scholarly journals Development and Evaluation of Microemulsions for Transdermal Delivery of Insulin

2011 ◽  
Vol 2011 ◽  
pp. 1-7 ◽  
Author(s):  
Jadupati Malakar ◽  
Suma Oomen Sen ◽  
Amit Kumar Nayak ◽  
Kalyan Kumar Sen
Keyword(s):  
Oleic Acid ◽  
Transdermal Delivery ◽  
Isopropyl Alcohol ◽  
Mouse Skin ◽  
Tween 80 ◽  
Isopropyl Myristate ◽  
Permeation Flux ◽  
Goat Skin ◽  
Surfactant Phase

Insulin-loaded microemulsions for transdermal delivery were developed using isopropyl myristate or oleic acid as the oil phase, Tween 80 as the surfactant, and isopropyl alcohol as the cosurfactant. The pseudoternary phase diagrams were constructed to determine the composition of microemulsions. The insulin permeation flux of microemulsions containing oleic acid as oil phase through excised mouse skin and goat skin was comparatively greater than that of microemulsions containing isopropyl myristate as oil phase. The insulin-loaded microemulsion containing 10% oleic acid, 38% aqueous phase, and 50% surfactant phase with 2% dimethyl sulfoxide (DMSO) as permeation enhancer showed maximum permeation flux (4.93 ± 0.12 μg/cm2/hour) through goat skin. The in vitro insulin permeation from these microemulsions was found to follow the Korsmeyer-Peppas model (R2=0.923 to 0.973) over a period of 24 hours with non-Fickian, “anomalous” mechanism. Together these preliminary data indicate the promise of microemulsions for transdermal delivery of insulin.

scholarly journals Ondansetron HCl Microemulsions for Transdermal Delivery: Formulation and In Vitro Skin Permeation

2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
Jadupati Malakar ◽  
Amit Kumar Nayak ◽  
Aalok Basu
Keyword(s):  
Transdermal Delivery ◽  
Isopropyl Alcohol ◽  
Skin Permeation ◽  
Tween 80 ◽  
Oral Route ◽  
Isopropyl Myristate ◽  
Surfactant Phase ◽  
In Vitro Skin Permeation ◽  
Pass Metabolism

Ondansetron HCl delivery through oral route suffers due to its low bioavailability due to first-pass metabolism. Therefore, the microemulsion-based transdermal delivery may be a better substitute for it. The pseudoternary phase diagrams were constructed to determine compositions of microemulsions, and ondansetron HCl microemulsions for transdermal delivery were developed using isopropyl myristate or oleic acid as the oil phase, Tween 80 as the surfactant, and isopropyl alcohol as the cosurfactant evaluated for in vitro skin permeation through excised porcine skin. The in vitro skin permeation from these formulated microemulsions was sustained over 24 hours. The microemulsion F-8 (contained 10% of isopropyl myristate as oil phase, 8% of aqueous phase, and 82% of surfactant phase containing Tween 80 and isopropyl alcohol, 3 : 1) showed the highest permeation flux of 0.284±0.003 μg/cm2/hour. All these microemulsions followed the Korsmeyer-Peppas model (R2=0.971  to  0.998) with non-Fickian, “anomalous” mechanism over a period of 24 hours.

scholarly journals Transdermal Delivery of Lidocaine-Loaded Elastic Nano-Liposomes with Microneedle Array Pretreatment

Biomedicines ◽  
2021 ◽  
Vol 9 (6) ◽  
pp. 592
Author(s):  
Yang Liu ◽  
Maosen Cheng ◽  
Junqi Zhao ◽  
Xiaoying Zhang ◽  
Zhen Huang ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Mouse Skin ◽  
Onset Time ◽  
Tween 80 ◽  
Component Ratio ◽  
Anesthetic Effect ◽  
Span 80 ◽  
Franz Diffusion Cells

This study aimed to improve the transdermal delivery of lidocaine hydrochloride (LidH) using elastic nano-liposomes (ENLs) and microneedle (MN) array pretreatment. LidH-containing ENLs were prepared using soybean phosphatidylcholine and cholesterol, with Span 80 or Tween 80, using a reverse-phase evaporation method. The ENL particle size, stability, and encapsulation efficiency (EE) were characterized and optimized based on the component ratio, pH, and type of surfactant used. In vitro transdermal diffusion study was performed on MN-pretreated mouse skin using Franz diffusion cells. The anesthetic effects of LidH in various formulations after dermal application were evaluated in vivo in rats by measuring the tail withdrawal latency after photothermic stimulation. Stable LidH-loaded Tween 80 or Span 80 ENLs were obtained with particle sizes of 115.8 and 146.6 nm and EEs of 27% and 20%, respectively. The formulations did not exert any cytotoxicity in HaCaT cells. Tween 80 and Span 80 ENL formulations showed enhanced LidH delivery on pretreated mice skin in vitro and prolonged the anesthetic effect in vivo compared to that by LidH application alone. LidH-loaded ENLs applied to MN-pretreated skin can shorten the onset time and prolong the anesthetic effect safely, which merits their further optimization and practical application.

scholarly journals Influence of Oleic Acid on the Rheology and in Vitro Release of Lumiracoxib from Poloxamer Gels

2010 ◽  
Vol 13 (2) ◽  
pp. 286 ◽  
Author(s):  
Tailane Sant´Anna Moreira ◽  
Valéria Pereira De Sousa ◽  
Maria Bernadete Riemma Pierre
Keyword(s):  
Oleic Acid ◽  
Rheological Behavior ◽  
Transdermal Delivery ◽  
In Vitro Release ◽  
Delivery Systems ◽  
Penetration Enhancer ◽  
Release Studies ◽  
Vitro Release ◽  
Gel Transition

Abstract PURPOSE: Transdermal delivery of anti-inflammatory lumiracoxib (LM) could be an interesting strategy to avoid the side effects associated with systemic delivery, but it is ineffective due to the drug poor skin penetration. We have investigated the effects of oleic acid (OA), a lipid penetration enhancer, on the in vitro release of LM from poloxamer-based delivery systems (PBDS). The rheological behavior (shear rate dependent viscosity) and gelation temperature through measurements of optimal sol-gel transition temperatures (Tsol-gel) were also carried out in these systems. METHODS: In vitro release studies of LM from PBDS were performed using cellulose acetate as artificial membrane mounted in a diffusion system. The amount of LM released was divided by exposition area (µg/cm2) and these values were plotted as function of the time (h). The flux of the drug across the membrane (J) was calculated from the slope of the linear portion of the plot and expressed as µg/cm2. h -1. The determination of viscosity was carried out at different shear rates (γ) between 0.1- 1000 S-1 using a parallel plate rheometer. Oscillatory measurements using a cone-plate geometry rheometer surrounded by a double jacket with temperature varying 4-40°C, was used in order to determine Tsol-gel. RESULTS: Increase of both polymer and OA concentrations increases the viscosity of the gels and consequently reduces the in vitro LM release from the PBDS, mainly for gels containing OA at 10.0% compared to other concentrations of the penetration enhancer. Tsol-gel transition temperature was decreased by increasing viscosity; in some cases the formulation was already a gel at room temperature. Rheological studies showed a pseudoplastic behavior, which facilitates the flow and improves the spreading characteristics of the formulations. CONCLUSIONS: Taken together, the results showed that poloxamer gels are good potential delivery systems for LM, leading to a sustained release, and also have appropriate rheological characteristics. Novelty of the work: A transdermal delivery of non-steroidal antinflammatory drugs like lumiracoxib (LM) can be an interesting alternative to the oral route of this drug, since it was recently withdraw of the market due to the liver damage when systemically administered in tablets as dosage form. There are no transdermal formulations of LM and it could be an alternative to treat inflammation caused by arthritis or arthrosis. Then, an adequate delivery system to LM is necessary in order to release the drug properly from the PBDS as well as have good characteristics related to semi-solid preparations for transdermal application, which were evaluated through in vitro release studies and rheological behavior in this paper, respectively.

scholarly journals Design, development and evaluation of novel nanoemulsion formulations for transdermal potential of celecoxib

2007 ◽  
Vol 57 (3) ◽  
pp. 315-332 ◽  
Author(s):  
Sanjula Baboota ◽  
Faiyaz Shakeel ◽  
Alka Ahuja ◽  
Javed Ali ◽  
Sheikh Shafiq
Keyword(s):  
Transdermal Delivery ◽  
Permeability Coefficient ◽  
Skin Permeation ◽  
Tween 80 ◽  
Surfactant Mixture ◽  
Design Development ◽  
Paw Edema ◽  
Steady State Flux ◽  
Nanoemulsion Gel

Design, development and evaluation of novel nanoemulsion formulations for transdermal potential of celecoxibThe aim of the present study was to investigate the potential of nanoemulsion formulations for transdermal delivery of celecoxib (CXB). Thein vitroskin permeation profile of optimized formulations was compared with CXB gel and nanoemulsion gel. Significant increase in the steady state flux (Jss), permeability coefficient (Kp) and enhancement ratio (Er) was observed in nanoemulsion formulations T1 and T2 (p< 0.05). The highest value of these permeability parameters was obtained in formulation T2, which consisted of 2% (m/m) of CXB, 10% (m/m) of oil phase (Sefsol 218 and Triacetin), 50% (m/m) of surfactant mixture (Tween-80 and Transcutol-P) and 40% (m/m) water. The anti-inflammatory effects of formulation T2 showed a significant increase (p< 0.05) in inhibition after 24 h compared to CXB gel and nanoemulsion gel on carrageenan-induced paw edema in rats. These results suggested that nanoemulsions are potential vehicles for improved transdermal delivery of CXB.

scholarly journals Formulation and Characterization of Felodipine as an Oral Nanoemulsions

2021 ◽  
Vol 30 (1) ◽  
pp. 209-217
Author(s):  
Sumaya B. Hamed ◽  
Shaimaa N. Abd Alhammid
Keyword(s):  
Particle Size ◽  
Oleic Acid ◽  
Zeta Potential ◽  
Water Solubility ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Compatibility Study ◽  
Drug Content ◽  
Drug Molecules

            Felodipine is a calcium-channel blocker with low aqueous solubility and bioavailability. Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE) is one of the popular methods that has been used to solve the dispersibility problems of many drugs. Felodipine was formulated as a NE utilizing oleic acid as an oil phase, tween 80 and tween 60 as surfactants and ethanol as a co-surfactant. Eight formulas were prepared, and different tests were performed to ensure the stability of the NEs, such as particle size, polydispersity index, zeta potential, dilution test, drug content, viscosity and in-vitro drug release. Results of characterization showed that felodipine nanoemulsion (F3) with (oleic acid 10%) ,(Smix 60% of tween80 :ethanol in a ratio of 3:1), (DDW 30%) was selected as the best formula, since it has a particle size of (17.01)nm, low PDI (0.392), zeta potential (-22.34mV), good dilution without drug precipitation , higher percent of drug content (99.098%) with  acceptable viscosity , and complete release of the drug after (45 min.) with significantly higher (P<0.05)   dissolution  rate in comparison with the pure drug powder. The selected formula (F3) subjected to further investigations as drug and excipient compatibility study by Fourier transform infrared spectroscopy (FTIR) The outcomes of the (FTIR) explain that the distinctive peaks for felodipine were not affected by other components and displayed the same functional group's band with very slight shifting. This indicates that there was no interaction between felodipine and other NE components. Therefore, these excipients were found to be compatible with felodipine. In conclusion, the NE was found to be an efficient method to enhance the dispersibility and permeatioins of drugs that have poor water solubility (lipophilic drugs).

scholarly journals Oleic Acid Based Emulgel for Topical Delivery of Ofloxacin

2019 ◽  
Vol 9 (4-A) ◽  
pp. 183-190
Author(s):  
A. Manaswitha ◽  
P. V. L. D. Sai Swetha ◽  
N.K.D. Devi ◽  
K. Naveen Babu ◽  
K. Ravi Shankar
Keyword(s):  
Oleic Acid ◽  
Drug Release ◽  
Ph Value ◽  
Liquid Paraffin ◽  
Tween 80 ◽  
Gelling Agent ◽  
Compatibility Study ◽  
Zero Order Kinetics ◽  
Carbopol 940

The objective of the present study is to formulate and evaluate ofloxacin emulgel. Emulgel formulations of ofloxacin were prepared using different concentrations of gelling agent’s Carbopol-940 and Xanthum gum. Tween-80 and span-80 were used as emulsifiers and propylene glycol as a humectant in the preparation of emulgel. The effect of the concentration of gelling agent on the drug release from the prepared emulgel was investigated. The compatibility study was conducted using Fourier-transform infrared (FTIR). The formulated emulgel was characterized by their physical appearance, pH determination, viscosity, spreadability, drug content, microbial test and in vitro diffusion study. FTIR indicated that the drug and excipients used in the study are compatible with each other. All the prepared formulations showed acceptable physical properties, homogeneity, consistency, spreadability, viscosity, and pH value. Drug release from all the formulations depended upon the concentration of the polymer used. As the concentration of Carbopol 940 increased the spreadability and drug release was found to be decreased. Emulgels formulated with oleic acid gave a much higher release rate of ofloxacin than emulgels formulated with liquid paraffin. The release of drug from all the emulgels prepared followed Zero-order kinetics. The linear Higuchi plots indicated that the drug release from all the emulgels prepared followed diffusion kinetics. Emulgel formulated with oleic acid exhibited greater flux when compared with those formulated with liquid paraffin. The formulations were found to be stable during stability testing. It can be concluded that Carbopol 940 and oleic acid are recommended for the formulation and preparation of Ofloxacin emulgels for topical drug delivery. Key words: Ofloxacin, Emulgel, Spreadibility, Zone of inhibition.

scholarly journals THERAPEUTIC MICROEMULSION OF CURCUMIN FOR THE MANAGEMENT OF OSTEOARTHRITIS

2018 ◽  
Vol 8 (5-s) ◽  
pp. 341-347
Author(s):  
Shreyasi Sharma ◽  
Eisha Ganju ◽  
Neeraj Upmanyu ◽  
Prabhat Jain
Keyword(s):  
Oleic Acid ◽  
Zeta Potential ◽  
Antioxidant Activities ◽  
In Vitro Release ◽  
Tween 80 ◽  
Drug Content ◽  
In Vitro Diffusion ◽  
Span 80 ◽  
Microemulsion Gel

Curcumin (diferuloylmethane) is a natural polyphenolic compound with potent anti-inflammatory, anticancer and antioxidant activities. However, its bioavailability is low as it is poorly absorbed in the gastrointestinal tract. Microemulsions offer the potential to improve the solubility and bioavailability of bioactive compounds; the present work investigated the topical delivery potential of microemulsion gel loaded with curcumas. Curcumin microemulsion was prepared by spontaneous emul­sification method using oil (Oleic acid), surfactant:cosurfactant (Smix) (Ethanol and Tween 80, Span 80 and n Butanol) and water. The optimized formulations of microemulsions were subjected to thermodynamic stability tests. After stability study, stable formulation was characterized for droplet size, pH determination, centrifugation, % drug content in microemulsion, zeta potential and vesicle size measurement and then microemulsion gel were prepared and characterized for spreadability, measurement of viscosity, drug content, In-vitro diffusion, in-vitro release data. Tween 80, Span 80 was selected as surfactant, ethanol, n Butanol as co surfactant and Oleic acid as oil component based on solubility study. The optimized formulation contained Curcumin (10 mg). The in vitro drug release from curcumin microemulsion gel was found to be considerably higher in comparison to that of the pure drug. The in-vitro diffusion of microemulsion gel was significantly good. Based on this study, it can be concluded the solubility and permeability of curcumin can be increased by formulating into microemulsion gel. Keyword: Curcumin, Microemulsion, In-vitro diffusion, Spreadability, Zeta potential, Stability, span 40

scholarly journals ENHANCING THE SUNSCREEN EFFICACY OF BEMOTRIZINOL MICROPIGMENT BY USING O/W NANOEMULSION TOPICAL PREPARATIONS

2019 ◽  
pp. 47-56
Author(s):  
Dina Medhat Hashim ◽  
Nermin Mohamed Sheta ◽  
Vivian Samir Elwazzan ◽  
Wedad Saed Sakran
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Tween 80 ◽  
Size Analysis ◽  
Isopropyl Myristate ◽  
Tape Stripping ◽  
Protection Factor ◽  
Potential Measurement ◽  
Optimum Formula

Objective: Bemotrizinol (BEMT) is the most efficient broad-spectrum UV-absorber having a dual mechanism of action in absorbing and reflecting photons. The main objective of this work was to develop successful oil in water (o/w) nanoemulsion for improving the solubility of BEMT and its protective characteristics. Methods: Pseudo-ternary phase diagrams were constructed using labrafac PG and isopropyl myristate as oil phase, tween 80 as surfactant (S) and cremophor EL as cosurfactant (CoS) the ratio of S/CoS was determined according to highest percent of water incorporation to the system. Full factorial study design (24) using Design-Expert® software was adopted to study the effect of four independent variables namely: oil type, oil concentration, S/CoSmix (3:1) concentrations and BEMT concentration on the particle size and the in vitro release at 2 h (Q2h) of the prepared nanoemulsion formulae. Two systems each of eight formulae were developed and evaluated through droplet size analysis, zeta potential measurement, refractive index, in vitro drug release and according to the desirability value two formulae (F6 and F14) were used for further evaluations including in vitro sun protection factor (SPF), ex-vivo deposition by tape stripping technique, permeation test and photostability study. Results: Formula (F14) was chosen as the optimum formula having an in vitro SPF of 16.08±0.39, lowest permeation of 140±0.06 μg/cm2after six h and highest photostability (t90% = 168.02) after 120 min. Conclusion: Despite the poor solubility of bemotrizinol, it could be enhanced by novel drug delivery systems with good SPF value while maintaining its photostability.

Design, Optimization and Characterization of Nanostructured Lipid Carriers of Raloxifene Hydrochloride for Transdermal Delivery

2020 ◽  
Vol 10 (1) ◽  
pp. 57-67 ◽  
Author(s):  
Durga Puro ◽  
Rajani Athawale ◽  
Anjali Pandya
Keyword(s):  
Particle Size ◽  
Transdermal Delivery ◽  
Tween 80 ◽  
Nanostructured Lipid Carriers ◽  
Polydispersity Index ◽  
Tape Stripping ◽  
Cremophor El ◽  
Scanning Calorimetry ◽  
Raloxifene Hydrochloride

Introduction: Raloxifene Hydrochloride (RXL), a BCS class II drug, is used for the treatment of invasive breast cancer and osteoporosis in post menopausal women. Even though the drug is highly efficient, it shows poor bioavailability of 2% when administered orally. The aim of the study was to develop, statistically optimize, and characterize Raloxifene Hydrochloride loaded Nanostructured Lipid Carriers (NLC) for transdermal delivery to overcome the bioavailability issue. Methods: The RXL-NLC’s were developed using glyceryl behenate (Compritol® 888 ATO), glyceryl monostearate (GMS), and capric triglyceride (Miglyol® 810) as solid and liquid lipids, and Polysorbate 80 (Tween 80) and cremophor EL were used as surfactants and co-surfactant. A response surface methodology was applied for the optimization of NLC, using Box-Behnken experimental design. Amount of the drug, tween 80 and polyethoxylated castor oil (cremophor EL), each at three levels, were selected as independent variables, while particle size and polydispersity index were identified as dependent variables. The optimized batch was characterized for Particle size (79.8 nm±3), Polydispersity index (0.229±0.05), Zeta potential (-12.3±5) and Entrapment efficiency (79.14%±5). Surface morphology of the NLC’s were studied using Transmission Electron microscopy (TEM) and the shift in the endotherm of Differential scanning calorimetry confirmed the entrapment of the drug within NLC. In vitro drug release studies were performed using dialysis bag (12000-14000 Da) method. The optimized NLC dispersion was then incorporated into gel and characterized for gel uniformity, spreadability, pH, viscosity and drug content. Results: In vivo skin penetration study was carried out by tape stripping method, which showed increase in penetration when incorporated into nanogel as compared to plain drug gel. Conclusion: Based on the above result it can be concluded that transdermal delivery of NLC’s can be a superior alternative for orally low bioavailable drugs such as RXL which undergoes rapid first pass metabolism.

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