Formulation and Evaluation of Nanoemulsion for Targeting and Systemic Delivery of Diclofenac Sodium (original) (raw)
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The aim of my present study is to Develop and Evaluate Microemulsion for topical application of Diclofenac sodium by using oleic acid at different ratios for the treatment of pain. Design of microemulsion formulation for topical use of drugs, having the potential to increase the solubility of poorly water soluble drugs. To avoid the first pass metabolism and there is a potential to deliver the drug in a controlled manner to minimize the adverse effect on the g.i.t like mild dyspepsia and heartburn to ulceration and hemorrhage. Reduction of dosing frequency due to longer duration of action. To improve patient compliance to provide sustained release drug for longer periods of time due to short half-life. To delivery of hydrophilic as well as lipophilic drug as drug carriers because of its improved drug solubilization capacity and long shelf –life. Microemulsion was prepared by water trituration method using oleic acid as oil phase, tween-80 as surfactant and polyethylen glycol-400 as co-surfactant. Different oils, surfactants and co-surfactants were screened to select ideal components of microemulsions with good solubility and excellent skin penetration of Diclofenac sodium. The solubility of diclofenac sodium was highest in oleic acid followed by olive oil, and isopropyl myristate, isopropyl palmitate. ME-3 was exhibited 98.54±0.26% higher drug content then other formulations. Among all formulations, the highest permeation flux of µg/cm2 /hour was observed in of formulation ME-3. Keywords: Microemulsion, Optical transparency, Particle size, Transmission Electron Microscopy, in –vitro skin permeation, FT-IR
Design of a Microemulsion-Based Drug Delivery System for Diclofenac Sodium
A microemulsion-based drug delivery system has been designed for Diclofenac Sodium (DS) comprising Span 60, 1-Propanol, Water, and Lemon Oil. The microemulsion system has been characterized by a pseudo-ternary phase diagram using the water titration method. The properties and structure of this system have been studied by the use of refractive index, electrical conductivity, viscosity and UV-Visible spectroscopy. The conductivity (σ) and viscosity (kη) measurements have provided evidence for percolation behavior with variation in Φ (weight fraction of aqueous phase). This phase transition corresponds to the structural change from water-in-oil to a bicontinuous microemulsion system. The percolation threshold (ΦC) obtained from conductivity measurements was in accordance with that obtained by viscosity measurements. Five microemulsion samples were selected and the changes in microstructure after incorporation of the drug, Diclofenac Sodium (DS) were examined by centrifugation, conductivity measurements, viscosity measurements and spectroscopic studies. The conductivity measurements showed that DS-loaded samples have higher conductivity values when compared to non-loaded samples. It was also found that DS is interfacially active. In addition, loading of DS had no negative effect on the stability of the system.
International Journal for Research in Applied Science and Engineering Technology, 2017
Diclofenac , non-steroidal anti-inflammatory drug (NSAID) belongs to BCS Class II drug with low dissolution and poor aqueous solubility. The main aim of the present study was to improve the solubility and dissolution rate of diclofenac using self-emulsifying drug delivery technique. Micro emulsion region was formed by preparing the ternary phase diagram. Ratio 0.15:0.85 , 0.5:0.5 and 0.3:0.7 was selected as the self-emulsification region for the development of formulation. Drugexcipient studies were performed by FT-IR .Parameters were evaluated include time of emulsification , freezing and thawing and dissolution. The present research work describes SEDDS of Diclofenac using olive oil, Tween 20 and PEG200 prepared by simple vortex in the mixture at 40 °c and packed in hard gelatine capsule shell of 00 size. In vitro dissolution was carried out using USPII by 6.8 pH buffer at 75 RPM and samples were measured at 276 nm using UV-Visible spectroscopy. From the studies the optimized SEDDS was composed of 30% oil, 45% Surfactant and 25% Co surfactant. The optimized formulation was found to be showing significant improvement in drug release and had 24 seconds self-emulsification time , having drug content 101.16% and complete 99.01% drug release in 60 minutes.
Nanoemulsions as vehicles for transdermal delivery of aceclofenac
Aaps Pharmscitech, 2007
The aim of the present study was to investigate the potential of a nanoemulsion formulation for transdermal delivery of aceclofenac. Various oil-in-water nanoemulsions were prepared by the spontaneous emulsification method. The nanoemulsion area was identified by constructing pseudoternary phase diagrams. The prepared nanoemulsions were subjected to different thermodynamic stability tests. The nanoemulsion formulations that passed thermodynamic stability tests were characterized for viscosity, droplet size, transmission electron microscopy, and refractive index. Transdermal permeation of aceclofenac through rat abdominal skin was determined by Franz diffusion cell. The in vitro skin permeation profile of optimized formulations was compared with that of aceclofenac conventional gel and nanoemulsion gel. A significant increase in permeability parameters such as steady-state flux (Jss), permeability coefficient (Kp), and enhancement ratio (Er) was observed in optimized nanoemulsion formulation F1, which consisted of 2% wt/wt of aceclofenac, 10% wt/wt of Labrafil®, 5% wt/wt of Triacetin®, 35.33% wt/wt of Tween 80®, 17.66% wt/wt of Transcutol P®, and 32% wt/wt of distilled water. The anti-inflammatory effects of formulation F1 showed a significant increase (P<.05) in percent inhibition value after 24 hours when compared with aceclofenac conventional gel and nanoemulsion gel on carrageenan-induced paw edema in rats. These results suggested that nanoemulsions are potential vehicles for improved transdermal delivery of aceclofenac.
Diclofenac sodium-loaded solid lipid nanoparticles prepared by emulsion/solvent evaporation method
Journal of Nanoparticle Research, 2011
The preparation of solid lipid nanoparticles (SLNs) suffers from the drawback of poor incorporation of water-soluble drugs. The aim of this study was therefore to assess various formulation and process parameters to enhance the incorporation of a water-soluble drug (diclofenac sodium, DS) into SLNs prepared by the emulsion/solvent evaporation method. Results showed that the entrapment efficiency (EE) of DS was increased to approximately 100% by lowering the pH of dispersed phase. The EE of DS-loaded SLNs (DS-SLNs) had been improved by the existence of cosurfactants and increment of PVA concentration. Stabilizers and their combination with PEG 400 in the dispersed phase also resulted in higher EE and drug loading (DL). EE increased and DL decreased as the phospholipid/DS ratio became greater, while the amount of DS had an opposite effect. Ethanol turned out to be the ideal solvent making DS-SLNs. EE and DL of DS-SLNs were not affected by either the stirring speed or the viscosity of aqueous and dispersed phase. According to the investigations, drug solubility in dispersion medium played the most important role in improving EE.
A Scientific Review on Nanoemulsion for Targeting Drug Delivery System
2019
Nanoemulsions have attracted great attention in research, dosage form design, and pharmacotherapy. This is as a result of some attributes peculiar to nanoemulsions such as optical clarity, ease of preparation, thermodynamic stability and increased surface area. Poor water solubility remains the main culprit for the formulation scientist which can be overcome by canonization. Nanoemulsion is a kinetically stable and isotropic system of two immiscible liquids in the submicron size range. Nanoemulsions are composed of oil droplets dispersed in an aqueous medium and stabilized by surfactant molecules. Many parenteral nutrition and drug emulsions on the market confirm the safe use of NE over the years. Parenteral emulsions loaded with APIs (active pharmaceutical ingredients) are considered as drug delivery systems (DDS). DDS focuses on the regulation of the in-vivo dynamics, such as absorption, distribution, metabolism, and extended bioavailability, thereby improving the effectiveness an...
International Journal of Pharmaceutics, 2009
The aim of this paper was to ascertain the role of drug crystalline form and preparation procedure in nanosuspension formulations in order to optimise dissolution properties of lipophilic, poorly soluble drugs, thus improving their oral bioavailability. The non-steroidal anti-inflammatory drug diclofenac acid (DCF), which is known to exist in different crystal forms, was chosen as a model drug. To this purpose, the influence of homogenization technique was studied by preparing several nanosuspensions with two different crystalline forms of the drug (DCF1 and DCF2). Particle size and size distribution, morphology, microstructure, and thermal behaviour of the different formulations were studied by photon correlation spectroscopy (PCS), scanning electron microscopy (SEM), X-ray powder diffraction (XRD) and differential scanning calorimetry (DSC). Solubility studies of the bulk drug crystalline forms and dissolution experiments of nanosuspensions in comparison with different controls (bulk drug, physical mixtures, coarse suspensions) were carried out in different media: distilled water, simulated gastric fluid (SGF) and simulated intestinal fluid (SIF).
Nanoemulsion Based Drug Delivery-A Review
2018
Nanoemulsions are submicron sized emulsion that is under extensive investigation as drug carriers for improving the delivery of therapeutic agents. Nanoemulsions have the potential in pharmaceutical industries because of the transparency at high droplet volume fraction, higher rate of bioavailability or diffusion and increased shelf life of the pharmaceuticals. Nanoemulsions are clear, thermodynamically stable, isotropic liquid mixtures of oil, water, surfactant and co-surfactant. These are oil-in-water (o/w) type of emulsions with the average droplet size ranging from 5nm to 100 nm. Reduction in droplet size to nanoscale leads to change in physical properties such as optical transparency & unusual elastic behavior. Thus the aim of this review is focused on nanoemulison advantage and disadvantage, various methods of preparation, characterization techniques and the various applications of sub micron size emulsion in different areas such as various route of administration, in chemothe...
A Review on Novel Drug Delivery System Nanoemulsion
International Journal of Current Science Research and Review
various researcher are innovate a replacement therapy regarding improvement of drug action. Improve drugs absorption, distribution also we improve its efficacy. Amongst that a replacement innovative technology are develops. A nanoemulsion is technique to enhance the solubility, bioavability, pharmacokinetic and pharmacodinemics of medicine .in this review article us familiar about the novel technique nanoemulsion and its preparation methods, charactorization of nanoemulsion. Nanoemulsion has been identified as a promising delivery system for various drugs including biopharmaceuticals. Nanoemulsion may be a heterogeneous system composed of one immiscible liquid dispersed as droplets within another liquid. The droplets size of nano emulsion is between 20 to 500 nm. Diameter and surface properties of droplets of nanoemulsion plays a crucial role in the biological behavior of the formulation. Small droplet sizes cause transparent emulsions so that product appearance is not altered by th...