to improve the aqueous solubility of CUR and make more favorable changes to bioactivity by preparing curcumin-loaded phospholipid-sodium deoxycholate-mixed micelles (CUR-PC-SDC-MMs). CUR-PC-SDC-MMs were prepared by the thin-film dispersion method. Based on the results of single factor exploration, the preparation technology was optimized using the central composite design-response surface methodology with drug loading and entrapment efficiency (EE%) as indicators. The images of transmission electron microscopy showed that the optimized CUR-PC-SDC-MMs were spherical and well dispersed. The average size of the mixed micelles was 66.5 nm, the zeta potential was about À26.96 mV and critical micelle concentration was 0.0087 g/l. CUR was encapsulated in PC-SDC-MMs with loading capacity of 13.12%, EE% of 87.58%, and the solubility of CUR in water was 3.14 mg/ml. The release results in vitro showed that the mixed micelles presented sustained release behavior compared to the propylene glycol solution of CUR. The IC 50 values of CUR-loaded micelles and free drug in human breast carcinoma cell lines were 4.10 mg/ml and 6.93 mg/ml, respectively. It could be concluded from the above results that the CUR-PC-SDC-MMs system might serve as a promising nanocarrier to improve the solubility and bioactivity of CUR.

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Section: Discussionmentioning

confidence: 96%

Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

et al. 2014

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“…38 While the pyrene was solubilized in micelles, which resulted in the formation of hydrophobic domains, a significant decrease of I 1 /I 3 ratio was observed. 39 The I 1 /I 3 ratio became finally steady with high surfactant concentration, proving that the pyrene was in a totally hydrophobic environment.…”

Section: Discussionmentioning

confidence: 96%

“…29,33,38,39 Pyrene monomer emission spectra are related to vibronic fine structures, whose intensities are heavily dependent on the polarity of the microenvironment. As a hydrophobic molecule with low aqueous solubility (∼0.3 µM), pyrene was sensitive to a more hydrophobic environment.…”

Section: Discussionmentioning

confidence: 99%

Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study

Jiang²,

Ren³

et al. 2012

IJN

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Background:The clinical application of nimodipine (NIM) is limited by several unfavorable properties, which are induced by its low aqueous solubility. In the present study, nimodipineloaded egg phosphatidylcholine-sodium glycocholate mixed micelles (NIM-EPC-SGC-MMs) were prepared to improve the water solubility of NIM, thus allowing it to be more applicable for clinical use. Methods: NIM-EPC-SGC-MMs were prepared using the coprecipitation method and the factors influencing formulation quality were optimized. After formulation, water solubility, solubilizing efficiency, drug loading, particle size, physical compatibility, pharmacokinetics, and vascular irritability were determined. Results: The mean size of the NIM-EPC-SGC-MMs was 6.099 ± 0.048 nm under optimized conditions. The water solubility of NIM in EPC-SGC-MMs was enhanced 250-fold compared with free NIM. The physical compatibility, pharmacokinetic, and vascular irritability studies showed that, in comparison to the commercially available NIM injections, NIM-EPC-SGCMMs presented better physical compatibility, the same pharmacokinetic profile, and less risk of local vascular irritation and phlebitis. Conclusion: EPC-SGC-MMs represent a promising new formulation suitable for the intravenous delivery of NIM.

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“…On the other hand, 24 hours of incubation was necessary to observe the IC 50 value of 0.56 mg/mL for Cremophor EL. These values could be related to the IC 50 of 0.25 mg/mL (by MTT) 62 found for Polysorbate 80, which is a nonionic surfactant commonly used in drug formulations, especially for IV formulation. 52 Surfactant cytotoxicity could be explained by its amphiphilic structure, which may cause damage on cell membranes.…”

Section: Cytotoxicitymentioning

confidence: 92%

Formulation and cytotoxicity evaluation of new self-emulsifying multiple W/O/W nanoemulsions

Sigward¹,

Mignet²,

Rat³

et al. 2013

IJN

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Three multiple water-in-oil-in-water (W/O/W) nanoemulsions have been designed for potential inclusion of either lipophilic or hydrophilic drugs using a two-step emulsification process exclusively based on low-energy self-emulsification. The W/O primary emulsion was constituted by a blend of oil (medium chain triglyceride), a mixture (7:3) of two surfactants, and a 10% water phase. The surfactants were a mixture of Polysorbate-85/Labrasol ® , Polysorbate-85/ Cremophor ® EL or glycerol/Polysorbate-85. The final W/O/W nanoemulsions were obtained by the addition of water, with a weight ratio nanoemulsion/water of 1:2. The multiple emulsion stability was found to increase from 24 hours to 2 and 6 months with Labrasol, glycerol, and Cremophor, respectively. Cytotoxicity was found for formulations including Labrasol and Cremophor EL. The concentration of emulsion inhibiting 50% cell viability (IC 50 ) was determined using the alamarBlue ® test, giving after 24 hours of incubation, IC 50 = 10.2 mg/mL for the Labrasol formulation and IC 50 = 11.8 mg/mL for the Cremophor EL formulation. Corresponding calculated IC 50 values for surfactants were 0.51 mg/mL for Labrasol and 0.59 mg/mL for Cremophor EL. In both cases, cytotoxicity was due to an apoptotic mechanism, evidenced by chromatin condensation and P2X7 cell death receptor activation. The formulation including glycerol, investigated between 1 and 100 mg/mL concentration of nanoemulsion, did not affect cell viability. Moreover, neither chromatin condensation nor P2X7 activation was found between the 10 and 30 mg/mL final concentration of the emulsion. This last formulation would therefore be of major interest for further developments.

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Drug solubilization and in vitro toxicity evaluation of lipoamino acid surfactants

Cited by 41 publications

References 23 publications

Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study

Formulation and cytotoxicity evaluation of new self-emulsifying multiple W/O/W nanoemulsions

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