AOT water-in-oil microemulsions as a penetration enhancer in transdermal drug delivery of 5-fluorouracil

Gupta, R.; Jain, Swantrant K.; Varshney, Manoj

doi:10.1016/j.colsurfb.2004.09.008

Cited by 100 publications

(64 citation statements)

References 43 publications

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“…6 There has been increased interest during recent years in the use of topical vehicle systems that could modify drug permeation through the skin using permeation enhancers, but use of these chemical enhancers may be harmful, especially in chronic application, as many of them are irritants. 4,7 Therefore, it is desirable to develop a topical vehicle system without chemical enhancers to facilitate drug permeation through the skin. One of the most promising techniques for enhancement of skin permeation of drugs is lipid-based nanocarrier delivery.…”

Section: Introductionmentioning

confidence: 99%

Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

Rajinikanth¹,

Chellian²

2016

IJN

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The aim of this study was to develop a nanostructured lipid carrier (NLC)-based hydrogel and study its potential for the topical delivery of 5-fluorouracil (5-FU). Precirol ® ATO 5 (glyceryl palmitostearate) and Labrasol ® were selected as the solid and liquid lipid phases, respectively. Poloxamer 188 and Solutol ® HS15 (polyoxyl-15-hydroxystearate) were selected as surfactants. The developed lipid formulations were dispersed in 1% Carbopol ® 934 (poly[acrylic acid]) gel medium in order to maintain the topical application consistency. The average size, zeta potential, and polydispersity index for the 5-FU-NLC were found to be 208.32±8.21 nm, −21.82±0.40 mV, and 0.352±0.060, respectively. Transmission electron microscopy study revealed that 5-FU-NLC was <200 nm in size, with a spherical shape. In vitro drug permeation studies showed a release pattern with initial burst followed by sustained release, and the rate of 5-FU permeation was significantly improved for 5-FU-NLC gel (10.27±1.82 μg/cm 2 /h) as compared with plain 5-FU gel (2.85±1.12 μg/cm 2 /h). Further, skin retention studies showed a significant retention of 5-FU from the NLC gel (91.256±4.56 μg/cm 2 ) as compared with that from the 5-FU plain gel (12.23±3.86 μg/cm 2 ) in the rat skin. Skin irritation was also significantly reduced with 5-FU-NLC gel as compared with 5-FU plain gel. These results show that the prepared 5-FU-loaded NLC has high potential to improve the penetration of 5-FU through the stratum corneum, with enormous retention and with minimal skin irritation, which is the prerequisite for topically applied formulations.

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Section: Introductionmentioning

confidence: 99%

Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

Rajinikanth¹,

Chellian²

2016

IJN

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“…It has been reported that the permeation of 5-fluorouracil increased significantly with the increase of water concentration in a water in oil (W/O) microemulsion (Gupta et al, 2005). It might be due to the increase of hydration level of SC and fluidization of lipid alkyl chain in SC, which could facilitate the permeation of drug through skin, but in our studied microemulsions (IPM/labrasol/plurol oleique ® /water), the transdermal permeation of LP decreases with the increase of water concentration.…”

Section: In Vitro Skin Permeation Studymentioning

confidence: 99%

“…Isopropyl myristate (IPM) is commonly used in cosmetics and is well-tolerated. It has been used as the oil phase in microemulsion producing no irritation on albino mice (Gupta et al, 2005). It has been reported that caprylocaproyl macrogolglycerides with IPM as oil phase could form large microemulsion area in their phase diagram (Choi et al, 1997).…”

Section: Introductionmentioning

confidence: 99%

Investigation of microemulsion system for transdermal delivery of ligustrazine phosphate

Cui¹,

Li²,

Gu³

et al. 2011

Afr. J. Pharm. Pharmacol.

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Ligustrazine phosphate is commonly used as an efficient drug to treat a variety of cardiovascular disorders with frequent administration for a short biological half-life. The purpose of the present study was to investigate a microemulsion system for transdermal delivery of ligustrazine phosphate for the convenient, efficient and safe administration. The existence regions of microemulsions containing isopropyl myristate, labrasol, plurol oleique ® and water were investigated in pseudo-ternary phase diagrams, according to which microemulsion vehicles were prepared to observe average diameter, pH value, stability and evaluate respective effect of each component on percutaneous delivery in vitro. The prepared microemulsions had average diameters ranging from 32.1 to 108.7 nm, mild pH values and suitable stability. The optimized microemulsion with permeation flux of 41.01 g/cm 2 /h across rat skin in vitro, showed no obvious irritation on back skin of rabbits. The results indicated that the studied microemulsion system might be a promising vehicle for transdermal delivery of ligustrazine phosphate.

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“…These results showed that the Gibbs free energy of nanoemulsion formulation may rely on the extent of which the surfactants and co-surfactant passively reduce the interfacial tension of the w/o interface and the variation in dispersion entropy. 13,26,27 Therefore, several nanoemulsions, which appeared clear and transparent, were selected from the phase diagram constructed by the S mix,1 1:2, and each combination was further examined for its water content, particle size, PDI, and in vitro membrane permeability (data not shown). The optimum w/o primary emulsion was composed of 21.4% aqueous phase (23.36% OXA or 67.52% OXA/DCK complex with 23.36% 5-FU), 50% mixture of Labrasol and Transcutol HP (1:2, w/w), and 28.6% Capryol 90.…”

Section: Pseudo-ternary Phase Diagrams and Preparation Of Drug-loadedmentioning

confidence: 99%

Multiple nanoemulsion system for an oral combinational delivery of oxaliplatin and 5-fluorouracil: preparation and in vivo evaluation

Pangeni¹,

Choi²,

Jeon³

et al. 2016

IJN

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AOT water-in-oil microemulsions as a penetration enhancer in transdermal drug delivery of 5-fluorouracil

Cited by 100 publications

References 43 publications

Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

Investigation of microemulsion system for transdermal delivery of ligustrazine phosphate

Multiple nanoemulsion system for an oral combinational delivery of oxaliplatin and 5-fluorouracil: preparation and in vivo evaluation

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