scholarly journals PHYSICAL PROPERTIES AND RATE OF DIFFUSION TRANSETHOSOME CURCUMIN USING A COMBINATION OF TWEEN 60 AND SPAN 60 AS SURFACTANT

2021 ◽  
pp. 66-70
Author(s):  
ANISA AMALIA ◽  
YUDI SRIFIANA ◽  
AMALIA ANWAR
Keyword(s):  
Particle Size ◽  
Physical Properties ◽  
Diffusion Rate ◽  
Entrapment Efficiency ◽  
Zero Order Kinetics ◽  
Significant Difference ◽  
Tween 60 ◽  
Span 60

Objective: Curcumin penetration can be increased by formulating it into the transethosome system. Surfactant is one of the transethosome components that affect the physical properties and penetration of vesicles. In this study, a combination of two surfactants was used to see the effect of surfactants on physical properties and curcumin penetration. Methods: This study used a combination of tween 60 and span 60 with a concentration ratio of 0:5 (F1), 1:1 (F2), 2:1 (F3), and 1:2 (F4). An evaluation included testing the distribution of particle size, zeta potential, and entrapment efficiency in the system. Evaluation continued with the determination of the diffusion rate in vitro.  Results: The transethosome system formed has a particle size of 167.9±4.7 nm-396±3.7 nm with a potential zeta value (-) 49.54±1.77 mV-(-) 59.05±0.95 mV, polydispersion index 0.0%-57.1% and entrapment efficiency of 83.76%-93.75%. The diffusion rate of F1 and F3 followed the Higuchi kinetics model, while F2 and F4 followed zero-order kinetics and the Korsmeyer-Peppas kinetics. Conclusion: The combination of tween 60 and span 60 could form a nano-sized transethosome of curcumin. Diffusion rate testing results show that using a surfactant combination can increase the diffusion rate of curcumin, where there is a significant difference between each formula (p<0.05).

scholarly journals ENHANCEMENT OF DISSOLUTION CHARACTERISTICS OF CLOPIDOGREL BISULPHATE BY PRONIOSOMES

2019 ◽  
pp. 77-85 ◽  
Author(s):  
EMAN A. MAZYED ◽  
SHERIN ZAKARIA
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
International Normalized Ratio ◽  
Angle Of Repose ◽  
Morphological Examination ◽  
Span 60

Objective: The present investigation aims to formulate and evaluate proniosomes of clopidogrel bisulphate for improving its dissolution characteristics. Methods: The slurry method was used for the preparation of proniosomes of clopidogrel using cholesterol, sorbitan monostearate (Span 60) and maltodextrin as a carrier. Clopidogrel proniosomes were evaluated for their entrapment efficiency and in vitro drug release. The best formula (F1) that achieved maximum drug release was further evaluated by measurement of the angle of repose, morphological examination, determination of vesicle size, determination of zeta potential, Fourier transform infrared spectroscopy and differential thermal analysis. The in vivo behavior of the selected proniosomal formula (F1) was studied by measuring the antiplatelet activity in adult male mice. Results: The entrapment efficiency of clopidogrel proniosomes was in the range of 83.04±1.99 to 90.14±0.30. % drug released from proniosomal formulations was in the range of 79.73±0.35 to 97.70±1.10 % within 4 h. Clopidogrel proniosomes significantly enhanced the in vitro release of clopidogrel compared with the plain drug that achieved 61.77±2.22 % drug release. F1 significantly (p ≤ 0.001) increased the bleeding time and bleeding volume and significantly (p ≤ 0.05) prolonged prothrombin time and decreased prothrombin activity and increased the international normalized ratio (INR) compared to plain clopidogrel. Conclusion: The present investigation introduced proniosomes as a promising carrier for clopidogrel that could enhance its dissolution and pharmacological effect.

scholarly journals SCREENING AND OPTIMIZATION OF VALACYCLOVIR NIOSOMES BY DESIGN OF EXPERIMENTS

2018 ◽  
Vol 10 (1) ◽  
pp. 79 ◽  
Author(s):  
Surya Teja Sp ◽  
Mothilal M. ◽  
Damodharan N ◽  
Jaison D
Keyword(s):  
Drug Release ◽  
Design Of Experiments ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Substantial Effect ◽  
Fickian Diffusion ◽  
Vesicle Size ◽  
Zero Order Kinetics ◽  
Significant Difference ◽  
Span 60

Objective: The objective of the study was to perform a screening, optimization of valacyclovir niosomal formulation to achieve a sustained release of drug using the design of experiments by 32 full factorial design.Methods: Valacyclovir loaded niosomes were prepared using thin film hydration method by varying the ratio of Span 60 and Cholesterol. The prepared niosomes were evaluated for vesicle size, entrapment efficiency, cumulative drug release, fourier transformed infrared spectroscopy (FTIR), zeta potential and surface morphology by field emission scanning electron microscopy (FESEM).Results: The valacyclovir was successfully encapsulated and its entrapment efficiency ranged from 36.70 % to 50.62 %. The average vesicle size of the niosomes was found to be 431 to 623 nm. At 8th hour the drug release varied from 77.50% to 96.31 %. The optimized niosomes were multilamellar with a surface charge potential of about-43.2 mV. The studies revealed that the interaction of cholesterol and surfactant had a substantial effect on vesicle size, entrapment efficiency and drug release from the niosomes. The release kinetics of the optimized niosomes followed zero order kinetics with fickian diffusion controlled mechanism. The stability studies were performed for the optimized formulation and found that the formulation is stable at 4°C ± 2°C.Conclusion: Model equations were developed for the responses. No significant difference was observed between the predicted and observed value, showing that the developed model is reliable.

scholarly journals Enhancement Solubilization of Dutasteride using Microsponge Formulation

2020 ◽  
Vol 10 (01) ◽  
pp. 60-67
Author(s):  
Hassanien S. Taghi ◽  
Mustafa R. Abdulbaqi ◽  
Esraa G. Jabar
Keyword(s):  
Particle Size ◽  
Physical Properties ◽  
Water Solubility ◽  
Oral Absorption ◽  
Entrapment Efficiency ◽  
Production Yield ◽  
Internal Surface Area ◽  
Prostate Hyperplasia ◽  
Saturated Solubility

Dutasteride (DU) (5α-reductase inhibitor) that is used for the treatment of benign prostate hyperplasia (BPH), DU has low water solubility and poor oral absorption that classified as Biopharmaceutics Classification System (BCS) class II. This study aims to improve the physical properties of Dutasteride (DU) like solubility by the preparation of microsponge (MS). Microsponges are spherical in shape, sponge-like structure, polymeric delivery systems composed of porous microspheres with a large internal surface area. Nine formulations of DU MS had been prepared by the technique of quasi-emulsion solvent diffusion (QESD) and utilizing Eudragit S100 as major polymer and glycerol as a plasticizer that dissolved in dichloromethane where polyvinyl alcohol PVA serves as a stabilizer in the external phase. The formulas were employed to optimize preparation variable factors include; different drug to polymer ratio, the addition of different concentrations of PVA, and stirring rate. Optimization was done using the response of production yield (PY), entrapment efficiency EE), particle size, and in vitro drug release; The results display that the best ratio of (drug: polymer) was 5:1, and the best rate of stirring was 1,000 rpm respecting the optimum characteristics of microsponge. The best-selected formula prepared (F2) was underwent to evaluation regarding saturated solubility, FTIR, DSC, and SEM and showed 1.28 folds enhancement in saturated solubility compared to plain DU, and was well fabricated with high entrapment efficiency (83.7% ± 1.37), production yield (85.61% ± 0.6), and particle size of 77μm. Moreover, the percent release of DU was 75.74 ± 1.5 after 4 hours, with good compatibility as confirmed by XRD, SEM, DSC, and fourier-transform infrared spectroscopy (FTIR) analysis. It can be concluded that the selected formula prepared (F2) of DU microsponge is reassuring and promising drug delivery with improved pharmaceutical physical properties.

FORMULATION AND EVALUATION OF ACECLOFENAC NIOSOMES BY USING MIXTURE OF SURFACTANTS

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (12) ◽  
pp. 21-26
Author(s):  
C.H. Sravanthi ◽  
◽  
S. Punitha
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Therapeutic Index ◽  
Reverse Phase ◽  
Evaporation Method ◽  
Zero Order Kinetics ◽  
Reduced Toxicity ◽  
Span 60

The present study was aimed at the overall improvement in the efficacy, reduced toxicity andenhancement of therapeutic index of aceclofenac. Niosomal delivery system of aceclofenac has beendeveloped by various techniques using mixture of Span 60/40 (surfactant) along with cholesterol in1:1 ratio. The formulations were then characterized with respect to vesicle diameter, drug content,entrapment efficiency, in-vitro drug release and release kinetics. The formulated aceclofenac niosomeswere discrete and round in shape. The lowest entrapment efficiency was found to be 75% (F2) andwas highest in reverse phase evaporation method 95% (F5). Percentage cumulative drug release waswell retarded for up to 24 h in F5 (59%) compared to all other formulations and its release pattern wasanalysed by using various mathematical models and found to follow under zero order kinetics. From thet50% values of F5, it is concluded that the reverse phase evaporation method seems to extend the drugrelease for prolonged period.

Preparation and In Vivo Characterization of Niosomal Carriers of the Antidiabetic Drug Repaglinide

2015 ◽  
Vol 8 (1) ◽  
pp. 2756-2767 ◽  
Author(s):  
Shrishti Namdev ◽  
Kishore Gujar ◽  
Satish Mandlik ◽  
Preeti Jamkar
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Therapeutic Effects ◽  
Drug Release Profile ◽  
Independent Variables ◽  
Span 60

The objective of this study is to prepare and characterise repaglinide niosomes using the Factorial Design strategy.Repaglinide is a potent second-generation oral hypoglycemic agent and has short half-life of 1 hour and oral bioavailability of 50%. Preparing Niosomal drugdelivery of repaglinide may increase its bioavailability which would lead to better therapeutic effects, reduce the frequency of dosing from twice a day to once a day and decrease side effects. The preliminary study was carried out for selection of surfactant and method of preparation based on least particle size and highest entrapment efficiency. For niosome preparation, organic solvent injection method was selected and span 60, cholesterol were selected as variable. A32 factorial design was used to optimize the effect of amounts of span 60(X1) and cholesterol (X2) which were the independent variables. Particle size (Y1) and entrapment efficiency (Y2) were the dependent variables. Relation between the dependent and independent variables were drawn out from the mathematical equations and response surface plots.Statistical analysis was performed using ANOVA which was found to be significant and quadratic equation was obtained by MLRA. The particle size was found to be in range of 144-497 nm and entrapment efficiency between 54-88%. Scanning electron microscopy indicated the spherical shape of the niosomes and formation of vesicle. Zeta potential analysis showed negatively charged surface with value of-36.7 mV. In vitro drug release profile showed that drug released fast initially followed by a slow release. In vivo pharmacokinetic study revealed that the niosomal preparation showed significant decrease in blood glucose level when compared to free repaglinide. The developed niosomal system also has potential of maintaining therapeutic level of RPG for longer period of time.Thus,the niosomes could be promising carriers for delivery ofrepaglinide with increased 

scholarly journals FORMULATION AND EVALUATION OF ITRACONAZOLE NIOSOMAL GEL

2018 ◽  
Vol 6 (5) ◽  
pp. 76-80
Author(s):  
Ashish Kumar ◽  
J.S Dua
Keyword(s):  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Systemic Fungal Infection ◽  
Drug Content ◽  
Carbopol 940 ◽  
Niosomal Gel ◽  
Span 60 ◽  
Anti Fungal

The preparation of niosomes. The main objective of the study was to enhance the antifungal activity of the formulation.  Itraconazole is a broad spectrum Imidazole derivative useful in the treatment of superfacial and systemic fungal infection. Various surfactants used were span 40 and span 60. Niosomes were prepared by using Rotary Vaccum evaporation method. Niosomes were prepared using different ratio of drug: surfactant: cholesterol (1:1:1, 1:2:1, 1:3:1).Evaluation of the Niosomal gel was done by determination of drug content 52.81-56.12, Entrapment Efficiency 42.20-45.20,Niosomal gel was prepared using Carbopol 940 (1.5%), Glycerol (10%), Triethanolamine (q.s.) and distilled water up to 15ml. Viscosity was determined by Brookfield programmable ultra-viscometer and the ranges 8173 centipoise. The drug content of the Itraconazole niosomal gel was determined at 262 nm against blank by using UV/visible spectrophotometer and found to be 56.12%. The percentage of drug entrapment in niosomal gel was calculated to be 45.20% .The in-vitro drug release study was carried out using phosphate buffer saline pH 7.4 and was found to be 41.18 ± 1.53% for 12 hours. It can be concluded that the gel formulation containing niosomes loaded with Itraconazole showed prolonged action than formulation containing Itraconazole in non-niosomal form and it can be developed successfully to improve the anti-fungal activity.

scholarly journals Evaluation of sonication on stability-indicating properties of optimized pilocarpine hydrochloride-loaded niosomes in ocular drug delivery

2021 ◽  
Author(s):  
K. Owodeha-Ashaka ◽  
M. Ilomuanya ◽  
A. Iyire
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Entrapment Efficiency ◽  
Process Variable ◽  
Hydrophilic Drugs ◽  
Stability Indicating ◽  
Long Term Stability ◽  
Tween 60 ◽  
Span 60 ◽  
Sonication Parameters

AbstractNiosomes are increasingly explored for enhancing drug penetration and retention in ocular tissues for both posterior and anterior eye delivery. They have been employed in encapsulating both hydrophilic and hydrophobic drugs, but their use is still plagued with challenges of stability and poor entrapment efficiency particularly with hydrophilic drugs. As a result, focus is on understanding the parameters that affect their stability and their optimization for improved results. Pilocarpine hydrochloride (HCl), a hydrophilic drug is used in the management of intraocular pressure in glaucoma. We aimed at optimizing pilocarpine HCl niosomes and evaluating the effect of sonication on its stability-indicating properties such as particle size, polydispersity index (PDI), zeta potential and entrapment efficiency. Pilocarpine niosomes were prepared by ether injection method. Composition concentrations were varied and the effects of these variations on niosomal properties were evaluated. The effects of sonication on niosomes were determined by sonicating optimized drug-loaded formulations for 30 min and 60 min. Tween 60 was confirmed to be more suitable over Span 60 for encapsulating hydrophilic drugs, resulting in the highest entrapment efficiency (EE) and better polydispersity and particle size indices. Optimum sonication duration as a process variable was determined to be 30 min which increased EE from 24.5% to 42% and zeta potential from (−)14.39 ± 8.55 mV to (−)18.92 ± 7.53 mV. In addition to selecting the appropriate surfactants and varying product composition concentrations, optimizing sonication parameters can be used to fine-tune niosomal properties to those most desirable for extended eye retainment and maintenance of long term stability.

scholarly journals Etodolac Containing Topical Niosomal Gel: Formulation Development and Evaluation

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Gyati Shilakari Asthana ◽  
Abhay Asthana ◽  
Davinder Singh ◽  
Parveen Kumar Sharma
Keyword(s):  
Particle Size ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Formulation Development ◽  
Topical Gel ◽  
Niosomal Gel ◽  
Span 60

The present study aimed to investigate the delivery potential of Etodolac (ETD) containing topical niosomal gel. Niosomal formulations were prepared by thin film hydration method at various ratios of cholesterol and Span 60 and were evaluated with respect to particle size, shape, entrapment efficiency, and in vitro characteristics. Dicetyl phosphate (DCP) was also added in the niosomal formulation. Mean particle size of niosomal formulation was found to be in the range of 2 μm to 4 μm. Niosomal formulation N2 (1 : 1) ratio of cholesterol and surfactant displayed good entrapment efficiency (96.72%). TEM analyses showed that niosomal formulation was spherical in shape. Niosomal formulation (N2) displayed high percentage of drug release after 24 h (94.91) at (1 : 1) ratio of cholesterol : surfactant. Further selected niosomal formulation was used to formulate topical gel and was characterized with respect to its various parameters such as pH, viscosity, spreadability, ex vivo study, and in vivo potential permeation. Ex vivo study showed that niosomal gel possessed better skin permeation study than the plain topical gel. Further in vivo study revealed good inhibition of inflammation in case of topical niosomal gel than plain gel and niosomal formulation. The present study suggested that topical niosomal gel formulations provide sustained and prolonged delivery of drug.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Preparation, Characterization and In-vitro release of Piroxicam-loaded Solid Lipid Nanoparticles

2010 ◽  
Vol 3 (3) ◽  
pp. 1136-1146
Author(s):  
V K Verma ◽  
Ram A
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Diffusion Method ◽  
Solid Lipid ◽  
Vitro Release

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 

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