Ashish Jain Ph.D. Viva PPT

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Published on July 21, 2014

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PowerPoint Presentation: Ph.D. (Pharmaceutical Sciences)Thesis Presentation by: Ashish Jain Reg. No. 0803PH22A31 1 “A Comparative Skin Permeability Study of Some Antihypertensive Agents by Iontophoresis and Passive Methods for their Transdermal Development.” Jawaharlal Nehru Technological University, Hyderabad. A.P. Supervisor: Dr. S. Nayak Co-Supervisor: Dr. Vandana Soni PowerPoint Presentation: 2 Presentation Flow PowerPoint Presentation: 3 Iontophoretic Drug Delivery System PowerPoint Presentation: 4 Iontophoretic System Comprises three basic components: 1 . Source of electronic current : battery and controlled electronics 2. Active reservoir , which contains the ionic therapeutic agent; 3. Indifferent or return reservoir system , which contains an electrolyte and serves to complete the electric circuit. (Both reservoir system placed on the skin  Battery on current flow to active reservoir electronic current change to ionic current flow through active reservoir, through skin, towards the indifferent reservoir electronic current transformed back at return electrode, for completing the circuit) PowerPoint Presentation: 5 How does it work?? Electrode placement is dependent on the electric charge of the ion which are trying to deliver. A positive ion will be delivered from the positive electrode and a negative ion will be delivered by the negative electrode. Electrical energy assists the movement of ions across the stratum corneum according to the basic electrical principle “like charges repel each other and opposite charges attract each other.” Diagram of iontophoretic technique: as current is applied the drug cations are repelled into the skin and eventually absorbed in the systemic circulation PowerPoint Presentation: BATTERY + - ON BLOOD VESSEL DERMIS EPIDERMIS IONTOPHORETIC SYSTEM + + + + + + + + + + + + + + + + + + + + + + + + + - - - - OFF ANODE DRUG RESERVIOR CATHODE + Drug - Counter ion - - - How does it work? PowerPoint Presentation: 7 NECESSITY OF THE DEVELOPMENT OF NOVEL DRUG DELIVERY SYSTEM FOR HYPERTENSION PowerPoint Presentation: ( Since antihypertensives suffer from the disadvantage of extensive first pass metabolism and variable bioavailability, they are considered ideal transdermal candidates, Moreover the drug input can be terminated at any point of time by removing transdermal patch .) 8 PowerPoint Presentation: 9 9 Advantages of Iontophoretic Drug D elivery PowerPoint Presentation: 10 Iontophoresis enhances transdermal drug delivery by three mechanisms J electric is the flux due to electric current application; J passive is the flux due to passive delivery through the skin; and J convective is the flux due to convective transport due to electro osmosis. PowerPoint Presentation: 11 Factors Affecting Iontophoretic Delivery of the Drug Operational Factors I. Composition of formulation: Concentration of drug solution pH of donor solution Ionic strength Presence of co-ions II. Physicochemical properties of the permeant : Molecular weight Charge Polarity III. Experimental conditions: Current density Duration of treatment Electrode material Polarity of electrodes Biological Factors Regional blood flow Skin pH Condition of skin PowerPoint Presentation: 12 Aluminum foil Platinum and Silver/Silver chloride A better choice of electrode is silver/silver chloride because it minimizes electrolysis of water during drug delivery. Commercial Electrodes Electrodes have a small chamber covered by a semipermiable membrane into which ionized solution may be injected. The electrode self adheres to the skin. Common electrodes used for iontophoretic drug delivery are : PowerPoint Presentation: Pharmacokinetics of Ion Transfer Transdermal iontophoresis delivers medication at a constant rate so that the effective plasma concentration remains within a therapeutic window for an extended period of time. 13 Iontophoresis appears to overcome the resistive properties of the skin to charged ions Iontophoresis decreases absorption lag time while increasing delivery rate when compared with passive skin application Iontophoresis provides both a spiked and sustained release of a drug Rate at which an ion may be delivered is determined by a number of factors The concentration of the ion The pH of the solution Molecular size of the solute Current density Duration of the treatment PowerPoint Presentation: 14 PowerPoint Presentation: 15 Commercially developed Iontophoretic delivery systems ZECUITY – To Deliver Sumatriptan for Migraines (NDA222278- Approved on 17 Jan 2013) IONSYS Fantanyl HCl (NDA 21338, 22 May 2006) LIDOSITE ® - To deliver lidocaine , an anesthetic agent. (NDA21504, 06 May2004) IONTOCAIN (NDA 20530 , 21 Dec 1995) EMPY LIDOPEL (NDA 21489, 26 OCT 2004) Phoresor ® II - To deliver botulinum molecule which is used for the treatment of hyperhydrosis . PowerPoint Presentation: 16 Objective and Plan of Work PowerPoint Presentation: 17 Plan of the work PowerPoint Presentation: 18 Drug Profile of  Captopril Chemical structure: PowerPoint Presentation: 19 Drug Profile of  Lisinopril Chemical structure: : 20 Materials & Methodology PowerPoint Presentation: 21 Instruments & Apparatus PowerPoint Presentation: 22 Photograph of DC source & Iontophoretic Diffusion cell used in this study PowerPoint Presentation: 23 Methodology PowerPoint Presentation: Preparation of Pig Skin: From a local abattoir, pig ear was obtained. The skin was removed carefully from the outer regions of the ear and separated from the underlying cartilage with a scalpel. Fat was removed using a scalpel and isopropyl alcohol. Finally the skin was washed with tap water and stored at refrigerator in aluminum foil packing and used within two days. Preparation of Rabbit Skin: The Rabbits were sacrificed by the I.V injection of chloroform. Skin samples were obtained from the back area of rabbits. The adherent fat and other visceral debris were removed. 24 Preparation of Skin PowerPoint Presentation: 25 Passive Permeation Studies (in-vitro) PowerPoint Presentation: 26 Procedure for Iontophoretic Permeation studies: PowerPoint Presentation: Permeation Enhancement by Chemical Enhancers : DMSO, Peppermint oil, Menthol, Oleic acid, SLS, PEG were used. Preparation of Gel formulation A polymer gel was prepared using HPMC Estimation of the drug (Content uniformity and in vitro diffusion study) Analysis of the samples were performed with Waters binary gradient HPLC system Estimation of Drugs in Blood Samples Blood was directly collected into vacuum tube (BD vacutainer TM) from rabbit ear vein Drug Content Analysis Content uniformity of the gel formulation was determined in cellulose membrane 27 PowerPoint Presentation: Physical Examination: The prepared gels were visually inspected for clarity, color and transparency. Determination of the viscosity and pH Viscosity of the gel formulations were determined using DV-E (BrookfieldViscometer) For determination of pH Digital pH meter as used. Compatibility studies The IR studies were performed to check the compatibility of excipients. Spectra of Pure drugs and formulations were taken individually by the potassium bromide pellet method using FTIR spectrophotometer Stability Studies The short term stability studies of formulated gels were carried out at different temperature and humidity according to ICH guidelines 28 PowerPoint Presentation: 29 Fig A schematic representation of the transdermal iontophoresis set up used in the study In-vivo Pharmacokinetic Study PowerPoint Presentation: Data analysis KP = JSS / Cd ……………. (1) D = KP h / K …………….. (2) where Kp represents permeability coefficient, Jss is the steady-state flux, Cd is the concentration of drug in donor compartment, D is the diffusion coefficient, K is the skin/vehicle partition coefficient and h the thickness of the skin. Statistical analysis One-way ANOVA Two-way ANOVA Bonferroni’s test 30 Data Analysis PowerPoint Presentation: 31 Results & Discussion PowerPoint Presentation: 32 Physicochemical Parameters of Captopril Trial No. Solubility Partition Coefficient Octanol /Water pKa Molecular Weight 0.9% NaCl mg/ml Water mg/ml 1 146.9 157.3 0.334 3.492 217.29 2 145.2 156.7 0.329 3.471 3 143.8 158.4 0.341 3.480 Mean 145.13 157.46 0.334 3.481 SD ±1.3012 ±0.8621 ±0.0060 ±0.0105 PowerPoint Presentation: 33 Experimental Design Different Donor System and their Composition Experimental Code Concentration of drug in Donor ( mg /ml) System-A 25 System-B 50 System-C 100  To evaluate this effect of concentration & Current the experiment was designed at three different drug concentrations & three different current densities. Effect of permeation enhancer on iontophoretic delivery also observed using various enhancers. Experimental Code Current Densities (mA/cm 2 ) System-A1 0.25 System-A2 0.5 System-A3 0.75 Effect of Concentrations Effect of Current PowerPoint Presentation: 34 Iontophoretic Passive Cumulative Permeation Profile of Captopril at different donor Concentrations. In passive process both rate and extent of permeation increased with increasing donor drug concentration In contrast iontophoresis concentration effects was found upto certain points. Each point represents the Mean  S.E. of three observations: Each point represents the Mean  S.E. of three observations 35 Comparison of hourly Flux Comparison of Cumulative Permeation . Overall iontophoretic permeability was significantly higher than that of their passive value . In passive process the rate of permeation was more or less same at all time point whereas Iontophoretic permeation was less linear . Competition by chloride ion is suggested to be the cause . Passive & Iontophoretic Permeation of Captopril in System-A PowerPoint Presentation: 36 Comparison of Cumulative Permeation of Captopril in System-B Comparison of hourly Flux of Captopril in System-B. Passive & Iontophoretic Permeation of Captopril in System-B &C Comparison of hourly Flux ofCaptopril in System-C. Comparison of Cumulative Permeation of Captopril in System-C. PowerPoint Presentation: 37 Comparison of Permeability & Diffusion Coefficients of Captopril by Passive and Iontophoresis Donor System Permeability Coefficient (cm/hr) Diffusion coefficient (cm 2 /s) Passive Iontophoretic Passive Iontophoretic System- A 29.0734* 10 -3 70.9476 * 10 -3 0.266* 10 -5 0.644* 10 -5 System-B 23.20223* 10 -3 54.29643 * 10 -3 0.211* 10 -5 0.495 *10 -5 System-C 21.30094* 10 -3 41.91307* 10 -3 0.19* 10 -5 0.382 * 10 -5 Permeability coefficients decreased with the increase in donor concentration. PowerPoint Presentation: 38 Enhancement Ratio and Benefit by Iontophoresis ( Captopril ) Donor System Steady State flux (  mol/ hr.cm 2 ) Benefit by Iontophoresis (  mol/hr.cm 2 ) Enhancement Ratio (R) Passive Iontophoretic System-A 3.345  0.39 8.1273  1.436 4.7823 2.430 System-B 5.339  0.165 12.494  0.687 7.155 2.3147 System-C 9.803  0.0149 19.289  0.0546 9.486 1.9676 Enhancement was highest at the lowest drug load and lowest at the highest drug load. The iontophoretic contribution is found to be slightly more at higher donor concentrations PowerPoint Presentation: Experimental Code Current Densities ( mA /c m 2 ) System-A1 0.25 System-A2 0.5 System-A3 0.75 39 Effect of Current Densities on Permeation of Captopril To evaluate the effect of Current the experiment was designed at three different current densities, as the density of current was Increased, permeation was found to be increased. Cumulative amount permeated Vs Time PowerPoint Presentation: 40 Cumulative Permeation Profile of Captopril with different permeation enhancers and Iontophoresis. Effect of Permeation Enhancers on Permeation of Captopril PowerPoint Presentation: Mode of Permeation/ Enhancer Cumulative amount Permeated at 8 hour (  mol/cm 2 ) (mean ± SD) Permeability Coefficient (cm/hr) Diffusion Coefficient (cm 2 /s) Passive 21.245 ± 1.285 0.0291 0.266*10 -5 DMSO 39.778 ± 1.231 0.0463 0.424*10 -5 Peppermint oil 34.993 ± 0.908 0.0397 0.363*10 -5 Menthol 32.786 ± 0.873 0.0381 0.348*10 -5 Oleic acid 30.699 ± 0.871 0.0353 0.323*10 -5 SLS 28.177 ± 0.916 0.0323 0.295*10 -5 PEG 24.861 ± 0.951 0.0297 0.272*10 -5 Iontophoresis 71.103 ± 3.485 0.0706 0.646*10 -5 Ionto + DMSO 103.940 ± 0.532 0.1293 1.183*10 -5 Ionto + Peppermint oil 98.221 ± 0.550 0.1247 1.141*10 -5 Ionto +Menthol 95.231± 0.358 0.1234 1.129*10 -5 Ionto +Oleic acid 93.430 ± 0.260 0.1212 1.109*10 -5 Ionto +SLS 88.554 ± 0.432 0.1147 1.050*10 -5 Ionto +PEG 82.799 ± 1.034 0.1072 0.981*10 -5 41 Cumulative Amount Permeation, Permeability Coefficients, and Diffusion Coefficients of Captopril (n=3) PowerPoint Presentation: Mode of Permeation/Enhancer Steady state fluxes (  mol/cm 2 /hr) (mean ± SD) Benefit by enhancers (  mol/cm 2 /hr) Enhancement Ratio Passive 3.345 ± 1.311 0 1 DMSO 5.328 ± 1.147 1.983 1.592 Peppermint oil 4.563 ± 1.025 1.217 1.364 Menthol 4.378 ± 1.020 1.033 1.308 Oleic acid 4.067 ± 0.802 0.721 1.215 SLS 3.716 ± 0.915 0.370 1.110 PEG 3.417 ± 0.955 0.072 1.021 Iontophoresis 8.127 ± 0.745 4.782 2.429 Ionto + DMSO 14.878 ± 0.707 11.533 4.447 Ionto + Peppermint oil 14.348± 0.478 11.003 4.289 Ionto +Menthol 14.202± 0.386 10.857 4.245 Ionto +Oleic acid 13.949± 0.317 10.603 4.170 Ionto +SLS 13.199± 0.336 9.853 3.945 Ionto +PEG 12.332± 0.915 8.987 3.686 42 Benefit and Enhancement Ratios by Different Permeation Enhancers for Captopril PowerPoint Presentation: 43 Comparison of steady state fluxes ( Captopril ) with different enhancers and iontophoresis Steady state fluxes increase in the following order Passive < PEG < SLS < Oleic acid < Menthol< Peppermint oil < DMSO< Iontophoresis < (Ionto+PEG) < (Ionto+SLS) < (Ionto+Oleic acid) < (Ionto+Menthol)< (Ionto+Peppermint oil) < (ionto+ DMSO). PowerPoint Presentation: 44 Pig skin Rabbit skin Comparison of passive and iontophoretic permeation of Captopril in excised pigskin and Rabbit Skin . In-vitro Permeation Studies of Captopril Gel PowerPoint Presentation: 45 Fig. Passive Fig. Iontophoresis Comparison of Rabbit and Pig Skin by permeation of Captopril In passive and iontophoresis Comparison of Rabbit and Pig Skin by permeation of Captopril Results showed that permeability of rabbit skin was much higher than compare to pig skin PowerPoint Presentation: Parameters Process Pig Skin Rabbit skin Steady State Fluxes (  g /hr. cm 2 ) Passive 32.200 40.137 Iontophoresis 162.185 251.471 Permeability Coefficients (cm/h) Passive 1.28×10 -3 1.605×10 -3 Iontophoresis 6.48×10 -3 10.05×10 -3 Enhancement Ratio (R) (Ionto /Passive) 5.036 6.265 Net Benefit of Iontophoresis (  g /hr. cm 2 ) ( Ionto -Passive) 129.985 211.333 46 Steady State Fluxes, Permeability Coefficients, and Enhancement Ratio of Captopril in Rabbit and Pig skin from Gel Formulation PowerPoint Presentation: 47 Plasma Concentration of Captopril after Passive and Iontophoretic Administration of Captopril Gel in Rabbits Very less amount of Captopril was determined in plasma after passive diffusion but as expected it was considerably higher when Iontophoresis was used in the study. PowerPoint Presentation: 48 IR spectra of Pure Drug-Captopril IR spectra of Captopril Formulation Compatibility Studies PowerPoint Presentation: S. NO Parameters Initial (0 days) 25±2° C (60±5%RH) 40±2° C (75±5%RH) 15 days 30 days 15 days 30 days 1 Physical Appearance Clear and transparent Clear and transparent Clear and transparent Clear and transparent Clear and transparent 2 Viscosity (cps) 14241.67 ±88.0814 14161.67 ± 128 14135.67 ± 46.44 14125.67 ± 70.57 14117.67 ± 113.36 3 pH 7.13 ± 0.11 6.99 ± 0.28 6.71 ± 0.24 6.46 ± 0.07 6.4 ± 0.02 4 Drug Contents(%) 99.13 ± 0.91 98.83 ± 0.25 98.83 ± 0.84 98.3 ± 0.85 98.7 ± 0.85 5 CAP* 2059.467 ± 92.147 2011.689 ± 111.306 2076.824 ± 87.208 1992.597 ± 86.039 2083.547 ± 86.843 49 Stability Studies of Captopril Gel at various Temperatures and Humidities *Cumulative Amount Permeated at end of 8th hour (  g/cm 2) by Iontophoresis. PowerPoint Presentation: 50 Iontophoretic Passive Cumulative Permeation Profile of Lisinopril at different donor Concentrations.  In passive process both rate and extent of permeation increased with increasing donor drug concentration  In contrast iontophoresis concentration effects was found upto certain points. LISINOPRIL RESULTS Each point represents the mean  S.E. of three observations: Each point represents the mean  S.E. of three observations 51 Comparison of hourly Flux Comparison of Cumulative Permeation.  In passive process the rate of permeation was more or less same at all time point whereas iontophoretic permeation was less linear .  Overall Iontophoretic permeability was significantly higher than that of their passive value . Passive & Iontophoretic Permeation of Lisinopril in System-A PowerPoint Presentation: 52 Comparison of Cumulative Permeation of Lisinopril in System-B Comparison of hourly Flux of Lisinopril in System-B. Passive & Iontophoretic Permeation of Lisinopril in System-B &C Comparison of hourly Flux of Lisinopril in System-C. Comparison of Cumulative Permeation of Lisinopril in System-C. PowerPoint Presentation: 53 Comparison of Permeation & Diffusion Coefficients of Lisinopril by Passive and Iontophoresis Donor System Permeability Coefficient (cm/hr) Diffusion coefficient (cm 2 /s) Passive Iontophoretic Passive Iontophoretic System- A 0.0252 0.0797 0.1147* 10 -5 0.3629* 10 -5 System-B 0.0250 0.0789 0.1138* 10 -5 0.359* 10 -5 System-C 0.0235 0.0543 0.1070* 10 -5 0.247* 10 -5  Permeability coefficients decreased with the increase in donor concentration. PowerPoint Presentation: 54 Enhancement Ratio and Benefit by Iontophoresis ( Lisinopril ) Donor System Steady State flux (  mol/ hr.cm 2 ) Benefit by Iontophoresis (  mol/hr.cm 2 ) Enhancement Ratio (R) Passive Iontophoretic System-A 1.429 4.517 3.088 3.160 System-B 2.841 8.636 5.795 3.0397 System-C 3.998 9.227 5.229 2.3079  Enhancement was highest at the lowest drug load and lowest at the highest drug load. PowerPoint Presentation: Experimental Code Current Densities ( mA /cm 2 ) System-A1 0.25 System-A2 0.5 System-A3 0.75 55 Effect of Current Densities on Permeation of Lisinopril To evaluate the effect of Current the experiment was designed at three different current densities, as the density of current was Increased, permeation was found to be increased. Cumulative Amount Permeated Vs Time PowerPoint Presentation: 56 Cumulative Permeation Profile of Lisinopril with different Permeation Enhancers and Iontophoresis. Effect of Permeation Enhancers on Permeation of Lisinopril PowerPoint Presentation: Mode of Permeation/Enhancer Cumulative amount Permeated at 8 hour (  g/cm 2 ) (mean ± SD) Permeability Coefficient (cm/hr) Diffusion Coefficient (cm 2 /s) × 10 -5 Passive (Pure Drug) 9.666 ± 0.285 0.0116 0.053 DMSO 18.260 ± 0.114 0.0222 0.101 Peppermint oil 16.347 ± 0.102 0.0191 0.086 Menthol 15.386 ± 0.083 0.0170 0.077 Oleic acid 14.436 ± 0.224 0.0163 0.074 SLS 12.946 ± 0.043 0.0147 0.066 PEG 12.242 ± 0.150 0.0141 0.064 Iontophoresis 28.944 ± 1.485 0.0365 0.165 Ionto + DMSO 44.506 ± 1.210 0.0548 0.248 Ionto + Peppermint oil 43.865 ± 3.141 0.0540 0.244 Ionto +Menthol 42.884 ± 3.212 0.0533 0.241 Ionto +Oleic acid 40.031 ± 2.803 0.0508 0.23 Ionto +SLS 37.040 ± 3.186 0.0484 0.219 Ionto +PEG 35.213 ± 2.921 0.0467 0.211 57 Cumulative amount permeation, Permeability Coefficients, and Diffusion Coefficients of Lisinopril PowerPoint Presentation: Mode of Permeation/Enhancer Steady state fluxes (  g/cm 2 /hr) (mean ± SD) Benefit by enhancers (  g/cm 2 /hr) Enhancement Ratio Passive (Pure Drug) 1.338 ± 0.211 0 1 DMSO 2.556 ± 0.147 1.2175 1.9099 Peppermint oil 2.193 ± 0.325 0.8547 1.6388 Menthol 1.950 ± 0.502 0.6122 1.4575 Oleic acid 1.872 ± 0.602 0.5342 1.3992 SLS 1.687 ± 0.515 0.3493 1.2611 PEG 1.618 ± 0.355 0.2797 1.2090 Iontophoresis (Pure Drug) 4.198 ± 0.445 2.8595 3.1371 Ionto + DMSO 6.302 ± 0.507 4.9635 4.7096 Ionto + Peppermint oil 6.209 ± 0.478 4.8712 4.6406 Ionto +Menthol 6.131 ± 0.386 4.7933 4.5825 Ionto +Oleic acid 5.848 ± 0.317 4.5097 4.3705 Ionto +SLS 5.571 ± 0.336 4.2330 4.1637 Ionto +PEG 5.371 ± 0.615 4.0325 4.0138 58 Benefit and Enhancement Ratio by Different Permeation Enhancers for Lisinopril PowerPoint Presentation: 59 Steady state fluxes increase in the following order Pure drug < PEG < SLS < Oleic acid < Menthol< Peppermint oil < DMSO< Iontophoresis < (Ionto+PEG) < (Ionto+SLS) < (Ionto+Oleic acid) < (Ionto+Menthol)< (Ionto+Peppermint oil) < (ionto+ DMSO). Comparison of steady state fluxes ( Lisinopril ) with different enhancers and iontophoresis PowerPoint Presentation: 60 Fig Pig skin Fig Rabbit skin Comparison of passive and iontophoretic permeation of Lisinopril in excised pigskin and Rabbit Skin . In-vitro permeation studies of Lisinopril Gel PowerPoint Presentation: 61 Fig. Passive Fig. Iontophoresis Comparison of Rabbit and Pig Skin by permeation of Lisinopril In passive and iontophoresis Comparative Permeation of Lisinopril through Rabbit and Pig Skin  Results showed that permeability of rabbit skin was much higher than compare to pigskin PowerPoint Presentation: Parameters Process Pig skin Rabbit skin Steady State Fluxes (  g /hr. cm 2 ) Passive 1.203 1.387 Iontophoresis 5.01 6.402 Permeability Coefficients (cm/h) Passive 0.048×10 -3 0.055×10 -3 Iontophoresis 0.20×10 -3 0.256×10 -3 Enhancement Ratio (R) ( Iontophoresis / Passive) 4.164 4.615 Net Benefit of Iontophoresis (  g/hr.cm 2 ) (Iontophoresis- Passive) 3.807 5.015 62 Steady State Fluxes, Permeability Coefficients, and Enhancement Ratio of Lisinopril in Rabbit and Pig skin from Gel Formulation. PowerPoint Presentation: 63 Plasma Concentration of Lisinopril after Passive and Iontophoretic administration of Lisinopril Gel in Rabbits  Very less amount of Lisinopril was determined in plasma after passive diffusion but as expected it was considerably higher when iontophoresis was used in the study PowerPoint Presentation: 64 IR Spectra of Pure Drug-Lisinopril IR Spectra of Lisinopril Formulation Compatibility Studies PowerPoint Presentation: S.N Parametes Initial (0 days) 25±2° C (60±5%RH) 40±2° C (75±5%RH) 15 days 30 days 15 days 30 days 1 Physical Appearance Clear and transparent Clear and transparent Clear and transparent Clear and transparent Clear and transparent 2 Viscosity (cps) 13162 ± 127.42 13128.67 ± 37.61 13122.33 ± 68.63 13115.67 ± 116.79 13162 ± 127.42 3 pH 7.06 ± 0.08 6.95 ± 0.16 6.78 ± 0.25 6.48 ± 0.1 6.41 ± 0.04 4 Drug Contents(%) 99.13 ± 0.91 98.83 ± 0.25 98.83 ± 0.84 98.3 ± 0.85 98.7 ± 0.85 5 CAP* 53.527 ± 5.504 54.814 ± 10.993 56.768 ± 4.364 57.406 ± 14.092 56.386 ± 11.622 65 Stability Studies of Lisinopril Gel at various Temperatures and Humidities *Cumulative Amount Permeated at end of 8th hour (  g/cm 2) by iontophoresis. PowerPoint Presentation: 66 In-vitro and In-Vivo iontophoretic transdermal delivery of Captopril & Lisinopril were investigated. At all concentration levels iontophoresis considerably increased the permeation rate compared to passive controls. Flux enhancement was highest at the lowest drug load and lowest at the highest drug load. As the current densities increased, permeation was found to increased. The non compartmental analysis of the pharmacokinetic data indicate that to meet the demand of maintenance therapy for 60 kg individual 1488 μg of Captopril and 26.7  g of Lisinopril must be supplied to the systemic circulation every hour. The in-vitro iontophoretic fluxes of drug formulations through rabbit skin were found to be 251.471  g/hr.cm 2 and 6.402  g/hr. cm 2 for Captopril and Lisinopril respectively, in our studies. As the Patch in the market usually have wider area (10 cm 2 and above), it can be expected to achieve the target. Overall results looked quite promising for transdermal delivery of Captopril and Lisinopril. Conclusion PowerPoint Presentation: 67 Banga AK. Electrically Assisted Transdermal and Topical Drug Delivery. Taylar & Francis Ltd . 1998; pp 1-32. Tripathi KD. Essentials of Medical Pharmacology. 5th ed. New Delhi: Jaypee Brothers Publishing house; 2004. Gupta A, Prajapati SK, Balamurugan M, Singh M, Bhatia D. Design and Development of a Proniosomal Transdermal Drug Delivery System for Captopril. Tropical Journal of Pharmaceutical Research 2007; 6(2): 687-693.. Aqil M, Chaudhary BI, Sultan Y, Talegaonkar S, Ahmad FJ, Aji MM. Transdermal therapeutic system of enalapril maleate using piperidine enhancer. Current Drug Deliv. 2008; 5(2): 148-152 Anroop B, Ghosh B, Parcha V, Khanam J. Transdermal delivery of atenolol: effect of prodrugs and iontophoresis. Curr Drug Del 2009; 6: 280-290. Omray LK, Kohli S, Khopade AJ, Gajbhiye A, Agrawal GP. Development of mesophasic microreservoir-based transdermal drug delivery system of propranolol. Ind J Pharma Sci 2008; 70(5): 578-584. Chien YW. Development of Transdermal drug delivery systems. Drug Dev Ind ……………… Bibliography PowerPoint Presentation: 68 A Jain , S Nayak, V Soni. Iontophoretic permeation of Lisinopril at different current densities and drug concentrations. Advanced Pharmaceutical Bulletin 2012; 2(2):239-244. 2. A Jain, S Nayak, V Soni ,  Effect of Enhancers and Iontophoresis on Captopril Permeability through Excised Pig Skin. Journal Applied Pharmacy 2012; 2(04): 556-566. 3. A Jain , S Nayak, V Soni . Synergistic Effect of Iontophoresis and Enhancers on Transdermal Delivery of Lisinopril. Inventi Impact: Pharm Tech 2012; 2. 4. A Jain, A Mishra, S Nayak, V Soni . Transdermal Delivery of Antihypertensive Agents: A tabular update. International Journal of Drug Delivery 2010; 3: 01-13. 5. A Jain , S Nayak, V Soni. In-Vitro  and  In-Vivo Transdermal Iontophoretic Delivery of Lisinopril Gel. Journal of Applied Pharmacy 03(04): 655-664; July, 2012. 6. A Jain , S Nayak, V Soni. Passive and Iontophoretic Permeation of Captopril Gel: An In-Vitro and In-Vivo Study. Indonesian J. Pharm. 2012; 23(2): 122 – 131 7. A Jain, S Nayak, V Soni. Study of Transdermal Delivery of Captopril Using Iontophoresis, Journal of Pharmaceutical and Biomedical Sciences 2011; 4(11). List of Publications PowerPoint Presentation: Thank you Ashish Jain [email protected] www.bansalpharmacy.com

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