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Indian Journal of Science Analysis The International Journal for Science ISSN 2319 – 7730 EISSN 2319 – 7749 © 2016 Discovery Publication. All Rights Reserved Formulation and evaluation of Aspirin Nanoemulsion Publication History Received: 20 January 2016 Accepted: 13 February 2016 Published: 1 March 2016 Page 245 Citation Selvi PP, Faustina S, Sowmiya A. Formulation and evaluation of Aspirin Nanoemulsion. Indian Journal of Science, 2016, 23(79), 245-252 FORMULATION AND EVALUATION OF ASPIRIN NANOEMULSION Mrs.P.P.Selvi, Faustina.S, Sowmiya.A Department of Chemical Engineering Kongu Engineering College (Autonomous), Perundurai Email-ID:[email protected] Keywords – Nanoemulsion, Solubility, Drug release, Aspirin INTRODUCTION Nanoemulsion can be defined as the oil in water emulsion with mean droplet diameters ranging from 50 to 1000nm.Usually, the average droplet size is between 100 and 500nm. The particles can exist as water in oil, respectively. The REASONS FOR SELECTION OF DRUG The efficacy of many drugs is often limited by their potential to reach the site of therapeutic action due to various problems such as - poor bioavailability, in vivo stability, solubility, intestinal absorption, sustained and targeted delivery to site of action, therapeutic effectiveness. In most cases only a small amount of administered dose reaches the target site, while the majority of the drug distributes throughout the rest of the body in accordance with its physicochemical and biological properties. It is estimated that at present 40% of New Chemical Entities under development and60% of synthesized drugs are poorly water soluble compounds. Even more 70% of drugs are discarded due to poor solubility. The dosage form of an active ingredient can have a great effect on its solubility and permeability, thereby affecting bioavailability. Nanonization forms have better approach for increased solubility of Drug and leads to an increase in Bioavailability of the Drug. The BioPharmaceutics Classification System classifies drugs into four groups: 246 Nanoemulsion can be defined as the emulsions with mean droplet diameter ranging from 20-500nm used as targeted drug delivery carrier in pharmaceutical products. The present objective is to formulate and evaluate the nanoemulsion of Aspirin. The first part of the work is considered to formulate Aspirin Nanoemulsion to overcome poor solubility. It is composed of Aspirin drug, Acetone as solvent, Arachis oil as oil phase, Tween 80 as surfactant, Polyethylene Glycol 400 as Co-Surfactant and Water. Various formulations of Oil in Water Nanoemulsions were prepared by varying the Smix ratios and formulating at constant temperature. Nanoemulsions were evaluated for various parameters and its compatibility studies were made. The obtained nanoemulsion has a particle size of about 111nm. FTIR data indicate the compatibility nature of drug in the formulation. The drug release was up to 77.35% at the end of 3rd hour. terms Sub-Micron Emulsion (SME) and Mini emulsion are used as synonyms. Usually, SME’s contain 10 to 20 percent oil stabilized with 0.5 to 2 percent egg or soya bean lecithin. Nanoemulsion are a group of dispersed particles used for pharmaceutical and biomedical aids and vehicles that show a great promise for the future of Cosmetics, Diagnostics, Drug Therapies and Biotechnologies. Page ABSTRACT Class 1: Solubility High Permeability, High Class 2: Solubility High Permeability, Low Class 3: Solubility Low Permeability, High Permeability, Low As the Drug Aspirin belongs to Class 4 system of classification it has Less Solubility which leads to Low Bioavailability. To overcome these problems, Aspirin must be formulated as a Nanoemulsion in size rage of 20-500nm. PROPOSED WORK The ultimate aim of the present work is to Formulate and Evaluate the Aspirin Nanoemulsion to increase the solubility of the Drug. To develop an ideal formulation of Aspirin Nano emulsion. To optimize the process parameters to produce a formulation with acceptable properties. To enhance the Solubility and the Bioavailability of the Aspirin. To evaluate different properties of prepared Nanoemulsion like Particle size, Density Viscosity, etc. To study the pattern of Drug Release Kinetics for the prepared Nano emulsion. FORMULATION OF NANOEMULSION The drug loaded Nanoemulsion was formulated by dissolving 5mg of the drug in acetone and adding varying concentration of oil to the acetonolic drug EVALUATION OF NANOEMULSION 1. CALIBRATION CURVE FOR DRUG 10mg of Aspirin was accurately weighed and dissolved in 100ml of phosphate buffer solution 7.4. Take 1ml and make up to 10ml in a standard flask to produce the concentration of 10µg/ml. Label this solution as primary stock solution. Then withdraw 1ml of primary stock solution and diluted to 10ml in a standard flask to produce the concentration of 10µg/ml. This solution is considered as secondary stock solution. From the secondary stock solution withdraw 2ml, 4ml, 6ml, 8ml and10ml and make up the volume to 10ml with phosphate buffer of pH7.4, in order to produce the concentration ranging from 2µg/ml, 4µg/ml, 6µg/ml, 8µg/ml and 10µg/ml. 2. PHYSICAL APPEARANCE The physical appearance of Drug, Excipients and Formulation were analysed visually. The Drug Aspirin, Arachis Oil as Oil Phase, Tween80 as Surfactant, and Polyethylene Glycol as Co-Surfactant are observed visually for the Physical Appearance. 3. PHASE DILUTION TEST Phase Dilution Test was performed in order to determine the type of emulsion. Here few ml of Nanoemulsion is diluted 247 Low Page Class 4: Solubility solution. The aqueous phase was prepared by adding Tween 80 and PEG-400 to distilled water. The oil phase was added to the aqueous phase drop by drop which is placed in a magnetic stirrer. It is then sonicated for about 45 mins. Nanoemulsions are formed. The procedure was repeated for varying concentration of oil, surfactant and co-surfactant. with water and it was visually observed and confirmed if there was any change in homogeneous phase. 4. PARTICLE SIZE ANALYSIS The most important physical property of particulate samples is particle size. Particle size analysis, particle size measurement, or simply particle sizing is the collective name of the technical procedures, or laboratory techniques which determines the size range, and/or the average, or mean size of the particles in a powder or liquid sample. The Particle Size was measured by Particle Size Analyzer. It is important to measure the Particle Size and necessary to understand how they affect the products. 5. ZETA POTENTIAL Zeta Potential is scientific term for electro kinetic potential. Zeta Potential is the potential difference existing between the surfaces of a solid particle immersed in a conducting liquid. It is determined to calculate the surface charge of the formulation. The Zeta Potential is a key indicator of the stability of colloidal dispersions. 7. IN-VITRO STUDIES In-vitro drug release study of Aspirin Nanoemulsion was performed in the Magnetic Stirrer with a hot plate with an agitation speed of 100rpm. One ml of Aspirin Nanoemulsion was placed in dialysis bag, sealed at the both ends placed in a glass beaker. The dissolution medium used was phosphate buffer saline pH 7.4. At designed intervals for 3 hours, the Absorbance was measured by UV-Vis spectrophotometer at 265nm. The concentration of Aspirin Nanoemulsion was determined from the calibration graph and the percentage of drug release was calculated by respective concentration of standard calibration curve with suitable dilution factor. RESULTS 1. PHYSICAL APPEARANCE The active substance Aspirin was in the form of white crystalline powder. The Tween 80 was amber coloured liquid and viscous in nature. The Arachis oil was pale yellow in colour and viscous in nature. The PEG 400 was a transparent liquid. The Nanoemulsion was Bluish translucent dispersion. Page The presence of peak at a specific wave number indicates the presence of a specific chemical bond. If specific interaction took place between the materials, the most obvious and significant difference would be the appearance of new peaks or a shift of existing peaks. FT-IR is used to study the interactions occurring between drug and excipient by matching the peaks of spectra. 248 6. FOURIER-TRANSFORM INFRARED SPECTROSCOPY 2. PHASE DILUTION TEST This test clearly indicates the type of emulsion to which it belongs. If water distributes uniformly then it is O/W Emulsion. If water separates out as a layer then it is W/O Emulsion. The Formulated Nanoemulsions belongs to O/W TYPE since when it is diluted with water, it distributes uniformly throughout the solution. 3. PARTICLE SIZE ANALYSIS NANOEMULSION 3 (1:3) – 111.3nm 5. FOURIER-TRANSFORM INFRARED SPECTROSCOPY ARACHIS OIL (OIL) 4. ZETA POTENTIAL TWEEN 80 (SURFACTANT) Page 249 NANOEMULSION 3 (1:3) RESULTS 7. IN-VITRO STUDIES PLOT HIGUCHI EQUATION The straight line of linear regression analysis indicates zero order of the data yields the equation of best line with value = 0.8703 and the slope of line corresponds to the Zero Order Rate constant was 2.138. The best linearity was found in Higuchi’s Equation plot = 0.8703 indicating the release of drug from matrix as a square root of time dependent process based on Fickian diffusion. The dissolution data was also plotted in accordance with Hixson Crowell cube root law. Applicability of data = 0.9295 indicates a change in surface area CONCLUSION The Major objective of the study was to develop Aspirin Nanoemulsion for increasing the solubility thus increasing the bio availability. The compatibility of the drugs and the excipients were performed in pre formulation studies. The formulations were made by varying the oil and surfactant concentration. The formulations were characterized by the UV spectroscopy, Particle size and Zeta potential. The impacts of different surfactant concentrations on drug loading 250 PLOT HIXON CROWELL EQUATION and diameter of Nanoemulsion with the progressive dissolution of matrix as a function of time. According to Korsmeyer-Peppas where n is the release exponent, indicative of mechanism of drug release 0.9926. Fickian diffusional release and a case-II relaxation release are the limits of this phenomenon. Fickian diffusional release occurs by the usual molecular diffusion of the drug due to a chemical potential gradient. 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