Formulation of microemulsion systems for transdermal delivery of aceclofenac

Lee, Jaehwi; Lee, Yoonjin; Kim, Jong-Seok; Yoon, Mikyeong; Choi, Young Wook

doi:10.1007/bf02977408

Cited by 65 publications

(43 citation statements)

References 12 publications

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“…The peak point in the viscosity-water content profile is denoted as the transition point of W/O to O/W microemulsion [15,16]. In this study, the peak points were only found in microemulsion systems using high HLB surfactants (i.e., Tween 20® and Labrasol®) but not in the ones using low HLB surfactants (i.e., Span 20®).…”

Section: Characterization Of the Selected Microemulsionsmentioning

confidence: 65%

Formulation of Microemulsion Systems for Dermal Delivery of Silymarin

2012

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Abstract. Silymarin is a standardized extract from Silybum marianum seeds, known for its many skin benefits such as antioxidant, anti-inflammatory, and immunomodulatory properties. In this study, the potential of several microemulsion formulations for dermal delivery of silymarin was evaluated. The pseudo-ternary phase diagrams were constructed for the various microemulsion formulations which were prepared using glyceryl monooleate, oleic acid, ethyl oleate, or isopropyl myristate as the oily phase; a mixture of Tween 20®, Labrasol®, or Span 20® with HCO-40® (1:1 ratio) as surfactants; and Transcutol® as a cosurfactant. Oil-inwater microemulsions were selected to incorporate 2% w/w silymarin. After six heating-cooling cycles, physical appearances of all microemulsions were unchanged and no drug precipitation occurred. Chemical stability studies showed that microemulsion containing Labrasol® and isopropyl myristate stored at 40°C for 6 months showed the highest silybin remaining among others. The silybin remainings depended on the type of surfactant and were sequenced in the order of: Labrasol®>Tween 20®>Span 20®. In vitro release studies showed prolonged release for microemulsions when compared to silymarin solution. All release profiles showed the best fits with Higuchi kinetics. Non-occlusive in vitro skin permeation studies showed absence of transdermal delivery of silybin. The percentages of silybin in skin extracts were not significantly different among the different formulations (p>0.05). Nevertheless, some silybin was detected in the receiver fluid when performing occlusive experiments. Microemulsions containing Labrasol® also were found to enhance silymarin solubility. Other drug delivery systems with occlusive effect could be further developed for dermal delivery of silymarin.

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Section: Characterization Of the Selected Microemulsionsmentioning

confidence: 65%

Formulation of Microemulsion Systems for Dermal Delivery of Silymarin

2012

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“…Similar solution was successfully applied to monitor the skin delivery of steroidal drugs from microemulsions. 23) Other studies also employed 40% propylene glycol solution as the receptor solution.…”

Section: Methodsmentioning

confidence: 99%

“…A 0.05 level of significance (pϽ0.05) was considered significant. The skin flux can be experimentally determined from the following equation 23) :…”

Section: Methodsmentioning

confidence: 99%

Development and Characterization of Eucalyptol Microemulsions for Topic Delivery of Curcumin

Liu

Chang

2011

Chem. Pharm. Bull.

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Transdermal drug delivery has many advantages over other administration routes: for example, avoidance of hepatic metabolism, convenient administration for the patient, and easy withdrawal of treatment if necessary. Despite extensive studies of transdermal drug delivery, only a few drug formulations are commercially available. 1) One of the reasons for this is the permeation barrier by the stratum corneum to exogenous substances. Skin penetration enhancement can be chieved using appropriate physical and chemical means to overcome the skin's barrier function. Chemical penetration enhancers such as fatty acids, fatty esters, surfactants, and terpenes have received considerable attention due to their low cost, ease of use, safety, and efficacy.2) Terpenes are lipophilic ingredients of essential oils which can disturb intracellular lipids and increase the fluidization of the stratum corneum, thereby enhancing drug penetration.3) Eucalyptus oil (eucalyptol, a terpene from trees) was adopted as the oil phase to design transdermal vehicles for various drugs including estradiol, progesterone, cyproterone acetate, finasteride, and hydrocortisone. 4,5) Investigations of microemulsions composed by eucalyptus/peppermint oil and water were reported to have many potential applications.6,7) Lipid-based systems such as microemulsions, nanoemulsions, solid lipid nanoparticles, and liposomes were recently applied to transdermal drug delivery. 8) Microemulsions are single phase, optically isotropic nano-structured solutions composed of a surfactant, cosurfactant, oil, and water. The ability of microemulsions to deliver drugs through a transdermal route in a controlled manner was recently reviewed. 9) Advantages of microemulsion delivery systems include spontaneous formation, easy preparation, low viscosity, high surface area, high drug solubilization, optical transparency, and thermodynamic stability.10) Microemulsions were applied to deliver different lipophilic drugs including fluconazole, 11) penciclovir, 12) quercetin, 13) diclofenac, 14) and progesterone 15) through the transdermal route. Those in vitro and in vivo studies demonstrated that lipophilic drugs incorporated into microemulsions can efficiently penetrate the skin.Curcumin and curcuminoids are yellow polyphenolic compounds extracted from the spice turmeric (Curcuma longa). Recent studies demonstrated that curcumin has the potential to protect skin by reducing inflammation through nuclear factor (NF)-kB inhibition and to reduce wound-healing time by improving collagen deposition.16) Curcumin can regenerate muscle cells after traumatic injury by modulating NF-kB activity within muscle tissues. Additionally, the use of curcumin for the chemoprevention and treatment of various skin diseases like scleroderma, psoriasis, and skin cancer was reviewed.16) Patel et al. demonstrated that curcumin-containing films have good anti-inflammatory activity against carrageenan-induced edema in rats similar to a standard formulation through the transdermal route.17) Those studies sugg...

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“…Zeta potential and the dynamic light scattering (DLS) of the microemulsions were analysed in triplicate at 25 o C [13].…”

Section: Zeta-potential Measurementmentioning

confidence: 99%