In vitro and in vivo behavior of ground tadalafil hot-melt extrudates: How the carrier material can effectively assure rapid or controlled drug release

2017 ◽  
Vol 528 (1-2) ◽  
pp. 498-510 ◽  
Author(s):  
Anna Krupa ◽  
Oriane Cantin ◽  
Beata Strach ◽  
Elżbieta Wyska ◽  
Zbisław Tabor ◽  
...  
2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Xiaoqin Qian ◽  
Wenping Wang ◽  
Wentao Kong ◽  
Yu Chen

A novel anticancer drug delivery system with contrast-enhanced ultrasound-imaging performance was synthesized by a typical hard-templating method using monodispersed silica nanoparticles as the templates, which was based on unique molecularly organic/inorganic hybrid hollow periodic mesoporous organosilicas (HPMOs). The highly dispersed HPMOs show the uniform spherical morphology, large hollow interior, and well-defined mesoporous structures, which are very beneficial for ultrasound-based theranostics. The obtained HPMOs exhibit excellent performances in contrast-enhanced ultrasonography bothin vitroandin vivoand can be used for the real-time determination of the progress of lesion tissues during the chemotherapeutic process. Importantly, hydrophobic paclitaxel- (PTX-) loaded HPMOs combined with ultrasound irradiation show fast ultrasound responsiveness for controlled drug release and higherin vitroandin vivotumor inhibition rates compared with free PTX and PTX-loaded HPMOs, which is due to the enhanced ultrasound-triggered drug release and ultrasound-induced cavitation effect. Therefore, the achieved novel HPMOs-based nanoparticle systems will find broad application potentials in clinically ultrasound-based imaging and auxiliary tumor chemotherapy.


2019 ◽  
Vol 220 (17) ◽  
pp. 1900188
Author(s):  
Vuk V. Filipović ◽  
Marija M. Babić ◽  
Dejan Gođevac ◽  
Aleksandar Pavić ◽  
Jasmina Nikodinović‐Runić ◽  
...  

2018 ◽  
Vol 15 (144) ◽  
pp. 20180236 ◽  
Author(s):  
Alessandra Marrella ◽  
Michele Iafisco ◽  
Alessio Adamiano ◽  
Stefano Rossi ◽  
Maurizio Aiello ◽  
...  

Alternative drug delivery approaches to treat cardiovascular diseases are currently under intense investigation. In this domain, the possibility to target the heart and tailor the amount of drug dose by using a combination of magnetic nanoparticles (NPs) and electromagnetic devices is a fascinating approach. Here, an electromagnetic device based on Helmholtz coils was generated for the application of low-frequency magnetic stimulations to manage drug release from biocompatible superparamagnetic Fe-hydroxyapatite NPs (FeHAs). Integrated with a fluidic circuit mimicking the flow of the cardiovascular environment, the device was efficient to trigger the release of a model drug (ibuprofen) from FeHAs as a function of the applied frequencies. Furthermore, the biological effects on the cardiac system of the identified electromagnetic exposure were assessed in vitro and in vivo by acute stimulation of isolated adult cardiomyocytes and in an animal model. The cardio-compatibility of FeHAs was also assessed in vitro and in an animal model. No alterations of cardiac electrophysiological properties were observed in both cases, providing the evidence that the combination of low-frequency magnetic stimulations and FeHAs might represent a promising strategy for controlled drug delivery to the failing heart.


Author(s):  
R. Shireesh Kiran ◽  
B. Chandra Shekar ◽  
B. Nagendra Babu

In the current study, gastro-retentive tablets of Ritonavir was developed to increase its oral bioavailability using hydrophilic polymers HPMC K 4M, K 15M, and K 100M as release retarding agents. Polyox WSR 303 was chosen as resin, sodium bicarbonate was used as effervescent agents. The tablets were prepared by direct compression method and FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K 100M, Crospovidone, Polyox WSR 303 and sodium bicarbonate, as gas generating agent was choosen as optimized formulation based on the evaluation parameters, floating lag time (33 sec) and total floating time (>24 h) and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product was shown 98.67% and 95.09 ± 5.01% of drug release respectively. From in vivo bioavailability studies, after oral administration of floating tablet containing 100 mg Ritonavir, the Cmax, Tmax, and AUC0–∞ of optimized gastroretentive formulation were found to be 30.11 ± 1.16μg/mL, 8.00±1.23 h and 173 ± 26.34μg*h/ml, respectively. Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for improved bioavailability.


2018 ◽  
Vol 8 (5-s) ◽  
pp. 215-222
Author(s):  
Mohammed Ali Firyal ◽  
Muthanna Ahmed Hameed

Modification of Pectin as natural polymer was accepted as new bio adhesive polymer, which was grafted with Maleic anhydride as vinylic monomore and insertion by using ceric ion it, was substituted with amino drugs produced amide polymer which do not lose their biological properties. This design carries controlled delivery which could release the entrapped drug over an extended period of time due to its slow digesting nature. The prepared adhesive drug polymer was characterized by FTIR, 1H-NMR spectroscopes, thermo gravimetric analysis TGA and DSC were careful. Physical properties of prepared polymer was quiet, Biological activity was studied for adhesive drug polymer, this new adhesive drug biological polymers were applied on different infected mice and wounds, It gave outstanding results and compliance mice infected with a full recovery by a short period of time.  The prepared drug copolymer was analyzed in different pH values at 37 0C in vitro study and controlled drug release was messured through three days. The rate of hydrolysis in basic medium was found higher than acidic medium. It was concluded that modified drug release with extended drug action via slow release and in vivo performance was renowned to be talented.  Keywords: Pectin, controlled delivery, adhesive drug polymers, Graft Copolymer


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