scholarly journals Olive Oil Based Methotrexate Loaded Topical Nanoemulsion Gel for the Treatment of Imiquimod Induced Psoriasis-Like Skin Inflammation in an Animal Model

Biology ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 1121
Author(s):  
Sheikh Abdur Rashid ◽  
Sajid Bashir ◽  
Faiza Naseem ◽  
Arshad Farid ◽  
Irfan A. Rather ◽  
...  
Keyword(s):  
Drug Release ◽  
Olive Oil ◽  
Release Kinetics ◽  
Skin Permeation ◽  
Physicochemical Characterization ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Penetration Enhancers ◽  
Nanoemulsion Gel

Psoriasis, a chronic inflammatory illness, is on the rise and is linked to several other life-threatening diseases. The primary goal of this study was to create a nanoemulsion gel loaded with methotrexate and olive oil (MTX NEG). The formulation was evaluated for physicochemical characterization, entrapment efficiency, drug release kinetics, skin permeation studies and stability tests. In addition, the efficacy of MTX NEG against psoriasis was tested using imiquimod-induced psoriasis in a rat model. The final optimized MTX NEG was developed with a particle size of 202.6 ± 11.59 nm and a PDI of 0.233 ± 0.01, with a 76.57% ± 2.48% average entrapment efficiency. After 20 h, the release kinetics predicted a 72.47% drug release at pH 5.5. FTIR findings demonstrated that the optimized MTX NEG formulation effectively fluidized both the epidermis and dermis of the skin, potentially increasing drug permeability and retention. The application of Tween 80 and PEG 400, on the other hand, significantly enhanced these effects, as these are well known penetration enhancers. After 24 h, an average of 70.78 ± 5.8 μg/cm2 of methotrexate was permeated from the nanoemulsion gel with a flux value of 2.078 ± 0.42 μg/cm2/h, according to permeation measurements. Finally, in vivo experiments on rabbit skin revealed that the increased skin penetration of methotrexate-loaded nanoemulsion gel was not due to structural alterations in intercellular lipid layers in the stratum corneum. In vivo antipsoriatic studies on rats revealed that MTX NEG produced a PASI decrease that was extremely similar and even better than the 91% reduction seen in the MTX tablet group. According to the pharmacokinetic profile, Cmax was 8.5 μg/mL, Tmax was 12 h, and t1/2 was 15.5 ± 2.37 h. These findings reinforce that MTX-NEG based on olive oil could be a possible treatment for psoriasis and could decrease the remission of psoriasis-like symptoms.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

scholarly journals Fabrication and in vitro characterization of polymeric nanoparticles for Parkinson's therapy: a novel approach

2014 ◽  
Vol 50 (4) ◽  
pp. 869-876 ◽  
Author(s):  
Neha Gulati ◽  
Upendra Nagaich ◽  
Shubhini Saraf
Keyword(s):  
Drug Release ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Mode Of Delivery ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Fickian Diffusion ◽  
Novel Approach

The objective of the research was to formulate and evaluate selegiline hydrochloride loaded chitosan nanoparticles for the Parkinson's therapy in order to improve its therapeutic effect and reducing dosing frequency. Taguchi method of design of experiments (L9 orthogonal array) was used to get optimized formulation. The selegiline hydrochloride loaded chitosan nanoparticles (SHPs) were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP) and tween 80 as surfactant. The SHPs had a mean size of (303.39 ± 2.01) nm, a zeta potential of +32.50mV, and entrapment efficiency of SHPs was 86.200 ± 1.38%. The in vitro drug release of SHPs was evaluated in phosphate buffer saline (pH 5.5) using goat nasal mucosa and found to be 82.529% ± 1.308 up to 28 h. Release kinetics studies showed that the release of drug from nanoparticles was anomalous (non-fickian) diffusion indicating the drug release is controlled by more than one process i.e. superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. SHPs showed good stability results as found during stability studies at different temperatures as mentioned in ICH guidelines. The results revealed that selegiline hydrochloride loaded chitosan nanoparticles are most suitable mode of delivery of drug for promising therapeutic action.

scholarly journals FLUCONAZOLE NANOGEL: FABRICATION AND IN VITRO EVALUATION FOR TOPICAL APPLICATION

2021 ◽  
pp. 272-277
Author(s):  
DIVYA ◽  
INDERBIR SINGH ◽  
UPENDRA NAGAICH
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Seborrheic Dermatitis ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Flow Index ◽  
In Vitro Evaluation

Objective: The aim of this study is to develop and in vitro evaluation of prepared fluconazole nanogel for seborrheic dermatitis Methods: Fluconazole nanogel was formulated to act against seborrheic dermatitis. The fluconazole nanoparticles were prepared by a simplified evaporation method and evaluated for particle size, entrapment efficiency, and percent in vitro drug release. The nanogel was also characterized based on parameters like particle size, percent entrapment efficiency, shape surface morphology, rheological properties, in vitro release R² = 0.9046, and release kinetics. Results: The nanoparticle with a combination of Eudragit RS and Tween 80 showed the best result with particle size in the range of 119.0 nm to 149.5 nm, with a cumulative percent drug release of 95 % up to 18 h. The formulated nanogel with optimum concentration of HPMC authenticate with particle size 149.50±0.5 with maximum drug release (92.13±0.32) %. Conclusion: Different percentages of polymers (ethyl-cellulose, eudragit, and tween 80) are used as variable components in the formulation of nanogel. The optimized batch showed good physical properties (flow index, spreadability, and viscosity) along with rapid drug release. Therefore, it can be concluded that nanogel containing fluconazole has potential application in topical delivery.

scholarly journals FORMULATION AND EVALUATION OF PRONIOSOMAL GEL-BASED TRANSDERMAL DELIVERY OF ATORVASTATIN CALCIUM BY BOX–BEHNKEN DESIGN

2019 ◽  
pp. 335-343 ◽  
Author(s):  
SOUJANYA C ◽  
RAVI PRAKASH P
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Skin Permeation ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Transmission Electron Microscopy Analysis ◽  
Box Behnken Design ◽  
Atorvastatin Calcium ◽  
Span 60

Objective: The aim of this study was to investigate the combined influence of three independent variables in the preparation of atorvastatin proniosomes by coacervation-phase separation method. Methods: On the basis of the preliminary trials, a 3-factor, 3-level Box–Behnken design was employed to study the effect of cholesterol, soya lecithin, and Span 60 independent variable on dependent variables (particle size and % entrapment efficiency). Transmission electron microscopy analysis of optimized formulation has demonstrated the presence of individual proniosomes in spherical shape. Results: Atorvastatin optimized proniosomal formulation F2 shown better particle size and % entrapment efficiency, and also, the drug release was 99.72% within 24 h in slow and controlled manner when compared with control. Kinetic analysis of drug release profiles showed that the drug release was followed by zero-order manner with Korsmeyer–Peppas model, which implies super case II release kinetics. The particle size and zeta potential of the optimized atorvastatin proniosomal gel were found to be 65.72 and −10.5, respectively. The optimized batch of proniosomes was used for the preparation of atorvastatin-based proniosomal hydrogel by incorporating hydrated proniosomes to carbopol matrix to enhance the stability and viscosity of the system. Conclusion: The enhanced skin permeation, for a prolonged period of time, may lead to improved efficacy and better patient compliance. This study suggests that proniosomal gel-containing atorvastatin could perform therapeutically better effects than the conventional formulations.

Development and Optimization of Lovastatin-loaded Trans-dermal Proniosomal Gel using Box-Behnken Design

2018 ◽  
Vol 11 (4) ◽  
pp. 4196-4207
Author(s):  
Soujanya C ◽  
Ravi Prakash P
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Skin Permeation ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Transdermal Drug Delivery System ◽  
Tem Analysis ◽  
Box Behnken Design ◽  
The Stability

In this study, a proniosome-based transdermal drug delivery system of lovastatin was developed by coacervation phase separation method. On the basis of the pilot trials, a 3-factor, 3-level Box–Behnken design was employed to characterize the effect of Cholesterol, soya lecithin and Tween 80 on dependent variables (particle size, entrapment efficiency, and drug release). TEM analysis of optimized formulation has demonstrated the presence of individual Proniosomes in spherical shape. Lovastatin optimized proniosomal formulation F1 shown better particle size and percentage entrapment efficiency and drug release of 99.49% within 24h in slow and controlled manner when compared with control. Kinetic analysis of drug release profiles showed that the systems predominantly released Lovastatin in a zero-order manner with a strong correlation coefficient (R2= 0.9990). The particle size and Zeta potential of the optimized lovastatin proniosomal gel was found to be 138.82 nm and -11.4 mV respectively. Optimized batch of Proniosomes was used for the preparation of Lovastatin - based proniosomal hydrogel by incorporating hydrated Proniosomes to Carbopol matrix to enhance the stability and viscosity of the system. The enhanced skin permeation for prolonged time may lead to improved efficacy and better patient compliance.      

scholarly journals Development and in vivo Evaluation of Lovastatin Loaded Transdermal Proniosomal Gel by Design of Experiment

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
C. Soujanya ◽  
P.Ravi Prakash
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
In Vivo Studies ◽  
In Vivo Evaluation ◽  
Time Curve ◽  
Alternative Approach ◽  
The Stability

The objectives of the present study were to define effects on the hypercholesterolemia activity and pharmacokinetics of a novel transdermal proniosomal gel incorporating Lovastatin prepared by coacervation phase separation method. On the basis of the preliminary trials, a 3-factor, 3-level Box–Behnken design was employed to study the effect of Cholesterol, soya lecithin and Tween 80 on dependent variables (particle size, % entrapment efficiency, and % of drug release). Lovastatin optimized proniosomal formulation F1 shown better particle size and % entrapment efficiency and drug release of 99.49% within 24 h in slow and controlled manner when compared with control. The particle size and zeta potential of the optimized lovastatin proniosomal gel was found to be 138.82 nm and -11.4 mV respectively. Optimized batch of Proniosomes was used for the preparation of Lovastatin-based proniosomal hydrogel by incorporating hydrated Proniosomes to Carbopol matrix to enhance the stability and viscosity of the system. From in vivo studies the maximal concentrations (Cmax) of drug was significantly reduced while the areas under the plasma concentration–time curve (AUC) and t1/2 were evidently increased and extended. The results suggest that proniosomes can act as promising carrier which offers an alternative approach for transdermal delivery of Lovastatin. The study demonstrated the effectiveness of proniosomal preparation of Lovastatin for effective management of hypercholesterolemia to reduce risk of cardiovascular disease.

Allopurinol Loaded Transferosomes for the Alleviation of Symptomatic After-effects of Gout: An Account of Pharmaceutical Implications

2020 ◽  
Vol 15 (4) ◽  
pp. 404-419
Author(s):  
Ruchi Tiwari ◽  
Gaurav Tiwari ◽  
Rachna Singh
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Skin Permeation ◽  
Skin Irritation ◽  
In Vivo Studies ◽  
Transdermal Drug Delivery System

Background: The present study assessed the transdermal potential of transferosomes loaded with allopurinol for the treatment of gout. Methods: Transferosomes of allopurinol were composed of different ratios of tween-80, soya lecithin and solvent using a thin-film hydration method. Transferosomes were characterized for Scanning Electron Microscopy (SEM), zeta potential, % entrapment efficiency (%EE), Fourier Transform Infrared Spectroscopy (FTIR), in-vitro drug release and kinetics as well as stability. Then, optimized formulation was incorporated in gel and evaluated for viscosity, pH, extrudability, homogeneity, skin irritation study, spreadability, ex vivo skin permeation study, flux, and stability. Results: SEM studies suggested that vesicles were spherical and zeta potential were in the range of -11.4 mV to -29.6 mV and %EE was 52.4- 83.87%. FTIR study revealed that there was no interaction between allopurinol and excipients during the preparation of transferosomes. The cumulative percentage of drug release from various transferosomes was ranged from 51.87 to 81.87%. A transferosomal gel of F8 formulation was prepared using dispersion method reported pseudoplastic rheological behavior, optimum pH, spreadability and maximum drug permeation i.e. 79.84% with flux 13.06 g/cm2/hr, followed zero-order release kinetics. Irritation and in-vivo studies of optimized transferosomal gel G8 on rabbits revealed better results than the standard allopurinol. Conclusion: This research suggested that allopurinol loaded transferosomal gel can be potentially used as a transdermal drug delivery system for the treatment of gout.

Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Anamika Saxena Saxena ◽  
Santosh Kitawat ◽  
Kalpesh Gaur ◽  
Virendra Singh
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Entrapment Efficiency ◽  
Repeated Administration ◽  
Alginate Beads ◽  
Delivery Systems ◽  
Sem Analysis ◽  
Formulation Development

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

Design and Synthesis of a Novel Gabapentin-Phosphotidylcholine Conjugate for Targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier

2020 ◽  
Vol 16 ◽  
Author(s):  
Anjali P.B ◽  
Jawahar N. ◽  
Jubie S. ◽  
Neetu Yadav ◽  
Selvaraj A. ◽  
...  
Keyword(s):  
Drug Release ◽  
Phospholipase A2 ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Structural Analog ◽  
Fickian Diffusion ◽  
Release Kinetic ◽  
Nanostructured Lipid Carrier ◽  
Discovery Studio

Background: : Epilepsy is a genuine neurological turmoil that effects around 50 million individuals around the world. Practically 30% of epileptic patients experience the ill effects of pharmaco-obstruction, which is related with social seclusion, subordinate conduct, low marriage rates, joblessness, mental issues and diminished personal satisfaction. At present accessible antiepileptic drugs have a restricted viability, and their negative properties limit their utilization and cause challenges in patient administration. Gabapentin 1-(aminomethyl)cyclohexane acetic acid, Gbp , (trade name Neurontin), a structural analog of γ-aminobutyric acid (GABA), BCS class 3 drug with having permeability issues. Objective: This work was an attempt to formulate and characterize a new approach to treat epilepsy by targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier. Methods: Docking studied carried out using Accelrys Discovery studio 4.1 Client and gabapentin and phosphotidylcholine were conjugated through chemical conjugation. Nanostructured lipid carrier (NLC) was prepared using hot homogenization technique. Results: The libdock score of Gabapentin- Phosphotidylcholine conjugate (192.535) were found to be more than Gabapentin (77.1084) and Phosphotidylcholine (150.212). For the optimized formulation the particle size (50.08), zeta potential (-1.48), PDI (0.472) and entrapment efficiency (77.8) was observed. The NLC was studies for in-vitro drug release studies and release kinetics. Finally found that the drug release from the NLC followed Higuchi release kinetic and the mode of drug release from the NLC was found to be Non- Fickian diffusion. Conclusion: The formulated Nanostructured lipid carrier of Gabapentin-Phosphotidylcholine conjugate may be able to use to prevent seizure.

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