scholarly journals Mixed Pluronic—Cremophor Polymeric Micelles as Nanocarriers for Poorly Soluble Antibiotics—The Influence on the Antibacterial Activity

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 435
Author(s):  
Maria Antonia Tănase ◽  
Adina Raducan ◽  
Petruţa Oancea ◽  
Lia Mara Diţu ◽  
Miruna Stan ◽  
...  
Keyword(s):  
Mixed Micelles ◽  
Polymeric Micelles ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Antibacterial Properties ◽  
Delivery Systems ◽  
Pluronic F127 ◽  
Clinical Strain ◽  
Cremophor El ◽  
Antibiotic Drug

In this work, novel polymeric mixed micelles from Pluronic F127 and Cremophor EL were investigated as drug delivery systems for Norfloxacin as model antibiotic drug. The optimal molar ratio of surfactants was determined, in order to decrease critical micellar concentration (CMC) and prepare carriers with minimal surfactant concentrations. The particle size, zeta potential, and encapsulation efficiency were determined for both pure and mixed micelles with selected composition. In vitro release kinetics of Norfloxacin from micelles show that the composition of surfactant mixture generates tunable extended release. The mixed micelles exhibit good biocompatibility against normal fibroblasts MRC-5 cells, while some cytotoxicity was found in all micellar systems at high concentrations. The influence of the surfactant components in the carrier on the antibacterial properties of Norfloxacin was investigated. The drug loaded mixed micellar formulation exhibit good activity against clinical isolated strains, compared with the CLSI recommended standard strains (Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29213, Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922). P. aeruginosa 5399 clinical strain shows low sensitivity to Norfloxacin in all tested micelle systems. The results suggest that Cremophor EL-Pluronic F127 mixed micelles can be considered as novel controlled release delivery systems for hydrophobic antimicrobial drugs.

Self-assemble Amphiphilic PEO-PPO-PEO Tri-block Co-polymeric Methotrexate Nanomicelles to Combat Against MCF7 Cancer Cells

2020 ◽  
Vol 17 ◽  
Author(s):  
Manoj Kumar Mishra ◽  
Jitendra Gupta ◽  
Reena Gupta
Keyword(s):  
Sustained Release ◽  
Partition Coefficient ◽  
Cancer Cells ◽  
Intravenous Administration ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
Sds Micelles

Background: Methotrexate (MTX) is a water-insoluble, anti-tumor agent, causes adverse effects like bone marrow suppression, chronic interstitial obstructive pulmonary disease, hepatotoxicity, leukopenia, interstitial pneumonitis and nephrotoxicity with slow drug release rate. Objective: The present study was aimed for successfully incorporating of MTX into novel-targeted Pluronic (PEO-PPOPEO tri-block co-polymer) F127 polymeric micelles intended for intravenous administration with improved drug loading and sustained release behavior necessary to achieve better efficacy of MTX. Method: MTX-loaded Pluronic F127 micelles were characterized for critical micelle concentration, particle size and zeta potential, 1H NMR, drug loading, encapsulation efficiency characterization, cell uptake, in-vitro release study along with partition coefficient and solubilization thermodynamics. Results: The micellar formulation resulted in nano size 27.32±1.43nm of PF127/SDS, as compared to Pluronic F127 micelles or PF127/Phosphatidyl choline which were 30.52±1.18nm and 154.35±5.5nm respectively. The uptake of PF127/SDS micellar formulation incorporating Rhodamine 123 in MCF7 cancer cells was found to be higher (84.25%) than PF127/PC, PF127 and MTX i.e. 66.26%, 73.59% and 53% respectively. The in-vitro MTX release from PF127, PF127/SDS and PF127/PC polymeric micelles formulations was observed 69%, 69.5% and 66% at 12 h whereas 80.89%, 77.67% and 78.54% after 24 h respectively and reveals sustained release. MTX loaded PF127/SDS micelles showed high Partition coefficient and negative free energy of solubilization compared to PF127 and PF127/PC which signifies self-assembly behavior and thermodynamic stability towards dissociation to be higher. Conclusion: Finally concluded that MTX loaded PF127/SDS micelles act as a potential anticancer delivery system in comparison to PF127/PC and PF127 to combat against tumor cells by enhancing its cellular uptake targeting with sustained release pattern and reducing the thermodynamic instability. Thus, PF127/SDS micellar formulation can provide a useful alternative dosage form for intravenous administration of MTX.

scholarly journals Functionalized Mesoporous Silica Nanoparticles as Delivery Systems for Doxorubicin: Drug Loading and Release

2021 ◽  
Vol 11 (13) ◽  
pp. 6121
Author(s):  
Candace M. Day ◽  
Martin J. Sweetman ◽  
Yunmei Song ◽  
Sally E. Plush ◽  
Sanjay Garg
Keyword(s):  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Mesoporous Silica Nanoparticles ◽  
Release Kinetics ◽  
Drug Loading ◽  
In Vitro Release ◽  
Delivery Systems ◽  
Stimuli Responsive ◽  
Kinetics Of

Functionalized nanoparticles have played a major role in the field of targeted therapy, owing to their ability to control the release and for the selective delivery of entrapped materials to tumours. In this work, we described the loading capacity and in vitro release kinetics of mesoporous silica nanoparticles (MSNs), functionalized with Poly-L-Histidine and Tamoxifen. The model drug Doxorubicin (DOX) was successfully encapsulated into MSN-based systems, using the technique of solvent immersion. A post-surface grafting loading method was investigated on functionalized systems, with DOX loading content determined using HPLC. Dialysis bag diffusion was employed to investigate the release kinetics of DOX-loaded-systems at pH 7.4 and 5. The amount of DOX released from native MSNs systems over a 72 h period at pH 5 was approximately 40%; and at pH 7.4 ≈ 30%. A moderate pH dependent release behaviour was observed with both our functionalized systems: DOX@MSN-PLH and DOX@MSN-PLH-TAM; with approximately 5% of DOX released from DOX@MSN-PLH-TAM at pH 7.4 and about 9% released at pH 7.4 over 72 h. The maximal cumulated release of DOX molecules from DOX@MSN-PLH after 72 h was ≈ 18% at pH 7.4 and ≈ 23% at pH 5, respectively. The outcome of this work offers a promising contribution towards building future stimuli-responsive nano-drug delivery systems.

Enhanced Release Kinetics and Stability of Resveratrol Loaded Self Nanoemulsifying Delivery Systems Developed using Experimental Design

2019 ◽  
Vol 9 (2) ◽  
pp. 128-145 ◽  
Author(s):  
Monika Sharma ◽  
Rajeev Garg ◽  
Satish Sardana
Keyword(s):  
Central Composite Design ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Oral Formulation ◽  
Delivery Systems ◽  
The Novel ◽  
Novel Approach ◽  
Vitro Release ◽  
Central Composite

Background: Resveratrol is a member of the stilbene family emerged as a leading candidate for improving healthspan through potentially slowing the aging process and preventing chronic diseases. A number of institutions and scientists specialized in this field across the world are working to develop a promising Self Emulsifying formulation to enhance bioavailability of hydrophobic resveratrol using oil. Objective: The objective of the current study is to develop self-nano emulsifying drug delivery systems using long-chain triglycerides of resveratrol to enhance solubility, stability, release kinetics and to overcome low bioavailability. Methods: Solubility studies performed in different lipids, surfactants and cosurfactants. Phase diagrams constructed to select the areas of nanoemulsion. SNEDDS formulation was optimized using 33 central composite design considering lipid (X1), surfactant (X2) and co-surfactant (X3) as critical variables, optimized formulation was located using overlay plot. Results: The nanometer size and high values of zeta potential depicted non-coalescent nature of SNEDDS. The resulted SNEDDS formulation had improved in vitro release followed by Hixson Crowell model with higher regression R2value 0. 929. Thermodynamic stability studies ascertained stable formulation. Mean droplet size in selected nanocarrier was found to be 83.29 nm. The nanocarriers subjected to 2-8°C (45% RH), 25-30°C (60% RH) and 45-50°C (75% RH) in glass vials exhibited no significant changes in 3 months. Conclusion: The novel approach was developed by selecting optimum blends of lipids, surfactants and cosurfactant using central composite design. This study not only offers a good example of augmenting bioavailability of resveratrol but will also provide a promising oral formulation for clinical application.

Formulation and Evaluation of Solubility Enhanced Ciprofloxacin

2013 ◽  
Vol 6 (3) ◽  
pp. 2131-2136
Author(s):  
R S Thakur ◽  
A Nayaz ◽  
Y Koushik
Keyword(s):  
Oral Absorption ◽  
Polymeric Micelles ◽  
In Vitro Release ◽  
Microemulsion System ◽  
Salt Form ◽  
Solubility Study ◽  
Ternary Phase Diagrams ◽  
Blood Ph ◽  
Vitro Release

In the case of solubility limited absorption, creating supersaturation in the GI fluid is very critical as supersaturation may provide great improvement of oral absorption. The techniques to create the so-called supersaturation in the GI fluid include microemulsions, emulsions, liposomes, complexations, polymeric micelles, and conventional micelles. Ciprofloxacin was chosen because it is practically insoluble in water; hence its salt form is used commercially, which is soluble in water. The objective of the present investigation was to enhance the solubility of Ciprofloxacin by formulating it into microemulsion system. For this purpose, initially, surfactant and cosurfactant were selected based on their HLB value, followed by pseudo-ternary phase diagrams to identify the microemulsion existing zone. Different formulations were developed and evaluated for pH, conductivity, in vitro release and stability. Solubility study was performed for optimized formulation. The pH of the designed formulations varied from 6.02-7.04. This was ideal and near blood pH 7.4. Conductivity data indicated that the microemulsion was of the o/w type. In vitro release of optimized formulation(FM3) was 95.2% as compared to pure drug 46.61% after 90 min and marketed product(salt form) 93.9%. Hence, by formulating into microemulsion, the solubility of ciprofloxacin is significantly enhanced.    

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.

Formulation and Evaluation of Atorvastatin Calcium-Poly-ε-Caprolactone Nanoparticles Loaded Ocular Inserts for Sustained Release and Antiinflammatory Efficacy

2020 ◽  
Vol 21 (15) ◽  
pp. 1688-1698
Author(s):  
Germeen N.S. Girgis
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
In Vivo Study ◽  
Average Weight ◽  
Drug Release Profile ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory

Purpose: The work was performed to investigate the feasibility of preparing ocular inserts loaded with Poly-ε-Caprolactone (PCL) nanoparticles as a sustained ocular delivery system. Methods: First, Atorvastatin Calcium-Poly-ε-Caprolactone (ATC-PCL) nanoparticles were prepared and characterized. Then, the optimized nanoparticles were loaded within inserts formulated with Methylcellulose (MC) and Polyvinyl Alcohol (PVA) by a solvent casting technique and evaluated physically, for in-vitro drug release profile. Finally, an in-vivo study was performed on the selected formulation to prove non-irritability and sustained ocular anti-inflammatory efficacy compared with free drug-loaded ocuserts. Results: The results revealed (ATC-PCL) nanoparticles prepared with 0.5% pluronic F127 were optimized with 181.72±3.6 nm particle size, 0.12±0.02 (PDI) analysis, -27.4± 0.69 mV zeta potential and 62.41%±4.7% entrapment efficiency. Nanoparticles loaded ocuserts manifested compatibility between drug and formulation polymers. Moreover, formulations complied with average weight 0.055±0.002 to 0.143±0.023 mg, and accepted pH. ATC-PCL nanoparticles loaded inserts prepared by 5% MC showed more sustained, prolonged in-vitro release over 24h. In-vivo study emphasized non-irritability, ocular anti-inflammatory effectiveness represented by smaller lid closure scores, and statistically significant lowering in PMN count after 3h. Conclusion: These findings proposed a possibly simple, new and affordable price technique to prepare promising (ATC-PCL) nanoparticles loaded inserts to achieve sustained release with prolonged antiinflammatory efficacy.

Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery

2020 ◽  
Vol 20 ◽  
Author(s):  
Sahil Kumar ◽  
Bandna Sharma ◽  
Tilak R. Bhardwaj ◽  
Rajesh K. Singh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Drug Release ◽  
Anticancer Agents ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Specific Treatment ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

Aims: In the present study, polymer-drug conjugates were synthesized based on azo-bond cleavage drug delivery approach for targeting erlotinib as anticancer drug specifically to the colon for the proficient treatment of colon cancer. Background: Colon cancer (CC) is the third commonly detected tumor worldwide and it make up about 10 % of all cases of cancers. Most of the chemotherapeutic drugs available for treating colon cancer are not only toxic to cancerous cells but also to the normal healthy cells. Among the various approaches to get rid of the adverse effects of anticancer agents, prodrugs are one of the most imperative approaches. Objective: The objective of the study is to chemically modify the erlotinib drug through azo-bond linkage and suitable spacer which will be finally linked to polymeric backbone to give desired polymer linked prodrug. The azo reductase enzyme present in colon is supposed to cleave the azo-bond specifically and augment the drug release at the colon. Methods: The synthesized conjugates were characterized by IR and 1H-NMR spectroscopy. The cleavage of aromatic azobond resulted in a potential colon-specific liberation of drug from conjugate studied in rat fecal contents. In vitro release profiles of polyphosphazene-linked conjugates of erlotinib have been studied at pH 1.2, pH 6.8 and pH 7.4. The stability study was designed to exhibit that free drug was released proficiently and unmodified from polyphosphazene-erlotinib conjugates having aromatic azo-bond in artificial colon conditions. Results: The synthesized conjugates were demonstrated to be stable in simulated upper gastro-intestinal tract conditions. The drug release kinetics shows that all the polymer-drug conjugates of erlotinib follow zero-order release kinetics which indicates that the drug release from the polymeric backbone is independent of its concentration. Kinetic study of conjugates with slope (n) shows the anomalous type of release with an exponent (n) > 0.89 indicating a super case II type of release. Conclusion: These studies indicate that polyphosphazene linked drug conjugates of erlotinib could be the promising candidates for the site-specific treatment of colon cancer with least detrimental side-effects.

Nanomaterials as drug delivery systems with antibacterial properties: current trends and future priorities

2021 ◽  
Author(s):  
Khatereh Khorsandi ◽  
Reza Hosseinzadeh ◽  
Homa Sadat Esfahani ◽  
Saeedeh Keyvani-Ghamsari ◽  
Saeed Ur Rahman
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Antibacterial Properties ◽  
Delivery Systems ◽  
Current Trends

scholarly journals Clinoptilolite Microparticles as Carriers of Catechin-Rich Acacia Catechu Extracts: Microencapsulation and In Vitro Release Study

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1655
Author(s):  
Zvezdelina Yaneva ◽  
Donika Ivanova ◽  
Nikolay Popov
Keyword(s):  
Composite System ◽  
Release Kinetics ◽  
Spectral Characteristics ◽  
In Vitro Release ◽  
Medium Ph ◽  
Release Capacity ◽  
Bioactive Substance ◽  
Acacia Catechu ◽  
Vitro Release

The main goal of the present study was to investigate the microencapsulation, in vitro release capacity and efficiency of catechin-rich Acacia catechu extract by Clinosorbent-5 (CLS-5) microparticles by in-depth detailed analyses and mathematical modelling of the encapsulation and in vitro release kinetics behaviour of the polyphenol-mineral composite system. The bioflavanol encapsulation and release efficiency on/from the mineral matrix were assessed by sorption experiments and interpretative modelling of the experimental data. The surface and spectral characteristics of the natural bioactive substance and the inorganic microcarrier were determined by Fourier Transform Infrared Spectroscopy (FTIR) and Ultraviolet/Visible (UV/Vis) spectrophotometric analyses. The maximum extent of catechin microencapsulation in acidic medium was 32%. The in vitro release kinetics study in simulated enzyme-free gastric medium (pH = 1.2) approved 88% maximum release efficiency achieved after 24 h. The in vitro release profile displayed that the developed bioflavanol/clinoptilolite microcarrier system provided sustained catechin in vitro release behaviour without an initial burst effect. Thus, the results from the present study are essential for the design and development of innovative catechin-CLS-5 microcarrier systems for application in human and veterinary medicine.

Sign in / Sign up

Export Citation Format

Share Document