Preparation, characterization and permeation studies of a nanovesicular system containing diclofenac for transdermal delivery

Gaur, Praveen Kumar; Purohit, Suresh; Kumar, Yatendra; Mishra, Shikha; Bhandari, Anil

doi:10.3109/10837450.2012.751406

Cited by 21 publications

(24 citation statements)

References 34 publications

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“…SLNs are at the forefront of the rapidly developing field of nanotechnology due to possibility for site specific drug delivery, controlled release, increased bioavailability, reduced side effects, smaller dosage form, dosage form stability, and reduction in fed/fasted variability [6, 7]. The SLN's ability to incorporate hydrophilic/hydrophobic drugs imparts unique diversity.…”

Section: Introductionmentioning

confidence: 99%

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles:In VitroDrug Release and Pharmacokinetics Studies

Gaur¹,

Mishra

Bajpai³

et al. 2014

BioMed Research International

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102

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Solid lipid nanoparticle is an efficient lipid based drug delivery system which can enhance the bioavailability of poorly water soluble drugs. Efavirenz is a highly lipophilic drug from nonnucleoside inhibitor category for treatment of HIV. Present work illustrates development of an SLN formulation for Efavirenz with increased bioavailability. At first, suitable lipid component and surfactant were chosen. SLNs were prepared and analyzed for physical parameters, stability, and pharmacokinetic profile. Efavirenz loaded SLNs were formulated using Glyceryl monostearate as main lipid and Tween 80 as surfactant. ESLN-3 has shown mean particle size of 124.5 ± 3.2 nm with a PDI value of 0.234, negative zeta potential, and 86% drug entrapment. In vitro drug release study has shown 60.6–98.22% drug release in 24 h by various SLN formulations. Optimized SLNs have shown good stability at 40°C ± 2°C and 75 ± 5% relative humidity (RH) for 180 days. ESLN-3 exhibited 5.32-fold increase in peak plasma concentration (C max⁡) and 10.98-fold increase in AUC in comparison to Efavirenz suspension (ES).

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Section: Introductionmentioning

confidence: 99%

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles:In VitroDrug Release and Pharmacokinetics Studies

Gaur¹,

Mishra

Bajpai³

et al. 2014

BioMed Research International

Self Cite

102

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“…Moreover, other physical parameters like low molecular weight (369.3) and pharmacological parameters such as poor bioavailability (40-60%), short biological half-life (2-3 h), and low dose (25-50 mg) are favorable for transdermal delivery [9]. Various transdermal delivery systems containing diclofenac have been reported, including patches [8,10], gels [11,12], mixed micelle formulations [13], microemulsion systems [11,[14][15][16][17], nanoemulsions [15] and vesicular systems [18][19][20]. Transdermal delivery of NSAIDs proved to be a convenient route of administration for a variety of clinical indications [21].…”

Section: Introductionmentioning

confidence: 99%

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation

Ali

Kumar

Ahad

et al. 2015

Journal of Polymer Engineering

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A transdermal therapeutic system (TTS) of diclofenac diethylamine (DDE) was developed to obtain a prolonged controlled drug delivery by the solvent evaporation technique. The matrix diffusion controlled systems used various combinations of hydrophilic (polyvinylpyrrolidone K30) and lipophilic (Eudragit RL 100  and Eudragit RS 100  ) polymers containing dimethyl sulfoxide (DMSO) (0, 5 and 10% w/w) as a penetration enhancer. In vitro drug release was improved with an increased fraction of hydrophilic polymer. Formulation F8 containing Eudragit RL 100 and polyvinylpyrrolidone K30 in the ratio 40:60 presented the highest drug release (92.45%) and permeation rate (0.0988±0.010 mg/cm 2 /h) with sustained release action for 48 h. In vivo pharmacodynamic study of DDE-loaded Eudragit RL 100  transdermal system (formulation F8) showed significant higher percent inhibition of rat paw edema compared with the marketed formulation of the drug. Our results suggest that a developed formulation is an efficient system for transdermal diclofenac delivery against inflammation. The optimized formulation was found to be stable and did not show physicochemical interaction. The system is envisaged to be stable for a sufficiently long period (2.52 years) at room temperature.

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“…Gaur et al (2014) had studied the transdermal formulations containing permeation enhancers that cause skin damage and diclofenac was used as a model drug. The presence of ceramid specifically promotes drug permeation through SC and dermis and also contributes to stability and non-irritancy.…”

Section: Resultsmentioning

confidence: 99%

Performance evaluation of Cryo Laser Phoresis technique as biophysical method to promote diclofenac sodium cutaneous perfusion

Andréo

Rufino

Ubaldo

et al. 2016

Braz. J. Pharm. Sci.

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Aiming to alter and/or improve permeation of active compounds in the skin, many strategies have been developed, including biophysical methods. One of the physical absorption techniques, currently known as Cryo Laser Phoresis (CLP), consists of an apparatus that emits radiation on polar or nonpolar molecules of the active substance, resulting in faster penetration when in comparison to the standard topical application. The goal of this work was to evaluate the efficacy of a method that proposes to increase cutaneous permeation of diclofenac sodium by using CLP technique. The influence on permeation was evaluated ex vivo, using Franz cell and human skin obtained from cosmetic surgery. The results were evaluated using statistical methods and data exploratory analysis: clusters, k-means and Principal Component Analysis. The results showed a larger increase in the concentration of diclofenac sodium in the dermis with the use of laser. In all samples (with or without laser application) it was observed that skin surface showed an amount of diclofenac sodium and that there was no active passage to the receptor liquid, suggesting that diclofenac sodium was not absorbed. These results indicate that CLP, when used under the conditions described in this study, is able to increase diclofenac sodium penetration and its retention into deeper layers. Uniterms:Cryo Laser Phoresis/dematologic use. Cutaneous permeation. Diclofenac sodium/cutaneous permeation. Franz cell.No sentido de alterar e/ou melhorar a penetração de substâncias na pele, diversas estratégias têm sido desenvolvidas, variando desde a aplicação de novos veículos e ativos encapsulados, até equipamentos que atuam por métodos biofísicos. Uma das técnicas de absorção física, atualmente conhecida como Crio Laser Forese (CLF), consiste em um aparato que emite radiação sobre moléculas polares ou apolares da substância ativa, tornando sua penetração mais rápida, se comparada à administração tópica comum. O objetivo deste trabalho foi avaliar a eficácia de um método que propõe aumentar a permeação cutânea do diclofenaco de sódio incorporado a um gel, por meio do uso da CLF. A influência sobre a permeação foi avaliada ex vivo, utilizando célula de Franz e pele humana obtida de cirurgia plástica. Os resultados foram balizados mediante aplicação de métodos estatísticos e análise exploratória de dados: clusters, k-means e Análise por Componentes Principais. Os resultados demonstraram aumento na concentração do diclofenaco de sódio na derme com o uso do laser. Em todas as amostras (com ou sem aplicação de laser), observou-se, uma quantidade de diclofenaco de sódio na superfície da pele e que não houve passagem de ativo para o líquido do receptor, sugerindo que o diclofenaco de sódio não foi absorvido. Estes resultados indicam que CLF usada sob as condições descritas neste estudo é capaz de aumentar a penetração do diclofenaco de sódio e sua retenção em camadas mais profundas da pele Unitermos: Crio Laser Forese/uso em dermatologia. Permeação cutânea. Diclofenaco de sódio/perme...

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Preparation, characterization and permeation studies of a nanovesicular system containing diclofenac for transdermal delivery

Abstract: The composition of the nanovesicle played an important role in physical properties and drug permeation.

Cited by 21 publications

References 34 publications

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles:In VitroDrug Release and Pharmacokinetics Studies

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles:In VitroDrug Release and Pharmacokinetics Studies

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation

Performance evaluation of Cryo Laser Phoresis technique as biophysical method to promote diclofenac sodium cutaneous perfusion

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Preparation, characterization and permeation studies of a nanovesicular system containing diclofenac for transdermal delivery

Abstract: The composition of the nanovesicle played an important role in physical properties and drug permeation.

Cited by 21 publications

References 34 publications

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles:In VitroDrug Release and Pharmacokinetics Studies

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles:In VitroDrug Release and Pharmacokinetics Studies

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100® transdermal system against inflammation

Performance evaluation of Cryo Laser Phoresis technique as biophysical method to promote diclofenac sodium cutaneous perfusion

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Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation