scholarly journals The Interactions between Ciprofloxacin and Parenteral Nutrition Admixtures

Pharmaceutics ◽  
2019 ◽  
Vol 12 (1) ◽  
pp. 27 ◽  
Author(s):  
Aleksandra Gostyńska ◽  
Maciej Stawny ◽  
Katarzyna Dettlaff ◽  
Anna Jelińska
Keyword(s):  
Particle Size ◽  
Pulmonary Embolism ◽  
Zeta Potential ◽  
Parenteral Nutrition ◽  
Calcium Ions ◽  
Visual Inspection ◽  
Color Change ◽  
Molar Ratio ◽  
Fat Emulsion ◽  
Potential Interactions

Background: Co-infusion of parenteral nutrition (PN) and other drugs increases the risk of the interaction between drug and PN admixtures that can cause embolization of small blood vessels, resulting in potentially fatal consequences, including pulmonary embolism, or liver and retina vascular damage. The present study aimed to determine the compatibility between ciprofloxacin (CF) and eighteen compounded PN admixtures in order to assess the possibility of their co-administration via Y-sites. Methods: CF and PN admixtures were mixed at two volume ratios (1:1 and 2:1) and potential interactions were examined using visual inspection, and measurements of pH, osmolality particle size, and zeta potential. The analyses were conducted immediately after sample preparation and after four hours of storage. Results: The compatibility tests showed that the addition of the CF to the PN admixtures did not cause any color change or sign of destabilization in the fat emulsion. However, precipitation was observed in formulations containing higher CF concentrations and, in the case of lower CF concentrations, in formulations containing magnesium and calcium ions at a molar ratio of 2:1. Conclusions: The administration of CF and PN admixtures via the Y-site should be avoided or performed only with PN admixtures for which compatibility has been confirmed and the CF concentration in samples is 1 mg/mL at a molar ratio of magnesium to calcium ions of 1:1.

scholarly journals Formulation and Characterization of Carvedilol Leciplex for Glaucoma Treatment: In-Vitro, Ex-Vivo and In-Vivo Study

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 197 ◽  
Author(s):  
Doaa Hassan ◽  
Rehab Abdelmonem ◽  
Menna Abdellatif
Keyword(s):  
Particle Size ◽  
Intraocular Pressure ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Duration Of Action ◽  
Corneal Permeability ◽  
Glaucoma Treatment

This study evaluated the efficacy of cationic nanoparticle (leciplex) to deliver carvedilol to ocular surface for glaucoma treatment as recent studies pointed out the effect of topical carvedilol on intraocular pressure, therefore carvedilol loaded leciplex formulae were prepared using soy phosphatidyl choline (SPC) and cationic surfactant (CTAB/DDAB) and characterized for morphology, entrapment efficiency, particle size, zeta potential and ex-vivo corneal permeation. Then the selected formula was evaluated via in-vivo studies in comparison with carvedilol solution. Leciplex nanoparticles appeared spherical in shape with entrapment efficiency exceeded 95% in all formulae. Leciplex formula composed of SPC and DDAB in (1:1) molar ratio showed the smallest particle size (16.04 ± 1.2 nm), highest zeta potential value (53.9 ± 0.91 mv) and highest apparent corneal permeability coefficient (0.1157 cm/h). Carvedilol leciplex reduced intraocular pressure (IOP) to normal range in ocular hypertensive rabbits after 30 min and duration of action lasted for 24 h, while carvedilol solution reduced IOP to normal value after 60 min and duration of action lasted for 6 h. Furthermore, histological examination of eyeballs of rabbits treated with carvedilol leciplex showed improvement of retinal atrophy of glaucomatous eyes. This study concluded that leciplex improve transcorneal permeation and bioavailability of carvedilol.

scholarly journals Assessment of the Effect of PLGA Co-polymers and PEG on the Formation and Characteristics of PLGA-PEG-PLGA Co-block Polymer Using Statistical Approach

2019 ◽  
Vol 9 (3) ◽  
pp. 382-392 ◽  
Author(s):  
Teuku Nanda Saifullah Sulaiman ◽  
Dwi Larasati ◽  
Akhmad Kharis Nugroho ◽  
Syaiful Choiri
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Statistical Approach ◽  
Phase Particle ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Scanning Calorimetry ◽  
Particle Size Reduction ◽  
Block Polymers ◽  
Block Polymer

Purpose: To assess the effect of the lactic acid (LA)-to-glycolic acid (GA) molar ratio and polyethylene glycol (PEG) concentration on the formation of poly-lactide co-glycolide acid (PLGA)-PEG-PLGA co-block polymers simultaneously using statistical approach. Methods: A 22 full factorial design with the addition of a point in the center of the design, namely curvature, was applied. Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), and nuclear magnetic resonance (NMR) were performed to confirm the formation of the co-block polymer. Simvastatin (SMV), a drug model was incorporated into the nano-polymeric micellar (NpM) of PLGA-PEG-PLGA followed by solubility phase, particle size, zeta potential, and entrapment efficiency characterizations. Results: FTIR, DSC, and NMR successfully confirmed the formation of co-block polymers. Solubility of SMV increased from 2 to 44-folds depending on co-block concentration with entrapment efficiency of 59%-80%. The NpM had size in the range of 206 to 402 nm with negative zeta potential. LA to GA ratio had greater effect on particle size reduction and increasing of co-polymer length. In addition, it had higher contributions on increasing of solubility and entrapment efficiency of SMV than PEG. Conclusion: According to these findings, the LA to GA ratio and PEG concentration gained a great consideration in order to prepare the PLGA-PEG-PLGA co-block which fulfilled the quality target product profile of NpM delivery system.

scholarly journals Effect of Molecular Weight and Molar Ratio of Dextran on Self-Assembly of Dextran Stearate Polymeric Micelles as Nanocarriers for Etoposide

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Farshid Hassanzadeh ◽  
Hojjat Sadeghi ◽  
Farzin Firozian ◽  
Mina Mirian
Keyword(s):  
Molecular Weight ◽  
Particle Size ◽  
Zeta Potential ◽  
Self Assembly ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Molar Ratio ◽  
Loading Capacity ◽  
Hydrophobic Polymers ◽  
Polymer Surfactants

Amphiphilic polymer surfactants are composed of hydrophilic and hydrophobic polymers and are widely used in targeted drug delivery. The purpose of this study was the evaluation of the effect of molecular weight and molar ratio of dextran on physicochemical properties of dextran stearate polymeric micelles. Dextran stearate was synthesized by acylation of dextran with stearoyl chloride. Etoposide loaded polymeric micelles were prepared by dialysis method. The resulting micelles were evaluated for particle size, zeta potential, critical micelle concentration (CMC), drug loading capacity, and release efficiency. Cytotoxicity and cellular uptake of micelles were studied in CT-26 colorectal carcinoma cell line. Molecular weight and molar ratio of dextran-stearate were impressive on zeta potential, CMC, drug loading capacity, and release efficiency. Unlike polymer molecular weight, molar ratio of stearate had a significant effect on cytotoxicity and particle size of etoposide loaded micelles. Although molecular weight of dextran had no significant effect on cytotoxicity of micelles on CT-26 cells, it had drastic attributes for stability of polymeric micelles. Consequently, both variables of molecular weight of dextran and molar ratio of stearate should be taken into account to have a stable and effective micelle of dextran-stearate.

Preparation and Characterization of Stable Dispersions of Ni Nanoparticles

2007 ◽  
Vol 534-536 ◽  
pp. 117-120 ◽  
Author(s):  
Eun Hee Lee ◽  
Min Ku Lee ◽  
Chang Kyu Rhee
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Particle Size Distribution ◽  
Visual Inspection ◽  
Organic Media ◽  
Ni Nanoparticles ◽  
Colloid Stability ◽  
Nanoparticle Suspensions ◽  
Polymeric Dispersant

Colloid stability of the suspensions of Ni nanoparticles has been investigated with adding polymeric dispersant in various organic media. We characterized the dispersion stability of Ni nanoparticles by means of visual inspection, transmission profiles measured by Turbiscan, the particle size distribution, and the zeta potential. 0.01 wt% of Ni nanoparticles were found to be optimally dispersed in ethanol among various organic media employed in this study with adding the dispersant (0.6 wt%-2 wt%). As the concentration of the dispersant increased, the particle size decreased in size from 300 nm to 200 nm due to less coalescence. The zeta potential values of the Ni nanoparticles in suspensions with the dispersant were greater than -40mV. Such stable Ni nanoparticle suspensions are attributed to the electrosteric effect of the polymeric dispersant.

scholarly journals 503. In vitro Evaluation of Sitagliptin-HIV-1 Trans-activator Transcription Peptide Nano-formula for Antiviral Activity Against SARS-CoV-2: Drug Repurposing Approach

2021 ◽  
Vol 8 (Supplement_1) ◽  
pp. S354-S354
Author(s):  
Khalid Eljaaly ◽  
Hani Asfour ◽  
Tarek Ibrahim ◽  
Osama Ahmed ◽  
Nabil Alhakamy ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Repurposing ◽  
Inhibitory Effect ◽  
Molar Ratio ◽  
Target Cells ◽  
Protease Inhibition ◽  
3Cl Protease ◽  
Hiv 1

Abstract Background The outbreak of COVID-19 pandemic in China regarded as a major health/economic hazard. The importance of coming up with mechanisms for preventing or treating COVID-19 has been felt across the world. This work aimed at examining the efficiency of Sitagliptin (SIT) and human immunodeficiency virus type 1 (HIV-1) trans-activator transcription peptide (TAT) against SARS-CoV-2. Methods SIT-TAT nano-conjugates were prepared according to a full three-factor bi-level (23) factorial design. SIT concentration (mM, X1), TAT concentration (mM, X2), and pH (X3) were selected as the factors. Particle size (nm, Y1) and zeta potential (mV, Y2) were assessed as responses. Characterization of the optimized formula for Fourier-transformed infrared (FTIR) and Transmission electron microscope was carried out. In addition, IC50 in Vero E6 cells, In vitro 3CL-protease inhibition and docking tests were investigated. Results The prepared complex’s formula was as follows 1: 1 SIT: TAT molar ratio, whereas zeta potential and particle size values were at 34.17 mV and 97.19 nm, respectively. This combination did exhibit its antiviral potentiality against SARS-CoV-2 via IC50 values of 9.083 5.415, and 16.14 µM for TAT, SIT-TAT, and SIT, respectively. In addition, the complex SIT-TAT showed a significant (P < 0.001) viral-3CL-protease inhibitory effect (IC50 = 3.959 µM ± 0.011) in comparison to isolated components (IC50 = 10.93 µM ± 0.25) and TAT (IC50 = 8.128 µM ± 0.42). This was further confirmed via in silico study. Molecular docking investigation has shown promising binding affinity of the formula components towards SARS-CoV-2 main protease (3-CL). Conclusion While offering significant binding interactions with protein’s key pocket residues, an optimized formulation of SIT-TAT could guarantee both the enhanced delivery to the target cells and the improved cellular uptake. The presented findings would guarantee further investigations regarding formula optimization against SARS-CoV-2. Disclosures All Authors: No reported disclosures

scholarly journals Evaluation of the Antiviral Activity of Sitagliptin-Glatiramer Acetate Nano-Conjugates against SARS-CoV-2 Virus

2021 ◽  
Vol 14 (3) ◽  
pp. 178
Author(s):  
Nabil A. Alhakamy ◽  
Osama A. A. Ahmed ◽  
Tarek S. Ibrahim ◽  
Hibah M. Aldawsari ◽  
Khalid Eljaaly ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Glatiramer Acetate ◽  
Molar Ratio ◽  
Target Cells ◽  
Protease Inhibition ◽  
23 Factorial Design ◽  
Ic50 Values ◽  
Approved Drugs ◽  
3Cl Protease

The outbreak of the COVID-19 pandemic in China has become an urgent health and economic challenge. There is a current race for developing strategies to treat and/or prevent COVID-19 worldwide. Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the strain of coronavirus that causes COVID-19. The aim of the present work was to evaluate the efficacy of the combined complex (nano-conjugates) of two FDA-approved drugs, sitagliptin (SIT) and glatiramer acetate (GA), against a human isolate of the SARS-CoV-2 virus. SIT-GA nano-conjugates were prepared according to a full three-factor bilevel (23) factorial design. The SIT concentration (mM, X1), GA concentration (mM, X2), and pH (X3) were selected as the factors. The particle size (nm, Y1) and zeta potential (mV, Y2) were assessed as responses. Characterization of the optimized formula for the Fourier-transform infrared (FTIR) spectroscopy and transmission electron microscopy (TEM) was carried out. In addition, the half-maximal inhibitory concentration (IC50) in Vero-E6 epithelial cells previously infected with the virus was investigated. The results revealed that the optimized formula of the prepared complex was a 1:1 SIT:GA molar ratio at a pH of 10, which met the required criteria with a desirability value of 0.878 and had a particle size and zeta potential at values of 77.42 nm and 27.67 V, respectively. The SIT-GA nano-complex showed antiviral potential against an isolate of SARS-CoV-2 with IC50 values of 16.14, 14.09, and 8.52 µM for SIT, GA, and SIT-GA nano-conjugates, respectively. Molecular docking has shown that the formula’s components have a high binding affinity to the COVID 3CL protease, essential for coronavirus replication, paralleled by 3CL protease inhibition (IC50 = 2.87 µM). An optimized formulation of SIT-GA could guarantee both enhanced deliveries to target cells and improved cellular uptake. Further clinical studies are being carried out to validate the clinical efficacy of the optimized formulation against SARS-CoV-2.

Incorporation of micro/nanoparticles of PCL with essential oil of Cymbopogon nardus in bacterial cellulose

2018 ◽  
Vol 1 (2) ◽  
pp. 37
Author(s):  
Aline Krindges ◽  
Vanusca Dalosto Jahno ◽  
Fernando Morisso
Keyword(s):  
Particle Size ◽  
Particulate Matter ◽  
Essential Oil ◽  
Zeta Potential ◽  
Bacterial Cellulose ◽  
Culture Medium ◽  
Static Culture ◽  
Cymbopogon Nardus ◽  
Cellulose Membranes

Incorporation studies of particles in different substrates with herbal assets growing. The objective of this work was the preparation and characterization of micro/nanoparticles containing cymbopogon nardus essential oil; and the incorporation of them on bacterial cellulose. For the development of the membranes was used the static culture medium and for the preparation of micro/nanoparticles was used the nanoprecipitation methodology. The incorporation of micro/nanoparticles was performed on samples of bacterial cellulose in wet and dry form. For the characterization of micro/nanoparticles were carried out analysis of SEM, zeta potential and particle size. For the verification of the incorporation of particulate matter in cellulose, analyses were conducted of SEM and FTIR. The results showed that it is possible the production and incorporation of micro/nanoparticles containing essential oil in bacterial cellulose membranes in wet form with ethanol.

Novel Formulation Development and Evaluation of Nanoparticles Based in Situ Gelling System for The Ophthalmic Delivery of Ciprofloxacin Hydrochloride

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Loading ◽  
In Vitro Release ◽  
Formulation Development ◽  
Ciprofloxacin Hydrochloride ◽  
Potential Value ◽  
The Mean ◽  
In Situ Gelling

Ciprofloxacin hydrochloride loaded Eudragit RS100 nanoparticles were prepared by using w/o/w emulsification (multiple emulsification) solvent evaporation followed by drying of nanoparticles at 50°C. The nanoparticles were further incorporated into the pH-triggered in situ gel forming system which was prepared using Carbopol 940 in combination with HPMC as viscosifying agent. The developed nanoparticles was evaluated for particle size, zeta potential value and loading efficiency; nanoparticle incorporated in situ gelling system was evaluated for pH, clarity, gelling strength, rheological studies, in-vitro release studies and ex-vivo precorneal permeation studies. The nanopaticle showed the mean particle size varying between 263.5nm - 325.9 nm with the mean zeta potential value of -5.91 mV to -8.13 mV and drug loading capacity varied individually between 72.50% to 98.70% w/w. The formulation was clear with no suspended particles, showed good gelling properties. The gelling was quick and remained for longer time period. The developed formulation was therapeutically efficacious, stable and non-irritant. It provided the sustained release of drug over a period of 8-10 hours.

Formulation and Evaluation of Nanosuspension of Simvastatin

2015 ◽  
Vol 8 (2) ◽  
pp. 2858-2873
Author(s):  
Rupali L. Shid ◽  
Shashikant N. Dhole ◽  
Nilesh Kulkarni ◽  
Santosh L Shid
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Factorial Design ◽  
Dissolution Rate ◽  
In Vitro Dissolution ◽  
Total Drug ◽  
23 Factorial Design ◽  
Rate Of Dissolution

Poor water solubility and slow dissolution rate are issues for the majority of upcoming and existing biologically active compounds. Simvastatin is poorly water-soluble drug and its bioavailability is very low from its crystalline form. The purpose of this study wasto increase the solubility and dissolution rate of simvastatin by the  preparation of nanosuspension by emulsification solvent diffusion method at laboratory scale. Prepared nanosus-pension was evaluated for its particle size and in vitro dissolution study and characterized by zeta potential,differential scanning calorimetry (DSC) and X-Ray diffractometry (XRD), motic digital microscopy, entrapment efficiency, total drug content, saturated solubility study and in vivo study. A 23 factorial design was employed to study the effect of independent variables, amount of SLS (X1), amount of PVPK-30 (X2) and poloxamer-188 (X3) and dependent variables are total drug content and polydispersity Index. The obtained results showed that particle size (nm) and rate of dissolution has been improved when nanosuspension prepared with the higherconcentration of PVPK-30 with the higher concentration of PVP K-30 and Poloxamer-188 and lower concentration of SLS. The particle size and zeta potential of optimized formulation was found to be 258.3 nm and 23.43. The rate of dissolution of the optimized nanosuspension was enhanced (90% in 60min), relative to plain simvastatin  (21% in 60 min), mainly due to the formation of nanosized particles. These results indicate the suitability of 23 factorial  design for preparation of simvastatin loaded nano-suspension significantly improved in vitro dissolution rate and thus possibly enhance fast onset of therapeutic drug effect. In vivo study shows increase in bioavailability in nanosuspension formulation than the plain simvastatin drug.

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.

Sign in / Sign up

Export Citation Format

Share Document