scholarly journals Supercritical Impregnation of Ketoprofen into Polylactic Acid for Biomedical Application: Analysis and Modeling of the Release Kinetic

Polymers ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 1982
Author(s):  
Lidia Verano Naranjo ◽  
Cristina Cejudo Bastante ◽  
Lourdes Casas Cardoso ◽  
Casimiro Mantell Serrano ◽  
Enrique José Martínez de la Ossa Fernández
Keyword(s):  
Drug Release ◽  
Polylactic Acid ◽  
Biomedical Application ◽  
Recovery Period ◽  
Controlled Drug Release ◽  
Release Kinetic ◽  
Temperature Conditions ◽  
Supercritical Impregnation ◽  
Release Devices

Ketoprofen (KET) is an anti-inflammatory drug often used in medicine due to its analgesic and antipyretic effects. If it is administered in a controlled form by means of different dosing devices, it acts throughout the patient’s recovery period improving its efficacy. This study intends to support the use of supercritical solvent impregnation (SSI) as an efficient technique to develop polylactic acid (PLA) functionalized with ketoprofen, for use as controlled drug release devices. For this purpose, firstly, the influence of different SSI variables on the desirable swelling of the polymer structure, while avoiding their foaming, were evaluated. Then, the resulting ketoprofen loading was evaluated under different pressure/temperature conditions. It was generally found that as pressure and temperature are higher, the drug impregnation loads also increase. The maximum impregnation loads (at about 9% KET/PLA) were obtained at 200 bar and 75 °C. In vitro drug release tests of the impregnated compound were also carried out, and it was found that drug release profiles were also dependent on the specific pressure and temperature conditions used for the impregnation of each polymer filament.

Design and Synthesis of a Novel Gabapentin-Phosphotidylcholine Conjugate for Targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier

2020 ◽  
Vol 16 ◽  
Author(s):  
Anjali P.B ◽  
Jawahar N. ◽  
Jubie S. ◽  
Neetu Yadav ◽  
Selvaraj A. ◽  
...  
Keyword(s):  
Drug Release ◽  
Phospholipase A2 ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Structural Analog ◽  
Fickian Diffusion ◽  
Release Kinetic ◽  
Nanostructured Lipid Carrier ◽  
Discovery Studio

Background: : Epilepsy is a genuine neurological turmoil that effects around 50 million individuals around the world. Practically 30% of epileptic patients experience the ill effects of pharmaco-obstruction, which is related with social seclusion, subordinate conduct, low marriage rates, joblessness, mental issues and diminished personal satisfaction. At present accessible antiepileptic drugs have a restricted viability, and their negative properties limit their utilization and cause challenges in patient administration. Gabapentin 1-(aminomethyl)cyclohexane acetic acid, Gbp , (trade name Neurontin), a structural analog of γ-aminobutyric acid (GABA), BCS class 3 drug with having permeability issues. Objective: This work was an attempt to formulate and characterize a new approach to treat epilepsy by targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier. Methods: Docking studied carried out using Accelrys Discovery studio 4.1 Client and gabapentin and phosphotidylcholine were conjugated through chemical conjugation. Nanostructured lipid carrier (NLC) was prepared using hot homogenization technique. Results: The libdock score of Gabapentin- Phosphotidylcholine conjugate (192.535) were found to be more than Gabapentin (77.1084) and Phosphotidylcholine (150.212). For the optimized formulation the particle size (50.08), zeta potential (-1.48), PDI (0.472) and entrapment efficiency (77.8) was observed. The NLC was studies for in-vitro drug release studies and release kinetics. Finally found that the drug release from the NLC followed Higuchi release kinetic and the mode of drug release from the NLC was found to be Non- Fickian diffusion. Conclusion: The formulated Nanostructured lipid carrier of Gabapentin-Phosphotidylcholine conjugate may be able to use to prevent seizure.

scholarly journals Organic-Inorganic Hybrid Hollow Mesoporous Organosilica Nanoparticles for Efficient Ultrasound-Based Imaging and Controlled Drug Release

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Xiaoqin Qian ◽  
Wenping Wang ◽  
Wentao Kong ◽  
Yu Chen
Keyword(s):  
Drug Release ◽  
Ultrasound Irradiation ◽  
Controlled Drug Release ◽  
Inorganic Hybrid ◽  
Templating Method ◽  
Anticancer Drug Delivery ◽  
Cavitation Effect ◽  
Contrast Enhanced

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.

scholarly journals FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN

2021 ◽  
pp. 206-215
Author(s):  
DHARMENDER PALLERLA ◽  
SUMAN BANOTH ◽  
SUNKARI JYOTHI
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Release Studies ◽  
Swelling Studies ◽  
Vitro Release

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.

scholarly journals FORMULATION AND IN VITRO–IN VIVO PHARMACOKINETIC EVALUATION OF CARDIOVASCULAR DRUG-LOADED PULSATILE DRUG DELIVERY SYSTEMS

2021 ◽  
pp. 144-151
Author(s):  
KUMAR BABU PASUPULETI ◽  
VENKATACHALAM A. ◽  
BHASKAR REDDY KESAVAN
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
The Core ◽  
Coated Tablet ◽  
Tablet Formulations ◽  
Core Tablet

Objective: This study is to formulate Nebivolol into a Pulsatile liquid, solid composite compression coated tablet, which will delay the release of the drug in early morning hypertension conditions. Methods: The liquid, solid composite tablet was formulated and compressed with the ethylcellulose coating polymer. The percent in vitro drug release of the liquid solid composite compressed tablet was tested. Based on disintegration time and wetting time, the LCS2, LCS3, LSC6, LCS7 and LCS12 formulations were found to be the optimized solid-liquid compacts fast-dissolving core tablet formulations, which may be excellent candidates for further coating with polymer to transfer into press coated pulsatile tablet formulations. Coating the core tablet with varying ethyl cellulose concentrations resulted in five different formulations of the pulsatile press-coated tablet (CT1, CT2, CT3, CT4, CT5). In vitro drug release, in vitro release, kinetic studies, in vivo pharmacokinetic and stability tests were all performed for the prepared pulsatile press coated tablet. Results: CT3 tablets are coated with ethyl cellulose polymer, which shows maximum controlled drug release from the core tablet i.e. 96.34±1.2% at 8th h. It shows there was an efficient delay in drug release form core tablet i.e. up to 3 h, followed by the maximum amount of drug release of 96.34±2.4 at 8h. Which shows the core drug will be more efficiently protected from the gastric acid environment 1.2 pH, duodenal environment 4.0 pH and release drug only in the small intestine. Conclusion: According to the findings, CT3 Pulsatile press-coated tablet increased the bioavailability of Nebivolol by 3.11 percent.

scholarly journals Prednisolone Loaded Tamarind Gum Microspheres for Colonic Delivery

2021 ◽  
pp. 324-332
Author(s):  
Harish K. Kunjwani ◽  
Dinesh M. Sakarkar
Keyword(s):  
Drug Release ◽  
Controlled Drug Release ◽  
Local Concentration ◽  
Colonic Delivery ◽  
Simulated Environment ◽  
S 100 ◽  
Long Time ◽  
Sensitive Property ◽  
Microsphere Preparation

The aim of this work was to formulate a novel multiparticulate system having pH sensitive property and specific enzyme biodegradability for colon specific drug delivery of Prednisolone (PD). Natural polysaccharide, Tamarind gum is used for microsphere preparation and Eudratit S- 100 for coating to provide pH controlled drug release. The formulation aims at minimal degradation and optimum delivery of the drug with relatively higher local concentration, which may provide more effective therapy for inflammatory bowel disease including Crohn disease and ulcerative colitis. Tamarind gum microspheres were prepared by emulsion dehydration technique using polymer in ratio of 1:1 to 1: 9. These microspheres were coated with Eudragit S-100 by oil in oil solvent evaporation method using core: coat ration (5:1). Tamarind gum microspheres and Eudragit coated tamarind gum microspheres were evaluated for surface morphology, particle size and size distribution, percentage drug entrapment, surface accumulation studies, in vitro drug release in simulated gastrointestinal fluids. The effect of various formulation variables were studied the prepared microspheres were spherical in shape in the size range of 64 µm to 113 µm, the encapsulation efficiency was in range of 30-72% depending upon the concentration of gum. The drug release was about 14-20% in first four hours of study gradually rises in 5th hour and 85% drug release occurs in 10-12% hr thus showing desirable drug release in the colonic simulated environment. PD tamarind gum microspheres are thought to have the potential to maintain drug concentration within target ranges for a long time, decreasing the side effects caused by concentration fluctuation, ensuring the efficiency of treatment and improving patient compliance by reducing dosing frequency. The animal study done using acetic acid induced colitis model on rats also suggest the anti inflammatory activity of the formulation.

FORMULATION AND EVALUATION OF NATEGLINIDE NANOSPONGES

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (02) ◽  
pp. 27-35
Author(s):  
A. A Bakliwal ◽  
◽  
D. S. Jat ◽  
S. G. Talele ◽  
A. G. Jadhav
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Synthesis Method ◽  
Ultra Sound ◽  
Size Analysis ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
Drug Content

The objective of the present study was to produce extended release nateglinide nanosponges for oral delivery. Preparation of nanosponges leads to solubility enhancement. Nateglinide is a BCS Class II drug, having low solubility. So, to increase the solubility of nateglinide it is formulated into nanosponges. Nanosponges using ethyl cellulose as a polymer and dichloromethane as a cross-linker were prepared successfully by ultra-sound assisted synthesis method. The effects of different drug: placebo ratios on the physical characteristics of the nanosponges as well as the drug content and in vitro drug release of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning and transmission electron microscopy of nanosponges showed that they were spongy in nature. The particle size was found to be in the range 46.37 - 97.23 nm out of which particle size of the optimized formulation was 51.79 nm and the drug content was found to 79.43 %. The optimized nanosponge formulations were selected for preparing nanosponge tablets for extended drug delivery by oral route. These tablets were prepared using xanthan gum and PVP K-30 and were evaluated by pre-compression and post-compression parameters. The nateglinide nanosponges tablet formulation were studied for different parameters using Design Expert Software. All formulations were evaluated for in vitro drug release analyzed according to various release kinetic models and it was found that it follows zero order release kinetics.

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF LEVOSULPIRIDE BY USING NATURAL POLYMER

2017 ◽  
Vol 10 (5) ◽  
pp. 285
Author(s):  
S Shanmugam
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Kinetic ◽  
Natural Polymers ◽  
In Vitro Drug Release

Objective: The objective of the present study was to develop sustained release matrix tablets of levosulpiride by using natural polymers.Method: The tablets were prepared with different ratios of Chitosan, Xanthan gum and Guar gum by wet granulation technique. The solubility study of the levosulpiride was conducted to select a suitable dissolution media for in vitro drug release studies.Results: Fourier transform infrared (FTIR) study revealed no considerable changes in IR peak of levosulpiride and hence no interaction between drug and the excipients. DSC thermograms showed that no drug interaction occurred during the manufacturing process. In vitro dissolution study was carried out for all the formulation and the results compared with marketed sustained release tablet. The drug release from matrix tablets was found to decrease with increase in polymer ratio of Chitosan, Xanthan gum and Guar gum.Conclusion: Formulation LF3 exhibited almost similar drug release profile in dissolution media as that of marketed tablets. From the results of dissolution data fitted to various drug release kinetic equations, it was observed that highest correlation was found for First order, Higuchi’s and Korsmeyer equation, which indicate that the drug release occurred via diffusion mechanism.  Keywords: Levosulpiride, sustained release tablets, natural polymers, in vitro drug release studies 

In Vitro and In Vivo Biocompatibility of Novel Zwitterionic Poly(Beta Amino)Ester Hydrogels Based on Diacrylate and Glycine for Site‐Specific Controlled Drug Release

2019 ◽  
Vol 220 (17) ◽  
pp. 1900188
Author(s):  
Vuk V. Filipović ◽  
Marija M. Babić ◽  
Dejan Gođevac ◽  
Aleksandar Pavić ◽  
Jasmina Nikodinović‐Runić ◽  
...  
Keyword(s):  
Drug Release ◽  
Controlled Drug Release ◽  
Amino Ester ◽  
Site Specific

scholarly journals A combined low-frequency electromagnetic and fluidic stimulation for a controlled drug release from superparamagnetic calcium phosphate nanoparticles: potential application for cardiovascular diseases

2018 ◽  
Vol 15 (144) ◽  
pp. 20180236 ◽  
Author(s):  
Alessandra Marrella ◽  
Michele Iafisco ◽  
Alessio Adamiano ◽  
Stefano Rossi ◽  
Maurizio Aiello ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Animal Model ◽  
Cardiovascular Diseases ◽  
Drug Release ◽  
Biological Effects ◽  
Low Frequency ◽  
Controlled Drug Release ◽  
Drug Dose

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.

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