Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology

Huang, Chih-Hsin; Tsai, Ming-Jun; Lin, Yu–Hsuan; Fu, Yaw-Sya; Huang, Yaw‐Bin; Tsai, Yi‐Hung; Wu, Pao‐Chu

doi:10.2147/ijn.s43474

Cited by 20 publications

(10 citation statements)

References 50 publications

(59 reference statements)

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“…IPM (molecular volume 528.2 g/cm 3 ) based microemulsion system showed a smaller area of microemulsion as compared to a system based on OA (molecular volume 523.9 g/cm 3 ). This result is in accordance with literature reported by [13] that also indicate the smaller area of microemulsion region when used PEG 400 as a co-surfactant, IPM as an oil phase and Brij 30/Brij 35 (HLB ~11.1) as a surfactant. Meanwhile, the result of OA based system is in good agreement with the previous study conducted by [14] that shows stable microemulsion system consisting of oleic acid (oil phase), Tween 20 (surfactant), PEG 400 (co-surfactant), water (aqueous phase).…”

Section: Effect Of Oa and Ipm On The System Of Brij 97/peg 400/watersupporting

confidence: 93%

Study on the Effect of Oil Phase and Co-Surfactant on Microemulsion Systems

Sisak

Daik²,

Ramli³

2017

MJAS

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The purpose of the present study was to investigate the effect of different oil and chain lengths of co-surfactant on microemulsion region. Oleic acid and isopropyl myristate were used as the oil phase, transcutol, polyethylene glycol 400 (PEG 400) and propylene glycol as co-surfactant and Brij 97 as a surfactant. From the ternary phase diagrams, isopropyl myristate based system is more feasible oil phase to formulate microemulsion compared to oleic acid based system. Moreover, transcutol (medium chain length) is the most suitable co-surfactant to blend with a single-chain surfactant, Brij 97 in order to have a high stability and a large area of microemulsion region.Keywords: microemulsion, oleic acid, isopropyl myristate, transcutol, propylene glycol Abstrak Kajian ini bertujuan untuk mengkaji kesan minyak yang berbeza dan panjang rantai ko-surfaktan terhadap rantau mikroemulsi. Asid oleik dan isopropil miristat telah digunakan sebagai fasa minyak, transcutol, polietilena glikol 400 (PEG 400) dan propilena glikol sebagai ko-surfaktan dan Brij 97 sebagai surfaktan. Berdasarkan rajah fasa tenari, sistem berasaskan isopropil miristat adalah fasa minyak yang lebih sesuai untuk membentuk mikroemulsi berbanding sistem berasaskan asid oleik. Selain itu, transcutol yang berantai sederhana panjang adalah ko-surfaktan yang sesuai untuk diformulasikan bersama surfaktan rantai tunggal, Brij 97 yang memberikan rantau kawasan mikroemulsi yang besar dengan kestabilan yang tinggi.Kata kunci: mikroemulsi, asid oleik, isopropil miristat, transcutol, propilena glikol Introduction Microemulsions are versatile systems and can be used in various applications such as for cutting oils, corrosion inhibitors, biotechnology, fuels, coating and textile finishing, food industries, lubricants, and also in pharmaceuticals [1]. Microemulsions have generated extensive interest over the years as potential drug delivery systems, especially for the delivery of the hydrophilic and lipophilic drug [2]. It is because of its several characteristics such as improved drug solubilization, longer shelf life, ease of preparation and improvement of bioavailability of poorly soluble drugs [3]. It is also can be used to deliver drugs via several routes and making them as a promising dermal delivery of the drug through an efficient route of drug administration [4].

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Section: Effect Of Oa and Ipm On The System Of Brij 97/peg 400/watersupporting

confidence: 93%

Study on the Effect of Oil Phase and Co-Surfactant on Microemulsion Systems

Sisak

Daik²,

Ramli³

2017

MJAS

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“…It is easy to decrease the flux of ESP by directly reducing its content, which in turn brings about the problem of dose depletion for long-acting transdermal patches. Thus, we cannot reduce the dose delivered or use a smaller patch (6). The flux of ESP should be controlled and the cumulative penetration amounts should meet the requirement of the long-acting ESP transdermal patch.…”

Section: Introductionmentioning

confidence: 99%

Regulating the Skin Permeation Rate of Escitalopram by Ion-pair Formation with Organic Acids

et al. 2016

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Abstract. In order to regulate the skin permeation rate (flux) of escitalopram (ESP), ion-pair strategy was used in our work. Five organic acids with different physicochemical properties, benzoic acid (BA), ibuprofen (IB), salicylic acid (SA), benzenesulfonic acid (BSA), and p-aminobenzoic acid (PABA), were employed as counter-ions to regulate the permeation rate of ESP across the rabbit abdominal skin in vitro. The interaction between ESP and organic acids was characterized by FTIR and 13 C NMR spectroscopy. Results showed that all organic acids investigated in this study performed a controlling effect on ESP flux. To further analyze the factors concerned with the permeation capability of ESP-acid complex, a multiple linear regression model was used. It is concluded that the steady-state flux (J) of ESP-acid complexes had a positive correlation with log K o/w (the n-octanol/water partition coefficient of ion-pair complex) and pK a (the acidity of organic acid counter-ion), but a negative correlation with MW (the molecular weight of ionpair complex). The logK o/w of ion-pair complex is the primary one in all the factors that influence the skin permeation rate of ESP. The results demonstrated that organic acid with appropriate physicochemical properties can be considered as suitable candidate for the transdermal drug delivery of escitalopram.

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“…Third, there was increased adhesion surface contact between the NE vesicles and the absorption site. 34 Further, transdermal application of ACV-NE hydrogel on the rat skin was significantly different than other formulations at all of the time intervals (P,0.001); except at the first hour with Figure 6). Moreover, enhancement of the steady-state flux, diffusion coefficient, and permeability coefficient with ACV-NE hydrogel, compared with the raw gel and marketed cream, were essential to improving the bioavailability of this formulation.…”

Section: Pharmacokinetics Studies Of Acv-ne Hydrogelmentioning

confidence: 81%

Utilization of nanotechnology to enhance percutaneous absorption of acyclovir in the treatment of herpes simplex viral infections

Al-Subaie¹,

Hosny²,

El-Say³

et al. 2015

IJN

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This study aimed to formulate an optimized acyclovir (ACV) nanoemulsion hydrogel in order to provide a solution for the slow, variable, and incomplete oral drug absorption in patient suffering from herpes simplex viral infection. Solubility of ACV in different oils, surfactants, and cosurfactants was explored utilizing a cubic model mixture design to obtain a nanoemulsion with minimum globule size. Preparation of an optimized ACV nanoemulsion hydrogel using a three-factor, three-level Box–Behnken statistical design was conducted. The molecular weight of chitosan (X 1 ), percentage of chitosan (X 2 ), and percentage of Eugenol as a skin permeation enhancer (X 3 ) were selected to study their effects on hydrogel spreadability (Y 1 ) and percent ACV permeated through rat skin after 2.5 hours (Y 2 ). A pharmacokinetic study of the optimized ACV nanoemulsion hydrogel was conducted in rats. Mixtures of clove oil and castor oil (3:1 ratio), Tween 80 and Span 80 (3:1 ratio), and propylene glycol and Myo-6V (3:1 ratio) were selected as the oil, surfactant, and cosurfactant phases, respectively. Statistical analysis indicated that the molecular weight of chitosan has a significant antagonistic effect on spreadability, but has no significant effect on the percent ACV permeated. The percentage of chitosan also has a significant antagonistic effect on the spreadability and percent ACV permeated. On the other hand, the percentage of Eugenol has a significant synergistic effect on percent ACV permeated, with no effect on spreadability. The ex vivo study demonstrated that the optimized ACV nanoemulsion hydrogel showed a twofold and 1.5-fold higher permeation percentage than the control gel and marketed cream, respectively. The relative bioavailability of the optimized ACV nanoemulsion hydrogel improved to 535.2% and 244.6% with respect to the raw ACV hydrogel and marketed cream, respectively, confirming improvement of the relative bioavailability of ACV in the formulated nanoemulsion hydrogel.

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Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology

Cited by 20 publications

References 50 publications

Study on the Effect of Oil Phase and Co-Surfactant on Microemulsion Systems

Study on the Effect of Oil Phase and Co-Surfactant on Microemulsion Systems

Regulating the Skin Permeation Rate of Escitalopram by Ion-pair Formation with Organic Acids

Utilization of nanotechnology to enhance percutaneous absorption of acyclovir in the treatment of herpes simplex viral infections

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