Preparation and evaluation of aceclofenac topical microemulsion (original) (raw)
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Studia Universitatis Vasile Goldis Arad, Seria Stiintele Vietii
The purpose of this study was to develop microemulsion-based drug vehicles for topical administration of sodium diclofenac (SD), using Tween 80 and 1-octanol as surfactant and cosurfactant, respectively. Three commonly pharmaceutical oils (isopropyl myristate, arachis oil and canola oil) were investigated as oil phases. Microemulsion existence region was identified through the construction of the pseudoternary phase diagrams, using water titration method. The prepared microemulsions were evaluated regarding their transparency/translucency, optical birefringence, electrical conductivity, viscosity, pH and stability. The isopropyl myristate-based systems showed a slightly higher area of microemulsion existence and permitted the formation of microemulsions at lower concentrations of surfactants. The effect of added active substance on the stability of microemulsions was also evaluated for 1% SD (w/w).
AAPS PharmSciTech, 2007
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.
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
A Review on Microemulsion – a Recent Approach for Topical Drug Delivery System
2021
Abstract: A drug delivery method has been explored as microelectric emulsions that are optically isotropical, and thermodynamically stable water, oil, surfactant and/or surfactants due to their potential to solubilize poorly water soluble medicines and to their increased topical and systemic availability. The lipophilic drugs mobility may be solubilized and the skin can be entered quickly and effectively. Thus the topical administration of drugs is helpful. Many commonly utilized topical treatments such as salts, creams and lotions have numerous drawbacks such as sticky texture, causing discomfort when applied, They have a lower coefficient of propagation so applied by rubbing and they also show a stability concern. The difficulty of stability of the microemulsion is low viscosity, but it may be solved by adding viscosity and the moisturizing stratum corneum into topical DDS, which increases dermal penetration and skin flow of medical devices. Because of all these considerations, th...
2013
The aim of the present study was to prepare and evaluate different formulations of Diclofenac diethylammonium in microemulsion base with a view to enhance its permeability through the skin. Various o/w and w/o microemulsions of Diclofenac diethylammonium were prepared by the spontaneous emulsification methods. Isopropyl myristate was used as oil phase, Polyoxyethylenesorbitan monooleate and Sorbitanmonolaurate as surfactants and Isopropyl alcohol, Dioctylsodium sulfosuccinate (AOT) and polyoxyethylene (10) octyl phenol ether as co-surfactants. Microemulsion existence region was determined using the pseudo-ternary phase diagrams for preparing different formulations. The optimized o/w and w/o microemulsions consist of 1.16% w/w Diclofenac diethylammonium as the active ingredient. The microemulsions were characterized for different parameters. In-vitro permeation studies through rat skin showed that permeability parameters like flux (Jss) and permeability coefficient (P) were significa...
Topical Delivery of Diclofenac using Microemulsion Systems
2008
The purpose of this study was to investigate microemulsions as delivery systems for diclofenac sodium (DS). Microemulsion systems were composed of: soybean oil, nonionic surfactants (Brij 58 and Span 80), and different alcohols: ethanol, and 1-buthanol as ...
Design Development and Evaluation of Topical Microemulsion
International Research Journal of Pharmacy
A microemulsion based gel was designed for the topical and targeted delivery of sertaconazole nitrate for the treatment of su perficial fungal infection. The microemulsion region was obtained using a ternary diagram, different ratio of oil and Smix were used. The microemulsion of sertaconazole containing 2% (w/w) of sertaconazole, 6.67% (w/w) of oil phase (Eugenol+Oleic acid 1:1), 60.18% (w/w) of surfactant mixture 2:1 ratio (Tween-80 and Transcutol-P) and 33.15% (w/w) with distilled water. The prepared microemulsion gel and commercial cream of sertaconazole were evaluated for in-vitro and ex-vivo studies. The highest drug retention was achieved with Tween 80 and Transcutol P (T80TC45) when the optimized formulation was converted to a gel. The designed formulation MG2 was safe to be used over the skin as the PDI=0 when compared with commercial cream and MG1. The optimized formulation also posse's anti-inflammatory activity. The average zone of inhibition of MG2 was (23.19 ± 0.478) which was more than the commercial cream (15.34 ± 0.382) or MG1 (17.78 ± 0.715). Candida albicans which may be due to better permeation and retention effect of microemulsion gel 2. The MG2 was found to be stable after six month. The results obtained in this research from in vitro and in vivo data it can be concluded that the developed microemulsions have great potential for topical drug delivery in the treatment of inflammation and fungal infection.
Development and Characterization of Topical Microemulsion of Levofloxacin
In the present work, levofloxacin based microemulsion was developed and its usefulness as topical drug carrier system for anti bacterial activity was investigated. Microemulsion was prepared by phase titration method using oleic acid as oil phase, tween-60 as surfactant and isopropyl alcohol as co-surfactant. Five different formulations were formulated with various amount of the oil, water and the mixture of surfactant and co-surfactant. Different formulations were prepared to evaluate the effect of oil content, surfactant/ cosurfactant concentration on in-vitro permeation rates. Microemulsions were characterized for pseudo-ternary phase diagrams, pH, viscosity, droplet size, in-vitro release profile and stability evaluation. In-vitro skin permeability of levofloxacin from the microemulsion was evaluated using franz diffusion cell method. The optimized microemulsion formulation was found to be o/w type emulsion by pseudo-ternary phase diagram. These results indicate that the microemulsion system studied is a promising tool for the topical delivery of levofloxacin.
Preparation and Evaluation of Fluconazole Topical Microemulsion
A fluconazole w/o microemulsion was developed for topical application using isopropyl myristate as the oil phase. Pseudo-ternaryphase diagrams were constructed to determine the microemulsion existence region using surfactant (tween 80) andco-surfactant (polyethylene glycol 400). Different formulations were prepared to evaluate the effect of oil content, surfactant/co-surfactant concentration on in-vitro permeation rates. In-vitro transdermal permeability of fluconazole from themicroemulsions was evaluated using Keshary Chien diffusion cells mounted with 0.45µ cellulose acetate membrane. Theamount of fluconazole permeated was analyzed by HPLC. The permeability of the fluconazole incorporated into themicroemulsion systems was 2.5 - fold higher than that of the marketed formulation. These results indicate that the microemulsionsystem studied is a promising tool for the percutaneous delivery of fluconazole.
Evaluation of a microemulsion-based gel formulation for topical drug delivery of diclofenac sodium
Journal of Pharmaceutical Investigation, 2017
Introduction: Etoricoxib is a poorly water-soluble oral NSAID and is associated with a number of complications such as bleeding, ulcers and dyspepsia but these can be overcome by delivering the drug topically. Objectives: Microemulgel for the topical delivery of etoricoxib was formulated to increase its solubility and thus improve the skin permeability. Methods: The solubility of etoricoxib was studied in various oils, surfactants and cosurfactants. Pseudo-ternary phase diagrams were constructed by varying the surfactant to cosurfactant (Smix) ratio. Microemulsions with different compositions were formulated and optimized. Selected o/w microemulsions contained 1% etoricoxib and were evaluated for pH, rheology, drug content, particle size and in vitro drug release. Optimized microemulsion was incorporated in 1% Carbopol® 934 and was evaluated for rheological properties, spreadability, in vitro permeation, skin irritation and stability. Results: Capryol™ 90, Tween 80 and Transcutol® P exhibited the highest solubility. Maximum microemulsion region was observed when the Smix ratio was 3:1. The average particle size of the optimized microemulsion was 37.61 nm, zeta potential was-2.88 mV and permeability of the drug from the microemulsion was 66.8% after 8 h. The prepared gel showed 57.8% drug release after 8 hr. Skin irritation studies indicated that the optimized formulation was safe for topical application. Stability studies indicated that the formulation remained unaffected at accelerated storage conditions. Conclusion: Results indicated that the micro-emulgel has potential for sustained action of drug release and may act as a promising tool to enhancepercutaneous delivery of etoricoxib.