Formulation, Characterization, and Clinical Evaluation of Microemulsion Containing Clotrimazole for Topical Delivery

Hashem, Fahima; Shaker, Dalia S.; Ghorab, Mahmoud M.; Nasr, Mohamed; Ismail, Aliaa

doi:10.1208/s12249-011-9653-7

Cited by 106 publications

(51 citation statements)

References 36 publications

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“…The mean particle size of ME slightly increased after storage. As reported, this might be caused by the high free energy of interfacial film together with some interactions and resulted in temporal aggregation of droplets (37)(38)(39). The selected ME was o/w type, and this was in accordance with previous studies.…”

Section: Discussionsupporting

confidence: 86%

Microemulsion-Based Oxyresveratrol for Topical Treatment of Herpes Simplex Virus (HSV) Infection: Physicochemical Properties and Efficacy in Cutaneous HSV-1 Infection in Mice

et al. 2012

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Abstract. The physicochemical properties of the optimized microemulsion and the permeating ability of oxyresveratrol in microemulsion were evaluated, and the efficacy of oxyresveratrol microemulsion in cutaneous herpes simplex virus type 1 (HSV-1) infection in mice was examined. The optimized microemulsion was composed of 10% w/w of isopropyl myristate, 35% w/w of Tween 80, 35% w/w of isopropyl alcohol, and 20% w/w of water. The mean particle diameter was 9.67±0.58 nm, and the solubility of oxyresveratrol in the microemulsion was 196.34±0.80 mg/ml. After accelerated and long-term stability testing, the microemulsion base and oxyresveratrol-loaded microemulsion were stable. The cumulative amount of oxyresveratrol permeating through shed snake skin from microemulsion at 6 h was 93.04 times compared to that of oxyresveratrol from Vaseline, determined at 20% w/w concentration. In cutaneous HSV-1 infection in mice, oxyresveratrol microemulsion at 20%, 25%, and 30% w/w, topically applied five times daily for 7 days after infection, was significantly effective in delaying the development of skin lesions and protecting from death (p<0.05) compared with the untreated control. Oxyresveratrol microemulsion at 25% and 30% w/w was significantly more effective than that of 30% w/w of oxyresveratrol in Vaseline (p<0.05) and was as effective as 5% w/w of acyclovir cream, topically applied five times daily (p>0.05). These results demonstrated that topical oxyresveratrol microemulsion at 20-30% w/w was suitable for cutaneous HSV-1 mouse infection.

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Section: Discussionsupporting

confidence: 86%

Microemulsion-Based Oxyresveratrol for Topical Treatment of Herpes Simplex Virus (HSV) Infection: Physicochemical Properties and Efficacy in Cutaneous HSV-1 Infection in Mice

et al. 2012

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“…In assessing the kinetics of the in vitro release of PB, ME50 obtained an amount of PB 4.8 times greater in 24 h (17.39 ± 3.13 mg.cm -1 ) than EM50 (3.84 ± 1.12 mg.cm -1 ), with p=0.0003 for the point 24 h ( Figure 5). This result was in accordance with the literature, considering that the ME is capable of increasing the drug release system (Hashem et al, 2011;Kreilgaard, 2002). Thus, the ME provides benefits, including increased solubility and absorption of drugs, and the possibility of modifying pharmacokinetic parameters, decreasing toxicity and increasing its clinical efficacy (Formariz et al, 2005;Klein, 2007).…”

Section: Kinetics Of the In Vitro Release Of Pb In Mesupporting

confidence: 89%

Phenobarbital loaded microemulsion: development, kinetic release and quality control

Figueiredo

Neves

Silva

et al. 2016

Braz. J. Pharm. Sci.

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This study aimed to obtain and characterize a microemulsion (ME) containing phenobarbital (PB). The PB was incorporated in the proportion of 5% and 10% in a microemulsion system containing Labrasol ® , ethanol, isopropyl myristate and purified water. The physicochemical characterization was performed and the primary stability of the ME was evaluated. An analytical method was developed using spectrophotometry in UV λ = 242 nm. The kinetics of the in vitro release (Franz model) of the ME and the emulsion (EM) containing PB was evaluated. The incorporation of PB into ME at concentrations of 5 and 10% did not change pH and resistance to centrifugation. There was an increase in particle size, a decrease of conductivity and a change in the refractive index in relation to placebo ME. The ME remained stable in preliminary stability tests. The analytical method proved to be specific, linear, precise, accurate and robust. Regarding the kinetics of the in vitro release, ME obtained an in vitro release profile greater than the EM containing PB. Thus, the obtained ME has a potential for future transdermal application, being able to compose a drug delivery system for the treatment of epilepsy.Uniterms: Microemulsion/physicochemical characterization. Microemulsion/In vitro release. Phenobarbital/microemulsion system/evaluation. Nanotechnology.O objetivo deste trabalho foi obter e caracterizar uma microemulsão (ME) contendo fenobarbital (FEN). O FEN foi incorporado na proporção de 5% e 10% em um sistema microemulsionado composto por labrasol ® , etanol, miristato de isopropila e água purificada. Foi realizada a caracterização físico-química e avaliada a estabilidade preliminar da ME. Desenvolveu-se um método analítico por espectrofotometria em UV λ = 242 nm. Foi avaliada a cinética de liberação in vitro (em modelo de Franz) da ME e da emulsão (EM) contendo FEN. A incorporação do FEN em ME nas concentrações de 5 e 10% não alterou o pH e a resistência à centrifugação. Houve aumento do tamanho da partícula, redução da condutividade e alteração do índice de refração em relação à ME placebo. A ME manteve-se estável nos ensaios de estabilidade preliminar. O método analítico demonstrou ser específico, linear, preciso, exato e robusto. Na cinética de liberação in vitro, a ME obteve um perfil de liberação in vitro superior a EM contendo FEN. Desta forma, a ME obtida tem potencial para uma futura aplicação transdérmica, podendo compor um sistema de liberação de fármacos para tratamento da epilepsia.Uniterms: Microemulsão/caracterização físico-química. Microemulsão/cinética de liberação in vitro. Fenobarbital/sistema microemulsionado/avaliação. Nanotecnologia.

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“…We have hypothesized that surfactant plays major role in skin permeation of FNS when the drug is applied as topical formulation of MO-based LCN. Polyoxyethylated nonionic surfactants have been widely utilized in the preparation of microemulsion, self-emulsifying system, and solid lipid nanoparticles (22)(23)(24). Moreover, these surfactants have shown to enhance skin permeation of drugs such as terbinafine and interferon alpha (24,25).…”

Section: Introductionmentioning

confidence: 99%

Enhanced Topical Delivery of Finasteride Using Glyceryl Monooleate-Based Liquid Crystalline Nanoparticles Stabilized by Cremophor Surfactants

et al. 2013

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Abstract. The aim of this study was to investigate the capability of two surfactants, Cremophor RH 40 (RH) and Cremophor EL (EL), to prepare liquid crystalline nanoparticles (LCN) and to study its influence on the topical delivery of finasteride (FNS). FNS-loaded LCN was formulated with the two surfactants and characterized for size distribution, morphology, entrapment efficiency, in vitro drug release, and skin permeation/retention. Influence of FNS-loaded LCN on the conformational changes on porcine skin was also studied using attenuated total reflectance Fourier-transform infrared spectroscopy. Transmission electron microscopical image confirmed the formation of LCN. The average particle size of formulations was in the range of 165.1-208.6 and 153.7-243.0 nm, respectively. The formulations prepared with higher surfactant concentrations showed faster release and significantly increased skin permeation. Specifically, LCN prepared with RH 2.5% presented higher permeation flux (0.100± 0.005 μgcm −2 h −1 ) compared with lower concentration (0.029±0.007 μgcm −2 h −1 ). Typical spectral bands of lipid matrix of porcine skin were shifted to higher wavenumber, indicating increased degree of disorder of the lipid acyl chains which might cause fluidity increase of stratum corneum. Taken together, Cremophor surfactants exhibited a promising potential to stabilize the LCN and significantly augmented the skin permeation of FNS.

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Formulation, Characterization, and Clinical Evaluation of Microemulsion Containing Clotrimazole for Topical Delivery

Cited by 106 publications

References 36 publications

Microemulsion-Based Oxyresveratrol for Topical Treatment of Herpes Simplex Virus (HSV) Infection: Physicochemical Properties and Efficacy in Cutaneous HSV-1 Infection in Mice

Microemulsion-Based Oxyresveratrol for Topical Treatment of Herpes Simplex Virus (HSV) Infection: Physicochemical Properties and Efficacy in Cutaneous HSV-1 Infection in Mice

Phenobarbital loaded microemulsion: development, kinetic release and quality control

Enhanced Topical Delivery of Finasteride Using Glyceryl Monooleate-Based Liquid Crystalline Nanoparticles Stabilized by Cremophor Surfactants

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