scholarly journals EFFECT OF PEGYLATED EDGE ACTIVATOR ON SPAN 60 BASED- NANOVESICLES: COMPARISON BETWEEN MYRJ 52 AND MYRJ 59

2019 ◽  
Author(s):  
Elsaied H. Elsaied ◽  
Hamdy M Dawaba ◽  
El Sherbini A Ibrahim ◽  
Mohsen I Afouna
Keyword(s):  
Polyethylene Glycol ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Potential Drug ◽  
Span 60 ◽  
Surface Modified ◽  
Vitro Release ◽  
Edge Activator

In recent years, Span 60 based nanovesicles have been the object of growing scientific attention as an alternative potential drug delivery system to conventional liposomes. Surface modification of nanovesicles can adjust the drug release rate and the affinity for the target site. The aim of present work was firstly to study the effects of different PEGylated edge activator (Myrj 52 and Myrj 59) on Span 60 based nanovesicles. Nanovesicles were prepared using Span 60 alone or in combination with Myrj 52 (polyethylene glycol 2000 monostearate) or Myrj 59 (polyethylene glycol 4400 monostearate) by employing the ethanol injection method. Myrj 52and Myrj 59 are hydrophilic nonionic surfactants were used to modify the surface of the developed vesicles. Dynamic light scattering was used to determine the size, zeta potential and polydispersity index of the nanovesicles formulation. The vesicles were also characterized for entrapment efficiency and in vitro release. In current work, the modified nanovesicles size (ranging from 54.32 to 141.7 nm), zeta potential (ranging from -5.67 to -27.1 mV) and polydispersity index (ranging from0.248 to 0.531) indicated that the surface modified nanovesicles vesicles are a homogenous and mono-disperse nanovesicles dispersions. The non-modified nanovesicles are showed higher particles size (>2 times) compared to modified nanovesicles. The modified nanovesicles were showed entrapment efficiency ranging from 36.42 to 78.13 %. All the modified nanovesicles showed accepted in vitro release of TN from nanovesicles (>70% released after 8 h), followed Higuchi models as drug release mechanism. In conclusion, these surface modified nanovesicles could be used as a potential drug carrier for a variety of drugs.

scholarly journals FORMULATION OF POLYMERIC NANOSUSPENSION CONTAINING PRAMIPEXOLE DIHYDROCHLORIDE AND HESPERIDIN FOR IMPROVED TREATMENT OF PARKINSON’S DISEASES

2018 ◽  
Vol 11 ◽  
Author(s):  
Somasundaram I
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Drug Content ◽  
Pramipexole Dihydrochloride ◽  
Vitro Release

Aims and Objectives: The present study is to formulate the nanosuspension containing a hydrophilic drug pramipexole dihydrochloride and hesperidin and to increase the drug entrapment efficiency.Methods: Hesperidin and pramipexole dihydrochloride loaded in chitosan nanosuspension is prepared by ionic gelation method using chitosan and tripolyphosphate. There was no incompatibility observed between the drug and polymer through Fourier transform infrared and differential scanning calorimetric. Various other parameters such as particle size, zeta potential, scanning electron microscope, drug content, drug entrapment efficiency, and in vitro release have been utilized for the characterization of nanoparticles.Results and Discussion: The average size of particle is 188 nm; zeta potential is 46.7 mV; drug content of 0.364±0.25 mg/ml; entrapment efficiency of 72.8% is obtained with HPN3 formulation. The PHC1 shows the highest drug release followed by PHC2 due to low concentration of polymer and PHC4 and PHC5 show less drug release due to high concentration of polymer. The in vitro release of PHC3 is 85.2%, initial the burst release is shown which is approximately 60% in 8 h; then, slow release later on drastic reduction in release rate is shown in 24 h. The in vivo study histopathological report confers the effective protective against rotenone induces Parkinson’s.Conclusion: PHC3 was chosen as the best formulation due to its reduced particle size and controlled release at optimum polymer concentration which may be used to treat Parkinson’s disease effectively..

scholarly journals BENAZEPRIL HYDROCHLORIDE LOADED NIOSOMAL FORMULATION FOR ORAL DELIVERY: FORMULATION AND CHARACTERIZATION

2018 ◽  
Vol 10 (5) ◽  
pp. 66
Author(s):  
Ameerah A. Radhi
Keyword(s):  
Zeta Potential ◽  
Oral Delivery ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Potential Range ◽  
Transmission Electron ◽  
Study Results ◽  
Span 60 ◽  
A Charge

Objective: The objective of the present study was to formulate niosomal formulations of benazepril hydrochloride in an attempt to overcome the hurdles associated with itʼs poor oral absorption.Methods: Nine formulations were prepared with various ratios of sorbitan monostearate (span 60), sorbitan monopalmitate (span 40) and polyoxyethylene 2 stearyl ether (brij 72) as non-ionic surfactants, cholesterol as a stabilizing agent and soya lecithin as a charge imparting agent. Then, they were characterized for vesicle size, polydispersity (PDI), entrapment efficiency (EE %), release profile, zeta (ζ) potential and transmission electron microscopy (TEM).Results: Niosomal formulations exhibited an efficient entrapment range between (80.4-97.8) percent, vesicles size analyses revealed the formation of homogenously dispersed vesicles having a size range of (3.9±1.7-8.72±4.4) micrometers. The in vitro release studies revealed that all formulations displayed sustained release in comparison with the pure drug. Formulations prepared with span 60 and span 40 possessed adequate stability according to zeta potential analysis, whereas brij 72 failed the test and possessed inadequate zeta potential range. TEM images of the optimized formulations (F7 and F8) have confirmed the formation of vesicles with spherical shapes.Conclusion: Based on the study results, niosomal formulations seem to be attractive alternatives to conventional delivery for benazepril hydrochloride.

scholarly journals DESIGN, OPTIMIZATION AND IN VITRO EVALUATION OF ANTIFUNGAL ACTIVITY OF NANOSTRUCTURED LIPID CARRIERS OF TOLNAFTATE

2019 ◽  
pp. 109-115
Author(s):  
AHMED GARDOUH ◽  
Samar H. Faheim ◽  
Samar M. Solyman
Keyword(s):  
Zeta Potential ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Homogenization Method ◽  
Nanostructured Lipid Carriers ◽  
Scanning Calorimetry ◽  
Release Study ◽  
Vitro Release

Objective: The main purpose of this work was to prepare tolnaftate (TOL) loaded nanostructured lipid carriers (NLCs), Evaluate its characteristics and in vitro release study. Methods: Tolnaftate loaded Nanostructured lipid carriers were prepared by the high shear homogenization method using different liquid lipids types (DERMAROL DCO® and DERMAROL CCT®) and concentrations, different concentration ratios of tween80® to span20® and different homogenization speeds. All the formulated nanoparticles were subjected to particle size (PS), zeta potential (ZP), polydispersity index (PI), drug entrapment efficiency (EE), Differential Scanning Calorimetry (DSC), Transmission Electron microscopy (TEM), release kinetics and in vitro release study was determined. Results: The results revealed that NLC dispersions had spherical shapes with an average size between 154.966±1.85 nm and 1078.4±103.02 nm. High entrapment efficiency was obtained with negatively charged zeta potential with PDI value ranging from 0.291±0.02 to 0.985±0.02. The release profiles of all formulations were characterized by a sustained release behavior over 24 h and the release rates increased as the amount of surfactant decreased. The release rate of TOL is expressed following the theoretical model by Higuchi. Conclusion: From this study, It can be concluded that NLCs are a good carrier for tolnaftate delivery

scholarly journals FORMULATION AND OPTIMIZATION OF ITRACONAZOLE PRONIOSOMES USING BOX BEHNKEN DESIGN

2018 ◽  
Vol 10 (2) ◽  
pp. 41
Author(s):  
Ahmed M. Samy ◽  
Afaf A. Ramadan ◽  
Amal S.m. Abu El-enin ◽  
Yasmin I. M. Mortagi
Keyword(s):  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Slow Phase ◽  
Optimum Level ◽  
Box Behnken Design ◽  
Vesicle Size ◽  
Transmission Electron ◽  
Span 60

Objective: The aim of the present study was to obtain an optimized formula of itraconazole (ITC) proniosomes using Box Behnken design.Methods: Itraconazole proniosomes were prepared using span 60 and/or brij 35 as surfactants, cholesterol and lecithin as a penetration enhancer by slurry method. Various trials have been carried out for investigation of proniosomes. Parameters such as entrapment efficiency (EE%), in vitro drug release, zeta potential, vesicle size and Transmission Electron Microscope were assessed for evaluation of proniosomes.Results: Entrapment efficiency (EE%) was found to be between 78.56% and 95.46%. The release profile of itraconazole proniosomes occurred in two distinct phases, an initial phase for about 8 h, followed by a slow phase for 16 h. The release pattern shown by these formulations was Higuchi diffusion controlled mechanism. The zeta potential values for all itraconazole proniosomes were in the range of-21.71 to-34.53 mV which confirms their stability. All itraconazoleproniosomes formula was found to be nano-sized and were appeared to be spherical in shape with sharp boundaries. One way analysis of variance (ANOVA) study showed that HLB (X1) had the main effects on most responses (Y).Conclusion: Box behnken design facilitates optimization of the formulation ingredients on entrapment efficiency, in vitro release of itraconazole proniosomes, zeta potential and vesicle size. Finally, an optimum level of factors was provided by the optimization process.

Characterization, Intestinal Absorption and Pharmacokinetics of Long-Circulating Nanoparticles Loaded with Panaxnotoginseng saponins

2013 ◽  
Vol 662 ◽  
pp. 227-232
Author(s):  
Guo Wei Zhao ◽  
Xu Long Chen ◽  
Xin Li Liang ◽  
Zheng Gen Liao ◽  
Chun Liu Wang ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Oral Administration ◽  
Intestinal Absorption ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Male Rats ◽  
Scanning Calorimetry ◽  
Time Curve ◽  
Vitro Release

The aim of the present study was to increase bioavailability after oral administration. In this study, Panaxnotoginseng saponins (PNS) was entrapped within the long-circulating nanoparticles (LCNs) by the multiple emulsion method. The PNS-LCNs were characterized in terms of size, zeta potential, morphology, thermal properties, drug entrapment efficiency (EE), and in vitro release of the PNS. In addition, the intestinal absorption of PNS-LCNs in vitro was investigated. The pharmacokinetics of PNS-LCNs following oral administration was determined over 72 h in male rats. It was found that the mean particle size and zeta potential of the PNS-LCNs were 147±4.5nm and −44.7±1.5mV, respectively, and the entrapment efficiency (EE) was 53.93%±0.69%. differential scanning calorimetry (DSC) indicated that PNS has different states in PNS-LCNs and original PNS. The release pattern of the PNS-LCNs followed the Weibull model. The release parameters (T50, TD) were observed to be higher for PNS-LCNs compared with original PNS (p< 0.01) in vitro release. The intestinal absorption study indicated that the intestinal permeability coefficient (Papp) of PNS-LCNs was higher than original PNS’s. The pharmacokinetics of PNS-LCNs was studied after oral administration to male rats, PNS-LCNs provided greater area under the concentration-time curve (AUC), higher plasma concentration (Cmax), longer mean residence time (MRT) and median time to maximum drug concentration (Tmax). LCNs could be used for improving permeability and increased bioavailability after oral administration of PNS.

Preparation and In-vitro Evaluation of Fe3O4 Encapsulated by Chitosan Loaded Capecitabine Nanoparticles for the Treatment of Breast Cancer

2016 ◽  
Vol 6 (3) ◽  
Author(s):  
Shanmuganathan S. ◽  
Nigma S. ◽  
Anbarasan B. ◽  
Harika B.
Keyword(s):  
Fe3o4 Nanoparticles ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Evaluation ◽  
Sem Image ◽  
Therapeutic Molecules ◽  
Dialysis Method ◽  
Vitro Release

Nanoparticulate Carriers which is biodegradable, biocompatible and bio adhesive have significant feasible applications for administration of therapeutic molecules. The present study was aimed to formulate and optimise Capecitabine loaded Chitosan-Fe3O4 Nanoparticles and to study the in-vitro evaluation by sigma dialysis method. Capecitabine loaded chitosan – Fe3O4 nanoparticles batches with different ratios of drug: polymer (1:1, 1:2, 1:3, 1:4, 1:5, 1:6) were prepared by ionic gelation method. Increase in polymer concentration increases the nanoparticle drug content. Entrapment efficiency was 60.12% with drug to polymer ratio F3 (1:3). In-vitro release was found to be 65.20% for 12 hrs. Capecitabine from chitosanFe3O4 nanoparticles SEM image reveals discrete spherical structure and particles with size range of 100-500nm. FTIR studies represent the functional groups present with no characteristics change in formulations. Samples stored at refrigerator conditions showed better stability compared with samples kept at other conditions during 8 weeks of storage.

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.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

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. 

Optimization and Characterization of Aqueous Micellar Formulations for Ocular Delivery of an Antifungal Drug, Posaconazole

2020 ◽  
Vol 26 (14) ◽  
pp. 1543-1555 ◽  
Author(s):  
Meltem E. Durgun ◽  
Emine Kahraman ◽  
Sevgi Güngör ◽  
Yıldız Özsoy
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Size Distribution ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
Glycol Succinate ◽  
Vitro Release

Background: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. Objective: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. Method: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. Results: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. Conclusion: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.

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