Sucrose Laurate Gels as a Percutaneous Delivery System for Oestradiol in Rabbits

Vermeire, An; Muynck, C. De; Vandenbossche, Geert; Eechaute, W.; Geerts, Marie-Louise; Remon, Jean Paul

doi:10.1111/j.2042-7158.1996.tb05955.x

Cited by 17 publications

(9 citation statements)

References 7 publications

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“…In addition, their anti-tumoral (Nishikawa et al, 1976), anti-bacterial (Kato and Arima, 1971), and insecticidal (Chortyk et al, 1996) properties have also been reported, thus indicating their great versatility. Sucrose laurate is especially suitable as an absorption enhancer for transdermal and topical drug delivery (Vermeire et al, 1996), being nonirritating and rapidly degraded.…”

Section: Introductionmentioning

confidence: 99%

Lipase-catalyzed regioselective acylation of sucrose in two-solvent mixtures

Ferrer

Cruces

Bernabé

et al. 1999

Biotechnol. Bioeng.

145

114

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Section: Introductionmentioning

confidence: 99%

Lipase-catalyzed regioselective acylation of sucrose in two-solvent mixtures

Ferrer

Cruces

Bernabé

et al. 1999

Biotechnol. Bioeng.

145

114

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“…10) Some sugar esters act as percutaneous absorption enhancers. It has been reported that sucrose stearate and sucrose laurate increase percutaneous absorption of bromhexine in rats 11) and oestradiol in rabbits, 12) respectively. The percutaneous absorption of diltiazem and hydromorphone are also aided by some sugar esters.…”

mentioning

confidence: 99%

Effect of Sucrose Fatty Acid Esters on Transdermal Permeation of Lidocaine and Ketoprofen

Okamoto

Sakai

Danjo

2005

Biological & Pharmaceutical Bulletin

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Skin has many advantages as a site for local and systemic drug administration. However, the barrier properties of the outermost layer, the stratum corneum, have limited the number of successful transdermal dosage forms developed thus far. One of the strategies for overcoming this problem is temporary local reduction of the barrier function of the stratum corneum with the aid of a percutaneous absorption enhancer.Sucrose fatty acid esters (sugar esters) are nonionic surfactants with sucrose as the polar head group and one or several fatty acid chains as the lipophilic moiety. Some of them are legally approved as food additives due to their high safety 1) and are registered as pharmaceutical excipients in Japan, USA, Canada, Australia, and New Zeeland.2) Sugar esters have low irritancy to the skin and eyes. 1) There have been several reports or patents about utilizing sugar esters as additives for drug formulations. Some sugar esters enhance gastrointestinal absorption of elastase 3) and blactam antibiotics.4) The nasal mucosal absorption of peptides such as calcitonin, 5) interferon, 6) and a-human atrial natriuretic polypeptide 7) are increased by sucrose laurate or sucrose stearate. Sucrose palmitate enhances the absorption of calcitonin from the oral mucosa 8) and gingiva 9) in rats. Ganem-Quintanar et al. examined the effect of sucrose stearate, oleate, palmitate, and laurate on the permeation of lidocaine hydrochloride through excised pig palate and cheek and reported that only sucrose laurate acted as an absorption enhancer.10) Some sugar esters act as percutaneous absorption enhancers. It has been reported that sucrose stearate and sucrose laurate increase percutaneous absorption of bromhexine in rats 11) and oestradiol in rabbits, 12) respectively. The percutaneous absorption of diltiazem and hydromorphone are also aided by some sugar esters. 13,14) Nakada et al. examined the effect of more than 10 sugar esters with HLB ranging 2 to 16 on the absorption of calcitonin from oral mucosa in rats.8) An enhancing effect was found for sugar esters with HLB values ranging from 11 to 16. However, the effect of the length of the fatty acid chain and HLB of sugar esters on their activity as percutaneous absorption enhancers has not been reported.In the present study, we selected six sugar esters with HLB 5-16 and evaluated their effect on percutaneous drug permeation in in vitro experiments using excised hairless mouse skin. We employed lidocaine (LC, pK a ϭ7.9) 15) and ketoprofen (KP, pK a ϭ4.0) 16) as model basic and acidic drugs, respectively. The drugs were dissolved in buffer solutions with several pHs so that we could evaluate the effect of the sugar esters on the percutaneous permeation of ionized and unionized drug species.It has been reported that sugar esters form micelles in water and in an organic solvent.17) The micelles would affect the thermodynamic properties of a penetrant in a vehicle. To examine the effect of sugar esters on skin permeability and to minimize the effect on vehicle or interaction wi...

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“…Sucrose is a biocompatible and biodegradable organic compound [43][44][45][46][47][48]. Sucrose gel is formed when 400 mg of the sucrose is mixed with 10 ml of the deionized water and can be completely dissolved in water within 1 h at room temperature.…”

Section: Materials Properties Of the Sucrose Gel And Polyimidementioning

confidence: 99%

Partially flexible MEMS neural probe composed of polyimide and sucrose gel for reducing brain damage during and after implantation

Jeon

Cho

Kim

et al. 2014

J. Micromech. Microeng.

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This paper presents a flexible microelectromechanical systems (MEMS) neural probe that minimizes neuron damage and immune response, suitable for chronic recording applications. MEMS neural probes with various features such as high electrode densities have been actively investigated for neuron stimulation and recording to study brain functions. However, successful recording of neural signals in chronic application using rigid silicon probes still remains challenging because of cell death and macrophages accumulated around the electrodes over time from continuous brain movement. Thus, in this paper, we propose a new flexible MEMS neural probe that consists of two segments: a polyimide-based, flexible segment for connection and a rigid segment composed of thin silicon for insertion. While the flexible connection segment is designed to reduce the long-term chronic neuron damage, the thin insertion segment is designed to minimize the brain damage during the insertion process. The proposed flexible neural probe was successfully fabricated using the MEMS process on a silicon on insulator wafer. For a successful insertion, a biodegradable sucrose gel is coated on the flexible segment to temporarily increase the probe stiffness to prevent buckling. After the insertion, the sucrose gel dissolves inside the brain exposing the polyimide probe. By performing an insertion test, we confirm that the flexible probe has enough stiffness. In addition, by monitoring immune responses and brain histology, we successfully demonstrate that the proposed flexible neural probe incurs fivefold less neural damage than that incurred by a conventional silicon neural probe. Therefore, the presented flexible neural probe is a promising candidate for recording stable neural signals for long-time chronic applications.

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Sucrose Laurate Gels as a Percutaneous Delivery System for Oestradiol in Rabbits

Cited by 17 publications

References 7 publications

Lipase-catalyzed regioselective acylation of sucrose in two-solvent mixtures

Lipase-catalyzed regioselective acylation of sucrose in two-solvent mixtures

Effect of Sucrose Fatty Acid Esters on Transdermal Permeation of Lidocaine and Ketoprofen

Partially flexible MEMS neural probe composed of polyimide and sucrose gel for reducing brain damage during and after implantation

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