Microemulsions for topical delivery of 8-methoxsalen

Baroli, Bianca Maria; López‐Quintela, M. Arturo; Delgado‐Charro, M. Begoña; Fadda, Anna Maria; Blanco-Méndez, J.

doi:10.1016/s0168-3659(00)00309-6

Cited by 195 publications

(108 citation statements)

References 11 publications

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“…3,4 There are many studies on microemulsions as topical drug delivery vehicles, and it has been shown that microemulsion formulations have improved transdermal and dermal delivery properties. [5][6][7][8][9][10][11][12][13][14][15][16] In this study, non-ionic surfactants (Brij 58 and Span 80), which are also compatible with the other 3 classes of surfactants and retain this utility over a broad range of pH values, were used in preference, because they have minimal toxicity. 3,4 As the study aimed to examine the in vitro release of microemulsion (M) formulations, diclofenac sodium (DS) was selected as a model drug.…”

Section: Introductionmentioning

confidence: 99%

Comparison of different water/oil microemulsions containing diclofenac sodium: Preparation, characterization, release rate, and skin irritation studies

Kantarcı¹,

Özgüney²,

Karasulu³

et al. 2007

AAPS PharmSciTech

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The aim of the present study was to make a comparison of the in vitro release rate of diclofenac sodium (DS) from microemulsion (M) vehicles containing soybean oil, nonionic surfactants (Brij 58 and Span 80), and different alcohols (ethanol [E], isopropyl alcohol [I], and propanol [P]) as cosurfactant. The optimum surfactant:cosurfactant (S:CoS) weight ratios and microemulsion areas were detected by the aid of phase diagrams. Three microemulsion formulations were selected, and their physicochemical properties were examined for the pH, viscosity, and conductivity. According to the release rate of DS, M prepared with P showed the significantly highest flux value (0.059 ± 0.018 mg/cm 2 /h) among all formulations (P G .05). The conductivity results showed that DS-loaded microemulsions have higher conductivity values (18.8-20.2 microsiemens/cm) than unloaded formulations (16.9-17.9 microsiemens/cm), and loading DS into the formulation had no negative effect on system stability. Moreover, viscosity measurements were examined as a function of shear rate, and Newtonian fluid characterization was observed for each microemulsion system. All formulations had appropriate observed pH values varying from 6.70 to 6.85 for topical application. A skin irritation study was performed with microemulsions on human volunteers, and no visible reaction was observed with any of the formulations. In conclusion, M prepared with P may be a more appropriate formulation than the other 2 formulations studied as drug carrier for topical application.

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Section: Introductionmentioning

confidence: 99%

Comparison of different water/oil microemulsions containing diclofenac sodium: Preparation, characterization, release rate, and skin irritation studies

Kantarcı¹,

Özgüney²,

Karasulu³

et al. 2007

AAPS PharmSciTech

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“…Besides, cationic materials (in this case chitosan), that facilitate DNA encapsulation in microemulsions, can easily be incorporated into the formulation (Lee et al, 2010). Another advantage of W/O microemulsion is confining and protecting DNA in its inner phase (Baroli et al, 2000). In this study, Plurol oleique was selected as a lipophilic surfactant because of its ability to create transparent ME systems.…”

Section: Discussionmentioning

confidence: 99%

Preparation and characterization of non-viral gene delivery systems with pEGFP-C1 Plasmid DNA

Karagöz

Kotmakçı

Çetintaş

et al. 2018

Braz. J. Pharm. Sci.

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In recent years, non-viral delivery systems for plasmid DNA have become particularly important. They can overcome the disadvantages of viral systems such as insertional mutagenesis and unpredicted immunogenicity. Some additional advantages of non-viral gene delivery systems are; good stability, low cost, targetability, delivery of a high amount of genetic materials. The aim of the study was to develop novel non-viral nanosystems suitable for gene delivery. Two formulations were developed for this purpose: water-in-oil microemulsion (ME) and solid lipid nanoparticles (SLN). The microemulsion was composed of Peceol, Tween 80, Plurol oleique, ethanol and water. The SLN was consisting of Precirol, Esterquat-1 (EQ1), Tween 80, Lecithin, ethanol and water. Characterization studies were carried out by measuring particle size, zeta potential, viscosity and pH. TEM imaging was performed on SLN formulations. Protection against DNase I degradation was examined. Cytotoxicity and transfection efficacy of selected formulations were tested on L929 mouse fibroblast cells. Particle sizes of complexes were below 100 nm and with high positive zeta potential. TEM images revealed that SLNs are spherical. The SLN:DNA complexes have low toxicity and good transfection ability. All results showed that the developed SLN formulations can be considered as suitable non-viral gene delivery systems.

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“…Such phenomenon was also discovered by previous studies. 16,27) In the systems with low oil fraction, there is a high ratio of propylene glycol, and this relatively high ratio of cosurfactant could distribute into the oil phase, which causes the oil droplet similar to amphiphilic particles. In a dynamic equilibrium course, these droplets are incorporated into the outer phase and also dispersed as inner phase.…”

Section: Characterization and Stability Of Microemulsion Studymentioning

confidence: 99%

“…28) The high radius can be explained as a temporal, apparent and aggregated radius. 27) In an o/w system, the phenyl groups of benzyl alcohol aggregate together and the groups of -CH 2 OH are arrayed toward the outer phase. But the water molecules aggregate at the centre combined with the group of -CH 2 OH in a w/o system.…”

Section: Characterization and Stability Of Microemulsion Studymentioning

confidence: 99%

In Vitro Evaluation of Topical Microemulsion of Capsaicin Free of Surfactant

Zhang

Gao

Zhang

et al. 2008

Biological & Pharmaceutical Bulletin

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Capsaicin (8-methyl N-vanillyl-6 nonenamide), an active compound extracted from Chilli peppers, is widely used for treatment of rheumatoid arthritis, osteoarthritis, diabetic neuropathy and postherpetic neuralgia. 1) However, first pass effect of capsaicin is very high, 2) and the half-life of capsaicin after intravenous administration is only 7.06 min in rats 3) and 12.44 min in rabbits. 4) Adverse events of capsaicin mainly include burning, stinging and erythema at the application site. 5) Topical application of this drug can avoid the first-pass metabolism. Moreover, due to the long period of treatment cycle, 5) topical therapeutical systems (TTS) is very suitable for capsaicin.Microemulsion is a single optically isotropic and thermodynamically stable liquid mixture of oil, water, surfactant and cosurfactant. Due to its advantages, for example, easy making, good stability, enhancing skin permeation and protecting drug against oxidation, 6) microemulsion has become a potential TTS for both hydrophilic and hydrophobic drugs. 7) The structure of microemulsion consists of a disordered, connected surfactant monolayer separating the two solvent domains. It is "balanced" in the sense that this monolayer sheet has no preference in curving toward either of the two solvents. 8) The conditions of microemulsion formation are as follows: (1) very low interfacial tension at the water-oil interface; (2) a highly fluid interfacial surfactant film; (3) the penetration and association of the molecules of the oil phase with the interfacial surfactant film. 9) However, in a microemulsion system, there is commonly a high ratio of surfactants in the formulation, therefore, they may affect the skin barrier function and cause potential risks of irritation and toxicity in long-term application. 10,11) Furthermore, some researches have demonstrated that the increased concentration of surfactant can depress the permeation rate of drugs. [12][13][14][15] This article was intended to investigate the potential of a new microemulsion formulation without surfactant for topical drug delivery of capsaicin. Surfactant-free microemulsions were prepared in other fields, [16][17][18] but were not used in topical pharmaceuticals. The novel microemulsion was based on benzyl alcohol and short-chain alcohol. Benzyl alcohol is a potential transdermal enhancer and has an amphiphilic molecular structure, 19) which is helpful for the formation of microemulsion, 16) and can be used as oil phase in microemulsions. 20,21) Furthermore, benzyl alcohol is a commonly used drug for local anesthesia and alleviating itching, thus, it may be helpful to reduce the side-effects of capsaicin. MATERIALS AND METHODS MaterialsCapsaicin was purchased from Nanjing Tianshu Bioengineering Co., Ltd. (Nanjing, China). Benzyl alcohol (BA), propylene glycol (PG), ethanol (EA) and n-butanol were obtained from Tianjin 1st Chemical Agent Factory. Tween 80 (Polysorbate 80) was purchased from Shanghai Chemical Co., Ltd. Water was double distilled in a quartz inferior-boiling apparatu...

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Microemulsions for topical delivery of 8-methoxsalen

Cited by 195 publications

References 11 publications

Comparison of different water/oil microemulsions containing diclofenac sodium: Preparation, characterization, release rate, and skin irritation studies

Comparison of different water/oil microemulsions containing diclofenac sodium: Preparation, characterization, release rate, and skin irritation studies

Preparation and characterization of non-viral gene delivery systems with pEGFP-C1 Plasmid DNA

In Vitro Evaluation of Topical Microemulsion of Capsaicin Free of Surfactant

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