d-α-Tocopheryl polyethylene glycol 1000 succinate conjugated folic acid nanomicelles: towards enhanced bioavailability, stability, safety, prolonged drug release and synergized anticancer effect of plumbagin

RSC Advances ◽  
2016 ◽  
Vol 6 (81) ◽  
pp. 78106-78121 ◽  
Author(s):  
Atmaram Pawar ◽  
Rabiya Patel ◽  
S. Arulmozhi ◽  
C. Bothiraja
Keyword(s):  
Folic Acid ◽  
Polyethylene Glycol ◽  
Drug Release ◽  
Targeted Delivery ◽  
Anticancer Effect ◽  
Polyethylene Glycol 1000 ◽  
Prolonged Drug Release

Plumbagin (PLB) loadedd-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) with folic acid (FOL) conjugated nanomicelles achieved controlled and targeted delivery with synergized anticancer potency and reduced PLB toxicity.

scholarly journals Targeted delivery of antibiotics to the infected pulmonary tissues using ROS-responsive nanoparticles

2019 ◽  
Vol 17 (1) ◽  
Author(s):  
Yu Wang ◽  
Qian Yuan ◽  
Wei Feng ◽  
Wendan Pu ◽  
Jun Ding ◽  
...  
Keyword(s):  
Folic Acid ◽  
Drug Release ◽  
Targeted Delivery ◽  
Bacterial Infections ◽  
Phenylboronic Acid ◽  
Vitro Assay ◽  
Control Drug ◽  
Lung Dysfunction ◽  
Mucus Barrier

Abstract Background Immunocompromised individuals and those with lung dysfunction readily acquire pulmonary bacterial infections, which may cause serious diseases and carry a heavy economic burden. Maintaining adequate antibiotic concentrations in the infected tissues is necessary to eradicate resident bacteria. To specifically deliver therapeutics to the infected pulmonary tissues and enable controlled release of payloads at the infection site, a ROS-responsive material, i.e. 4-(hydroxymethyl) phenylboronic acid pinacol ester-modified α-cyclodextrin (Oxi-αCD), was employed to encapsulate moxifloxacin (MXF), generating ROS-responsive MXF-containing nanoparticles (MXF/Oxi-αCD NPs). Results MXF/Oxi-αCD NPs were coated with DSPE-PEG and DSPE-PEG-folic acid, facilitating penetration of the sputum secreted by the infected lung and enabling the active targeting of macrophages in the inflammatory tissues. In vitro drug release experiments indicated that MXF release from Oxi-αCD NPs was accelerated in the presence of 0.5 mM H2O2. In vitro assay with Pseudomonas aeruginosa demonstrated that MXF/Oxi-αCD NPs exhibited higher antibacterial activity than MXF. In vitro cellular study also indicated that folic acid-modified MXF/Oxi-αCD NPs could be effectively internalized by bacteria-infected macrophages, thereby significantly eradicating resident bacteria in macrophages compared to non-targeted MXF/Oxi-αCD NPs. In a mouse model of pulmonary P. aeruginosa infection, folic acid-modified MXF/Oxi-αCD NPs showed better antibacterial efficacy than MXF and non-targeted MXF/Oxi-αCD NPs. Meanwhile, the survival time of mice was prolonged by treatment with targeting MXF/Oxi-αCD NPs. Conclusions Our work provides a strategy to overcome the mucus barrier, control drug release, and improve the targeting capability of NPs for the treatment of pulmonary bacterial infections.

scholarly journals In VitroCharacterization of Pluronic F127 and D--Tocopheryl Polyethylene Glycol 1000 Succinate Mixed Micelles as Nanocarriers for Targeted Anticancer-Drug Delivery

2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Adeel Masood Butt ◽  
Mohd Cairul Iqbal Mohd Amin ◽  
Haliza Katas ◽  
Narong Sarisuta ◽  
Wasu Witoonsaridsilp ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Polyethylene Glycol ◽  
Anticancer Drug ◽  
Targeted Delivery ◽  
Mixed Micelles ◽  
Chemotherapeutic Agents ◽  
Pluronic F127 ◽  
Breast Adenocarcinoma ◽  
Anticancer Drug Delivery ◽  
Polyethylene Glycol 1000

Mixed micelles of Pluronic F127 andD-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) in different molar ratios (10 : 0, 7 : 3, 5 : 5, and 3 : 7) were prepared to characterize this system as nanocarriers for targeted delivery of chemotherapeutic agents. Their size, zeta potential, critical micelle concentration, drug loading content, entrapment efficiency, drug release, cytotoxicity, and stability in serum were evaluatedin vitroby using doxorubicin as the model anticancer drug. The micellar sizes ranged from 25 to 35 nm. The 7 : 3 and 5 : 5 micellar combinations had lower critical micelle concentrations ( M) than the 10 : 0 combination ( M). The entrapment efficiencies of the 7 : 3, 5 : 5, and 3 : 7 micellar combinations were 72%, 88%, and 69%, respectively. Doxorubicin release was greater at acidic tumour pH than at normal physiological pH. The doxorubicin-loaded mixed micelles showed greater percent inhibition and apoptosis activity in human breast adenocarcinoma (MCF-7) and acute monocytic leukaemia (THP-1) cell lines than free doxorubicin did. The mixed micelles were also stable against aggregation and precipitation in serum. These findings suggest that Pluronic F127-TPGS mixed micelles could be used as nanocarriers for targeted anticancer-drug delivery.

pH Dependent Release Potential of Natural Polymers in Sustained Release of Ornidazole From Colon Targeted Delivery System)

2019 ◽  
Vol 9 (02) ◽  
Author(s):  
Sharma Pankaj ◽  
Tailang Mukul
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Targeted Delivery ◽  
Guar Gum ◽  
Acidic Environment ◽  
Natural Polymers ◽  
Weight Variation ◽  
Curve Determination ◽  
Preformulation Studies

The aim of present work was to prepare colon specific delivery system of Ornidazole using different ratio of shellac, zein and guar gum. From study of various literature it revealed that shellac, zein and guar gum released drug from dosage form at the pH of 6.9, 11.5, 7-9 respectively. The main problem associated with colon targeted drug delivery system is degradation of drug in the acidic environment of stomach to circumvent the present problem different combinations of shellac, zein and guar gum were employed in the formulation of colon targeted tablet. Several preformulation parameters were determined such as melting point, FTIR spectroscopy, preparation of calibration curve, determination of λmax and partition coefficient. After the preformulation studies, next steps were preparation of core tablets, evaluation of core of tablets and coating of tablets. The data obtained from preformulation study seven formulations were developed and evaluated for various parameters. Based on evaluated parameter such as weight variation, friability, dissolution study, invitro drug release etc. the F7 formulation show better results colon targeted tablets. Drug content in F7 formulation was 95% and drug release after 6 hrs was 96%. Formulation containing combination of shellac, zein and guar gum released least amount of drug in the acidic environment of stomach and released most of the drug in colon. It is evide

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