Dissolution behavior of Olmesartan Medoxomil drug in Polymeric Micelles of Soluplus and Pluronic F127

2021 ◽  
pp. 2200-2204
Author(s):  
Suchetana Dutta ◽  
P. K. Kulkarni ◽  
Shailesh T.
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Olmesartan Medoxomil ◽  
Water Soluble ◽  
Pluronic F127 ◽  
Dissolution Behavior ◽  
Compatibility Study ◽  
Poorly Water Soluble

The aim of the present work was to study the dissolution behaviour of a poorly water-soluble Olmesartan Medoxomil (class II drug), by forming polymeric micelles (PMs) of SoluPlus and Pluronic F127. Polymeric Micelles of SoluPlus and Pluronic F127 were prepared by the co-solvent evaporation method. Drug and excipient compatibility study were carried out by Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry. The formulations were evaluated for particle size, Zeta Potential, Solubility studies, drug loading and encapsulation efficiency. Scanning Electron Microscopy (SEM) analysis was performed to study the surface morphology of the PMs. The SEM images showed spherical surface of the micelles. The drug loading efficiency was more for SoluPlus micelles compared to Pluronic F127 micelles. The Polymeric micelles showed negative zeta potential value indicating that they are stable and resist aggregation. The particle size was around 100nm and polydispersity index was less than 1 indicating uniform size distribution. The drug release from the SoluPlus micelles was higher than the Pluronic micelles. These results suggest that the polymeric micelles can be used to increase the solubility of poorly water-soluble drugs.

Dissolution Behaviour of the Poorly Water-Soluble Drug Mefenamic Acid from Polymeric Micelles

2018 ◽  
Vol 11 (3) ◽  
pp. 4098-4105
Author(s):  
Tibey Mary Koshy ◽  
Parthasarathi K Kulkarni
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Mefenamic Acid ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Water Soluble ◽  
Pluronic F127 ◽  
Compatibility Study ◽  
Dissolution Behaviour ◽  
Poorly Water Soluble

The aim of the work was to study the dissolution behaviour of the poorlywater-soluble drug mefenamic acid (MA), a NSAID, from polymeric micelles (PMs) of Pluronic F127 and DexbLG micelles.DexbLG Copolymer was synthesised by cross-linking reaction using Dextran and PLGA. Drug excipient compatibility study was carried out by Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). Pluronic F 127 and DexbLG Polymeric micelles formulation were prepared by co-solvent evaporation technique. Formulations were evaluated for particle size, Zeta potential, solubility studies, drug loading and encapsulation efficiency. Scanning electron microscopy (SEM) analysis was performed to study the size and surface morphology of the PMs. SEM image showed smooth surfaced spherical micelles. The drug loading efficiency was more inpluronic F 127 micelles. Polymeric micelles showed negative Zeta potential value indicating that they are stable and resist aggregation. Solubility of MA has increased to 6 - 13 folds from PMs of pluronic F127 and 4-11folds from DexbLG micelles. Particle size was less than 100 nm and polydispersity index was less than 0.5 indicating uniform size distribution. Percentage cumulative drug release from the Pluronic micelles was higher than DexbLG micelles. It can be concluded that MA PMs formulation has significantly increased the solubility and thereby increases the dissolution of the drug.These results suggest that polymeric micelles can be used to increase the solubility of poorly water-soluble drugs.  

scholarly journals SPRAY DRIED LACTOSE BASED PRONIOSOMES AS STABLE PROVESICULAR DRUG DELIVERY CARRIERS: SCREENING, FORMULATION, AND PHYSICOCHEMICAL CHARACTERIZATION

2018 ◽  
Vol 10 (5) ◽  
pp. 125 ◽  
Author(s):  
Ali Nasr ◽  
Mona Qushawy ◽  
Shady Swidan
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Oral Drug Delivery ◽  
Physicochemical Characterization ◽  
Water Soluble ◽  
Oral Drug ◽  
Flow Properties ◽  
Poorly Water Soluble ◽  
Spray Dried

Objective: In the present investigation efforts were considered to optimize the different conditions for the preparation of spray dried lactose based proniosomes. The aim of this research was to investigate the feasibility of proniosomes as stable precursors for the development of niosomes as oral drug delivery system for poorly water-soluble drugs.Methods: A total of twenty-eight plain proniosomal formulae were prepared with various surfactant-cholesterol loading ratios in each formula using spray dried lactose as a carrier. Span 20, 40, 60 and 80 were used in various molar ratios with cholesterol. Different evaluation techniques were performed to study the performance of the prepared proniosomes. The micromeritic properties of the prepared proniosomes were analyzed. The reconstituted niosomes were further evaluated for morphological characterization using transmission electron microscope (TEM), particle size analysis, zeta potential, and polydispersity index (PDI). Finally, selected proniosomal formulae were tested for stability study.Results: The proniosomal formulae prepared using span 40 and span 60 exhibited excellent flowability while those prepared with span 20 and span 80 showed poor flow properties. TEM photographs revealed that the vesicles were discrete, spherical without aggregation. The mean vesicle size of reconstituted niosomes was found to be in the range between (252.9±0.43–624.3±0.23 nm) with perfect PDI values (0.387±0.05–0.835±0.03). The negative values of zeta potential indicated that all prepared formulae were stabilized by electrostatic repulsion forces. Stability studies confirmed that proniosomes give a more stable system that could overcome the problems of standard niosomes. Formulae with the smallest particle size, higher surface charge values and best flow properties were selected to be loaded with poorly soluble drugs for further study.Conclusion: The obtained results offered evidence that spray-dried lactose based proniosomes are promising stable drug delivery carriers and ready to incorporate various poorly water-soluble drugs in order to improve their limited oral bioavailability.

scholarly journals FORMULATION AND EVALUATION OF ETHAMBUTOL POLYMERIC NANOPARTICLES

2020 ◽  
pp. 207-217
Author(s):  
MONOWAR HUSSAIN ◽  
ANUPAM SARMA ◽  
SHEIKH SOFIUR RAHMAN ◽  
ABDUL MATIN SIDDIQUE ◽  
TANUKU PAVANI EESWARI
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Compatibility Study ◽  
Bacterial Disease ◽  
Dose Frequency

Objective: Tuberculosis (TB) is an infectious bacterial disease caused by Mycobacterium tuberculosis which most commonly affects the lungs. TB has the highest mortality rate than any other infectious disease occurs worldwide. The main objective of the present investigation was to develop polymeric nanoparticles based drug delivery system to sustain the ethambutol (ETB) release by reducing the dose frequency. Methods: The Preformulation studies of drug ETB were done by physical characterization, melting point determination, and UV spectrophotometric analysis. The ETB loaded nanoparticles were prepared by double-emulsion (W/O/W) solvent evaporation/diffusion technique. The prepared polymeric nanoparticles were evaluated for particle size, polydispersity index, zeta potential, drug entrapment efficiency, drug loading, drug-polymer compatibility study, surface morphology, in vitro drug release, and release kinetics. Results: Based on the result obtained from the prepared formulations, F11 showed the best result and was selected as the optimized formulation. Optimized batch (F11) showed better entrapment efficiency (73.3%), good drug loading capacity (13.21%), optimum particle size (136.1 nm), and zeta potential (25.2 mV) with % cumulative drug release of 79.08% at the end of 24 h. Conclusion: These results attributed that developed polymeric nanoparticles could be effective in sustaining the ETB release over 24 h. Moreover, the developed nanoparticles could be an alternate method for ETB delivery with a prolonged drug release profile and a better therapeutic effect can be achieved for the treatment of tuberculosis.

scholarly journals Preparation and characterization of N-benzyl-N,O-succinyl chitosan polymeric micelles for solubilization of poorly soluble non-steroidal anti-inflammatory drugs

2017 ◽  
Vol 16 (10) ◽  
pp. 2349-2357
Author(s):  
Thisirak Woraphatphadung ◽  
Warayuth Sajomsang ◽  
Theerasak Rojanarata ◽  
Prasert Akkaramongkolporn ◽  
Tanasait Ngawhirunpat ◽  
...  
Keyword(s):  
Particle Size ◽  
Surface Charge ◽  
Polymeric Micelles ◽  
Rank Order ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Water Soluble ◽  
Loading Efficiency ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Purpose: To investigate the solubilization of poorly water-soluble non-steroidal  anti-inflammatory drugs (NSAIDs) in N-benzyl-N,O-succinyl chitosan (BSCS)  polymeric micellesMethods: BSCS was synthesized by reductive amination and succinylation,  respectively. NSAIDs; meloxicam (MX), piroxicam (PRX), ketoprofen (KP) and indomethacin (IND) were entrapped in the hydrophobic inner cores by evaporation method. The effects of drug structure on loading efficiency, particle size and surface charge of micelles were investigated.Results: The critical micelle concentration of BSCS micelles was 0.0385 mg/mL and cytotoxicity on Caco-2 cells depends on the polymer concentration (IC50 = 3.23 ± 0.08 mg/mL). BSCS micelles were able to entrap MX, PRX, KP and IND and also improve the solubility of drugs. Drug loading efficiency was highly dependent on the drug molecules. The drug loading capacity of these BSCS micelles was in the following rank order: KP (282.9 μg/mg) > PRX (200.8 μg/mg) > MX (73.7 μg/mg) > IND (41.2 μg/mg). The highest loading efficiency was observed in KP-loaded BSCS micelles due to the attractive force between phenyl groups of KP and benzyl groups of the polymer. Particle size and surface charge were in the range of 312 - 433 nm and -38 to -41 mV, respectively.Conclusion: BSCS copolymer presents desirable attributes for enhancing the  solubility of hydrophobic drugs. Moreover, BSCS polymeric micelles might be beneficial carrier in a drug delivery system.Keywords: BSCS, polymeric micelles, solubilization, non-steroidal anti-inflammatory drugs

scholarly journals Inulin-Grafted Stearate (In-g-St) as the Effective Self-Assembling Polymeric Micelle: Synthesis and Evaluation for the Delivery of Betamethasone

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Gholamabbas Chehardoli ◽  
Parham Norouzian ◽  
Farzin Firozian
Keyword(s):  
Zeta Potential ◽  
Sustained Release ◽  
Targeted Delivery ◽  
Encapsulation Efficiency ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Polymeric Micelle ◽  
Water Soluble ◽  
Burst Release ◽  
Potential Measurement

Background. Betamethasone as a corticosteroid drug is commonly used for the treatment of rheumatoid arthritis. Unfortunately, betamethasone is a low water-soluble drug and its efficacy is low. So an attractive strategy is the targeted delivery of betamethasone to the damaged joint using polymeric micelle-based carriers. Methods. Inulin-grafted stearate (In-g-St) was synthesized via the reaction of stearoyl chloride and inulin, then characterized by FT-IR and H-NMR. In-g-St forms micelles in the presence of betamethasone. The prepared polymeric micelles were characterized for size, zeta potential, drug loading, particles’ morphology, critical micelle concentration (CMC), and encapsulation efficiency. So sustained release polymeric micelles of betamethasone were developed by employing In-g-St. Results. The measurement of particle size showed a mean diameter of 60 and 130 nm for 10% and 20% drug-loaded micelles, respectively, and SEM showed that the particle’s morphologies are spherical. Zeta potential measurement for the drug-containing micelles showed a value of -11.8 mV. Drug loading efficiency and the encapsulation efficiency were 6.36% and 63.6%, as well as 18.97% and 94.88% for 10% and 20%, respectively. 20% drug-loaded polymer showed a small burst release of betamethasone at the first 3 h which was followed by sustained release in the next 24 h. Furthermore, the formula with 10% exhibited good sustained release properties except for the minor initial burst release. Conclusion. Data from the zeta potential, CMC, drug loading capacity, and in vitro drug release studies indicated that In-g-St polymeric micelles can be suitable candidates for the efficient delivery of hydrophobic drugs like betamethasone.

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.

scholarly journals Formulation and In Vitro Evaluation of Casein Nanoparticles as Carrier for Celecoxib

2020 ◽  
Vol 10 (3) ◽  
pp. 408-417
Author(s):  
Jyotsana R. Madan ◽  
Izharahemad N. Ansari ◽  
Kamal Dua ◽  
Rajendra Awasthi
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
Polydispersity Index ◽  
Drug Dissolution ◽  
Permeation Studies ◽  
Poorly Water Soluble

Purpose : The objective of this work was to formulate casein (CAS) nanocarriers for the dissolution enhancement of poorly water soluble drug celecoxib (CLXB). Methods: The CLXB loaded CAS nanocarriers viz., nanoparticles, reassembled CAS micelles and nanocapsules were prepared using sodium caseinate (SOD-CAS) as a carrier to enhance the solubility of CLXB. The prepared formulations were characterized for particle size, polydispersity index, zeta potential, percentage entrapment efficiency, and surface morphology for the selection of best formulation. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray powder diffraction study was used to for the confirmation of encapsulation of CLXB. Further, in vitro drug dissolution, ex-vivo permeation studies on chicken ileum and stability studies were carried out. Results: The CLXB loaded casein nanoparticles (CNP) (batch A2) showed a particle size diameter 216.1 nm, polydispersity index 0.422 with percentage entrapment efficiency of 90.71% and zeta potential of -24.6 mV. Scanning electron microscopy of suspension confirmed globular shape of CNP. The in vitro release data of optimized batch followed non Fickian diffusion mechanism. The ex vivo permeation studies on chicken ileum of CLXB loaded CNP showed permeation through mucous membrane as compared to pure CLXB. The apparent permeability of best selected freeze dried CLXB loaded CNP (batch A2) was higher and gradually increased from 0.90 mg/cm2 after 10 min to a maximum of 1.95 mg/cm2 over the subsequent 90 min. A higher permeation was recorded at each time point than that of the pure CLXB. Conclusion: The study explored the potential of CAS as a carrier for solubility enhancement of poorly water soluble drugs.

scholarly journals Uptake of Etoposide in CT-26 Cells of Colorectal Cancer Using Folate Targeted Dextran Stearate Polymeric Micelles

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Farshid Hassanzadeh ◽  
Hojjat Sadeghi-Aliabadi ◽  
Farzin Firozian
Keyword(s):  
Colorectal Cancer ◽  
Particle Size ◽  
Nmr Spectroscopy ◽  
Zeta Potential ◽  
Cellular Uptake ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Research Areas ◽  
Ir And Nmr Spectroscopy ◽  
Ft Ir

Targeted drug delivery using folate receptors is one of the most interesting chemotherapeutic research areas over the past few years. A novel folate targeted copolymer was synthesized using dextran stearate coupled to folic acid. FT-IR and NMR spectroscopy were used to confirm successful conjugation. Micelles prepared using this copolymer were characterized for their particle size, zeta potential, critical micelle concentration (CMC), drug loading capacity, and release efficiency. Cytotoxicity and cellular uptake of the micelles were estimated using CT-26 colorectal carcinoma cell line. FT-IR and NMR spectroscopy confirmed production of folate grafted dextran stearate copolymer. Low CMC value indicates that the copolymers are suitable for preparation of stable micelles useful in parenteral dosage forms. Particle size and zeta potential of the targeted nanoparticles were105.5±2.0 nm and −21.2 mV, respectively. IC50of etoposide loaded in folate grafted dextran stearate enhanced about 20-fold compared to the pure drug (0.49±0.11 μg/mL versus9.41±0.52 μg/mL). It seems that etoposide loaded in micelles of folate grafted dextran stearate copolymer is promising in reducing drug resistance of colorectal cancer by boosting etoposide cellular uptake.

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.

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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