Influence of lipophilic surfactant on the release kinetics of water-soluble molecules entrapped in a W/O/W multiple emulsion

Jager-Lezer, N.; Terrisse, I.; Bruneau, F.; Tokgöz, Serkan; Ferreira, Lucas Antônio Miranda; Clausse, Danièle; Seiller, M.; Grossiord, J. L.

doi:10.1016/s0168-3659(96)01507-6

Cited by 120 publications

(93 citation statements)

References 15 publications

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“…This swelling of the droplets was expected, due to the unbalanced osmotic pressure gradient, promoting a migration of water from the outer to the inner water phase. Similar studies performed on hypo-osmotic W/O/W emulsions have earlier reported a swelling-mediated breakdown/rupturing of the samples, contributing to release of the encapsulated substance (Hattrem, et al, 2014;JagerLezer, et al, 1997). For the present system, a similar explanation seems reasonable, as a significant decrease in the encapsulation efficiency for the hypo-osmotic samples are observed during the first 24 hours, with a corresponding increase in droplet size.…”

Section: Resultssupporting

confidence: 89%

Ibuprofen-in-cyclodextrin-in-W/O/W emulsion – Improving the initial and long-term encapsulation efficiency of a model active ingredient

Hattrem

Kristiansen

Aachmann

et al. 2015

International Journal of Pharmaceutics

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A challenge with formulating water-in-oil-in-water (W/O/W) emulsions is the uncontrolled release of encapsulated compound prior to application. Pharmaceuticals and nutraceuticals usually have amphipathic nature, which may contribute to leakage of the active ingredient. In the present study, cyclodextrins (CyDs) were used to impart a change in the relative polarity and size of a model compound (ibuprofen) by the formation of inclusion complexes. Various inclusion complexes (2-hydroxypropyl (HP)-β-CyD-, α-CyD-and -CyD-ibuprofen) were prepared and presented within W/O/W emulsions and the initial and long-term encapsulation efficiency was investigated. HP-β-CyD-ibuprofen provided the highest retention of ibuprofen in comparison to a W/O/W emulsion with unassociated ibuprofen confined within the inner water phase, with a 4 fold increase in the encapsulation efficiency. An improved, although lower encapsulation efficiency was obtained for the inclusion complex -CyD-ibuprofen in comparison to HP-β-CyD-ibuprofen, while α-CyDibuprofen had similar encapsulation efficiency as unassociated ibuprofen. The lower encapsulation efficiency of ibuprofen in combination with α-CyD and γ-CyD was attributed to a lower association constant for the γ-CyD-ibuprofen inclusion complex and the ability of α-CyD to form inclusion complexes with fatty acids. For the W/O/W emulsion prepared with HP--CyD-ibuprofen, the highest retention of ibuprofen was obtained at hyper-and iso-osmotic conditions and by using an excess molar ratio of CyD in comparison to ibuprofen. In the last part of the study it was suggested that the chemical modification of the HP--CyD molecule did not influence the encapsulation of ibuprofen, as similar encapsulation efficiency was obtained for an inclusion complex prepared with mono-1-glucose--CyD.

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Section: Resultssupporting

confidence: 89%

Ibuprofen-in-cyclodextrin-in-W/O/W emulsion – Improving the initial and long-term encapsulation efficiency of a model active ingredient

Hattrem

Kristiansen

Aachmann

et al. 2015

International Journal of Pharmaceutics

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“…The possible explanation may be that some water in the internal aqueous phase leaked into the external aqueous phase due to the breakdown of the oil globules, leading to the underestimation of the water transport rates. JagerLezer et al (20) reported no net water transfer between the two aqueous phases under iso-osmotic conditions, whereas Garti and Romano-Pariente (19) and Kinugasa et al (23) found that water transport rates decrease with decreasing osmotic pressure gradients. However, it still remains unclear how the osmotic pressure gradients affect water transport rates, especially when the water migration is controlled by different mechanisms as described above.…”

Section: Introductionmentioning

confidence: 99%

Effects of Osmotic Pressure on Water Transport in W1/O/W2 Emulsions

Wen

Papadopoulos

2001

Journal of Colloid and Interface Science

100

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“…Microscopic analysis has shown the presence of the multiple characters. The conductivity of all formulations showed a high entrapment (over 90%); this means a lower breakdown rate and better stability (Özer et al 2000;Jager-Lezer et al 1997). Both the thermal stability tests performed at 25±1…”

Section: Characterization Of Multiple Emulsionsmentioning

confidence: 95%

W/O/W Multiple Emulsions Containing Nitroimidazole Derivates for Vaginal Delivery

et al. 2007

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The aim of our study was to formulate a stable multiple emulsions containing two nitroimidazole derivates, metronidazole (MT) and ornidazole (OR), for vaginal therapy. MT and OR were located internal and external phases of multiple emulsion, respectively, and the in vitro release studies were realized in phosphate (pH 7) and lactate buffer (pH 4.5) solutions to investigate better the effect of pH and location of active substance on the release. The imaging studies were realized in rabbits following labeling MT and OR with Technethium-99m ( 99m Tc) to evaluate the in vivo absorption characteristics. The percentage of MT and OR released from the multiple emulsions in alkaline media were 3.2-and 2.8-fold greater than that observed in acidic media, respectively, when they were introduced in the internal phase of the multiple emulsions. The absorption rate of MT from vaginal epithelium was faster than OR. We observed that especially in alkaline medium a high release was found that was convenient for the vaginal infections seen in the alkaline pH. We concluded that W/O/W multiple emulsions were locally effective in vagina and they could be introduced as a new drug carrier system for vaginal delivery.

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Influence of lipophilic surfactant on the release kinetics of water-soluble molecules entrapped in a W/O/W multiple emulsion

Cited by 120 publications

References 15 publications

Ibuprofen-in-cyclodextrin-in-W/O/W emulsion – Improving the initial and long-term encapsulation efficiency of a model active ingredient

Ibuprofen-in-cyclodextrin-in-W/O/W emulsion – Improving the initial and long-term encapsulation efficiency of a model active ingredient

Effects of Osmotic Pressure on Water Transport in W1/O/W2 Emulsions

W/O/W Multiple Emulsions Containing Nitroimidazole Derivates for Vaginal Delivery

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