Development of modified polymer dot as stimuli-sensitive and 67Ga radio-carrier, for investigation of in vitro drug delivery, in vivo imaging and drug release kinetic

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.

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A Smart Drug Delivery System Based on Thermo-Responsive Polymer Gated Au NRs@SiO2 Nano-Platform

Journal of Nanoelectronics and Optoelectronics ◽

10.1166/jno.2021.3071 ◽

2021 ◽

Vol 16 (7) ◽

pp. 1029-1036

Author(s):

Hongzhu Wang ◽

Mengxun Chen ◽

Liping Song ◽

Youju Huang

Keyword(s):

Drug Delivery ◽

Block Copolymer ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Photothermal Therapy ◽

Drug Loading ◽

Temperature Sensitive

A key challenge for nanoparticles-based drug delivery system is to achieve manageable drug release in tumour cell. In this study, a versatile system combining photothermal therapy and controllable drug release for tumour cells using temperature-sensitive block copolymer coupled Au NRs@SiO2 is reported. While the Au NRs serve as hyperthermal agent and the mesoporous silica was used to improve the drug loading and decrease biotoxicity. The block copolymer acted as “gatekeeper” to regulate the release of model drug (Doxorubicin hydrochloride, DOX). Through in vivo and in vitro experiments, we achieved the truly controllable drug release and photothermal therapy with the collaborative effect of the three constituents of the nanocomposites. The reported nanocomposites pave the way to high-performance controllable drug release and photothermal therapy system.

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Using in vitro lipolysis and SPECT/CT in vivo imaging to understand oral absorption of fenofibrate from lipid-based drug delivery systems

Journal of Controlled Release ◽

10.1016/j.jconrel.2019.11.024 ◽

2020 ◽

Vol 317 ◽

pp. 375-384 ◽

Cited By ~ 2

Author(s):

Thuy Tran ◽

Peter Bønløkke ◽

Cristina Rodríguez-Rodríguez ◽

Zeynab Nosrati ◽

Pedro Luis Esquinas ◽

...

Keyword(s):

Drug Delivery ◽

In Vivo Imaging ◽

Drug Delivery Systems ◽

Oral Absorption ◽

Delivery Systems ◽

In Vitro Lipolysis

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Linseed hydrogel based floating drug delivery system for fluoroquinolone antibiotics: Design, in vitro drug release and in vivo real-time floating detection

Saudi Pharmaceutical Journal ◽

10.1016/j.jsps.2020.03.005 ◽

2020 ◽

Vol 28 (5) ◽

pp. 538-549 ◽

Cited By ~ 4

Author(s):

Fatima Akbar Sheikh ◽

Muhammad Ajaz Hussain ◽

Muhammad Umer Ashraf ◽

Muhammad Tahir Haseeb ◽

Muhammad Farid-ul-Haq

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Real Time ◽

Drug Delivery System ◽

In Vitro Drug Release ◽

Floating Drug Delivery ◽

Fluoroquinolone Antibiotics ◽

Floating Drug Delivery System

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

Journal of The Royal Society Interface ◽

10.1098/rsif.2018.0236 ◽

2018 ◽

Vol 15 (144) ◽

pp. 20180236 ◽

Cited By ~ 8

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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NANOMEDICINES: DELIVERING DRUGS USING BOTTOM UP NANOTECHNOLOGY

International Journal of Nanoscience ◽

10.1142/s0219581x05003802 ◽

2005 ◽

Vol 04 (05n06) ◽

pp. 855-861 ◽

Cited By ~ 1

Author(s):

MARTIN GARNETT

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Biodegradable Polymers ◽

Drug Loading ◽

Dna Delivery ◽

Delivery Systems ◽

The Body ◽

Nanosized Materials

The use of nanosized materials changes the way in which drugs are handled by the body and offers opportunities to improve drug delivery. The physiological mechanisms controlling the distribution of nanosized materials (enhanced permeability and retention effect, cellular uptake pathways and opsonisation/elimination of nanoparticles) are described. Two different nanosized drug delivery systems are considered; drug delivery and DNA delivery. The deficiencies of currently available biodegradable polymers for preparation of drug containing nanoparticles are mainly the amount of drug that can be incorporated and the rapid rate of drug release. The development of new biodegradable polymers which can interact with the drug and so significantly increase drug loading and decrease the rate of drug release are outlined. DNA delivery necessitates overcoming a variety of biological barriers. We are developing polyelectrolyte complexes of DNA with cationic polyamidoamines (PAA) as a delivery system. Complexing PAA with DNA results in good transfection of cells in vitro. However, in vivo, a more complex arrangement of PAA, Polyethylene glycol-PAA copolymers, DNA and the use of ligands will be required. Despite these efforts, further developments will be needed in nanotechnology for both drug and DNA nanoparticle delivery systems to achieve our clinical objectives.

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Laser-activated drug implant for controlled release to the posterior segment of the eye

10.1101/2020.06.17.111641 ◽

2020 ◽

Author(s):

Xingyu He ◽

Zheng Yuan ◽

Samantha Gaeke ◽

Winston W.-Y. Kao ◽

S. Kevin Li ◽

...

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Posterior Segment ◽

Zero Order ◽

First Order ◽

Drug Implants

AbstractThe current standard of care for posterior segment eye diseases, such as age-related macular degeneration and diabetic macular edema, is frequent intravitreal injections or sustained-release drug implants. Drug implants have side effects due to the burst release of the drugs, and their release cannot be easily controlled after implantation. Present study attempts to develop a dosage-controllable drug delivery implant which consists of a nanoporous biodegradable PLGA capsule and light-activated liposomes. Controllable drug release from the implant was achieved by using pulsed near-infrared (NIR) laser both in vitro and in vivo. The in vitro drug release kinetics from two different initial dose implants, 1000 μg and 500 μg, was analyzed by fitting zero order and first order kinetics, as well as the Korsmeyer-Peppas and Higuchi models. The 1000 μg and 500 μg implants fit the first-order and zero-order kinetics model, respectively, the best. The multiple drug releases in the vitreous was determined by in vivo fluorimeter, which was consistent with the in vitro data. The dose released was also clinically relevant. Histology and optical and ultrasound imaging data showed no abnormality in the eyes received implant treatment suggesting that the drug delivery system was safe to the retina. This on-demand dose-controllable drug delivery system could be potentially used for long-term posterior eye disease treatment.

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Formulation and evaluation of resveratrol loaded cubosomal nanoformulation for topical delivery

Current Drug Delivery ◽

10.2174/1567201817666200902150646 ◽

2020 ◽

Vol 17 ◽

Author(s):

Bhaskar Kurangi ◽

Sunil Jalalpure ◽

Satveer Jagwani

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

Topical Application ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Drug Permeation

Aim: The aim of the study was to formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC) through topical application. Background: Resveratrol (RV) is a nutraceutical compound that has exciting pharmacological potential in different diseases including cancers. Many studies of resveratrol have been reported for anti-melanoma activity. Due to its low bioavailability, the activities of resveratrol are strongly limited. Hence, an approach with nanotechnology has been done to increase its activity through transdermal drug delivery. Objective: To formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC). To evaluate resveratrol-loaded cubosomal gel (RC-Gel) for its topical application. Methods: RC was formulated by homogenization technique and optimized using a 2-factor 3-level factorial design. Formulated RCs were characterized for particle size, zeta potential, and entrapment efficiency. Optimized RC was evaluated for in vitro release and stability study. Optimized RC was further formulated into cubosomal gel (RC-Gel) using carbopol and evaluated for drug permeation and deposition. Furthermore, developed RC-Gel was evaluated for its topical application using skin irritancy, toxicity, and in vivo local bioavailability studies. Results: The optimized RC indicated cubic-shaped structure with mean particle size, entrapment efficiency, and zeta potential were 113±2.36 nm, 85.07 ± 0.91%, and -27.40 ± 1.40 mV respectively. In vitro drug release of optimized RC demonstrated biphasic drug release with the diffusion-controlled release of resveratrol (RV) (87.20 ± 2.25%). The RC-Gel demonstrated better drug permeation and deposition in mice skin layers. The composition of RC-Gel has been proved non-irritant to the mice skin. In vivo local bioavailability study depicted the good potential of RC-Gel for skin localization. Conclusion: The RC nanoformulation proposes a promising drug delivery system for melanoma treatment simply through topical application.

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