Drug Release
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2021 ◽  
Vol 22 ◽  
pp. 100581
A.I. Karacolak ◽  
F.M. Emen ◽  
D. Kılıç ◽  
E. Kutlu ◽  
M.A. Ali ◽  

Polymers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 3541
Muhammad Suhail ◽  
Chuan-Ming Shih ◽  
Jia-Yu Liu ◽  
Wan-Chu Hsieh ◽  
Yu-Wen Lin ◽  

Glutamic acid-co-poly(acrylic acid) (GAcPAAc) hydrogels were prepared by the free radical polymerization technique using glutamic acid (GA) as a polymer, acrylic acid (AAc) as a monomer, ethylene glycol dimethylacrylate (EGDMA) as a cross-linker, and ammonium persulfate (APS) as an initiator. Increase in gel fraction was observed with the increasing concentration of glutamic acid, acrylic acid, and ethylene glycol dimethylacrylate. High percent porosity was indicated by developed hydrogels with the increase in the concentration of glutamic acid and acrylic acid, while a decrease was seen with the increasing concentration of EGDMA, respectively. Maximum swelling and drug release was exhibited at high pH 7.4 compared to low pH 1.2 by the newly synthesized hydrogels. Similarly, both swelling and drug release increased with the increasing concentration of glutamic acid and acrylic acid and decreased with the increase in ethylene glycol dimethylacrylate concentration. The drug release was considered as non-Fickian transport and partially controlled by viscoelastic relaxation of hydrogel. In-vivo study revealed that the AUC0–∞ of fabricated hydrogels significantly increased compared to the drug solution and commercial product Keten. Hence, the results indicated that the developed hydrogels could be used as a suitable carrier for controlled drug delivery.

2021 ◽  
Vol 11 (20) ◽  
pp. 9541
Zhichu Xiang ◽  
Mouquan Liu ◽  
Jun Song

Biocompatible nanosystems based on polymeric materials are promising drug delivery nanocarrier candidates for antitumor therapy. However, the efficacy is unsatisfying due to nonspecific accumulation and drug release of the nanoparticles in normal tissue. Recently, the nanosystems that can be triggered by tumor-specific stimuli have drawn great interest for drug delivery applications due to their controllable drug release properties. In this review, various polymers and external stimuli that can be employed to develop stimuli-responsive polymeric nanosystems are discussed, and finally, we delineate the challenges in designing this kind of Nanomedicine to improve the therapeutic efficacy.

Cancers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 5146
Marjolein I. Priester ◽  
Sergio Curto ◽  
Ann L. B. Seynhaeve ◽  
Anderson Cruz Perdomo ◽  
Mohamadreza Amin ◽  

This paper presents three devices suitable for the preclinical application of hyperthermia via the simultaneous high-resolution imaging of intratumoral events. (Pre)clinical studies have confirmed that the tumor micro-environment is sensitive to the application of local mild hyperthermia. Therefore, heating is a promising adjuvant to aid the efficacy of radiotherapy or chemotherapy. More so, the application of mild hyperthermia is a useful stimulus for triggered drug release from heat-sensitive nanocarriers. The response of thermosensitive nanoparticles to hyperthermia and ensuing intratumoral kinetics are considerably complex in both space and time. To obtain better insight into intratumoral processes, longitudinal imaging (preferable in high spatial and temporal resolution) is highly informative. Our devices are based on (i) an external electric heating adaptor for the dorsal skinfold model, (ii) targeted radiofrequency application, and (iii) a microwave antenna for heating of internal tumors. These models, while of some technical complexity, significantly add to the understanding of effects of mild hyperthermia warranting implementation in research on hyperthermia.

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1679
Anna Lion ◽  
Ricky D. Wildman ◽  
Morgan R. Alexander ◽  
Clive J. Roberts

One of the most striking characteristics of 3D printing is its capability to produce multi-material objects with complex geometry. In pharmaceutics this translates to the possibility of dosage forms with multi-drug loading, tailored dosing and release. We have developed a novel dual material hot-melt inkjet 3D printing system which allows for precisely controlled multi-material solvent free inkjet printing. This reduces the need for time-consuming exchanges of printable inks and expensive post processing steps. With this printer, we show the potential for design of printed dosage forms for tailored drug release, including single and multi-material complex 3D patterns with defined localised drug loading where a drug-free ink is used as a release-retarding barrier. For this, we used Compritol HD5 ATO (matrix material) and Fenofibrate (model drug) to prepare both drug-free and drug-loaded inks with drug concentrations varying between 5% and 30% (w/w). The printed constructs demonstrated the required physical properties and displayed immediate, extended, delayed and pulsatile drug release depending on drug localisation inside of the printed formulations. For the first time, this paper demonstrates that a commonly used pharmaceutical lipid, Compritol HD5 ATO, can be printed via hot-melt inkjet printing as single ink material, or in combination with a drug, without the need for additional solvents. Concurrently, this paper demonstrates the capabilities of dual material hot-melt inkjet 3D printing system to produce multi-material personalised solid dosage forms.

Ashish Y. Pawar ◽  
Sejal R. Jadhav ◽  
Deelip V. Derle

Despite advancements in medicines and novel surgical methods, osteomyelitis is still a complex and difficult to treat multi-bacterial bone infection. It generates in tissue necrosis along with rupturing of bone in chronic cases leading towards limited vascularity at infection site, local treatment might not show accountable level of antibiotic at infection site. The present research aims towards development and evaluation of bio-degradable implant of Ciprofloxacin hydrochloride to treat local osteomyelitis. Chitosan is widely investigated biodegradable polymer with hydroxyl moiety which is active and can be altered chemically to develop biomedical and therapeutic dosage forms. Here this active group was modified using epichlorohydrin & crosslinked Chitosan matrices were used as carrier to formulate different Ciprofloxacin implant. In vivo parameters and in vitro study was conducted for optimized batch. The formulation having 40% drug loading (EC4) was found to be optimum when all evaluation parameters were tested. The concentration of Ciprofloxacin Hydrochloride (HCl) in bone and surrounding tissues is much higher than minimum inhibitory concentration (MIC) even after a month. After observing the water uptake and extended release of drug from all formulations the drug loading was found to be higher. The present work concluded that, the highly branched chitosan remarkably reduce the percent (%) drug release up to a month which could be useful in the treatment of osteomyelitis.

2021 ◽  
Vol 11 (1) ◽  
Miroslav Almáši ◽  
Anna Alexovič Matiašová ◽  
Monika Šuleková ◽  
Eva Beňová ◽  
Juraj Ševc ◽  

AbstractA drug delivery system based on mesoporous particles MCM-41 was post-synthetically modified by photo-sensitive ligand, methyl-(2E)-3-(4-(triethoxysilyl)-propoxyphenyl)-2-propenoate (CA) and the pores of MCM-41 particles were loaded with Naproxen sodium salt (NAP). The CA was used as a photoactive molecule that can undergo a reversible photo-dimerization by [2π + 2π] cycloaddition when irradiated with UV light of specific wavelengths. Thus, it has a function of gate-keeper that is responsible for opening/closing the pores and minimizing premature release of NAP. The physicochemical properties of the prepared system were studied by infrared spectroscopy (IR), nitrogen adsorption measurements, thermogravimetric analysis (TGA), scanning transmission electron microscopy (STEM) and energy dispersive X-ray spectroscopy (EDX). The mechanism of the opening/closing pores was confirmed by UV measurements. In vitro and in vivo drug release experiments and the concentration of released NAP was determined by UV spectroscopy and high-performance liquid chromatography (HPLC). In vivo drug release in the blood circulatory system of rats has demonstrated the effective photo-cleavage reaction of CA molecules after UV-light stimulation. The localization and morphological changes of the particles were studied in the blood and liver of rats at different time intervals. The particles in the blood have been shown to retain their original rod-like shape, and the particles in the liver have been hydrolysed, which has resulted in spherical shape with a reduced size.

Yingnan Liu ◽  
Lei Xie ◽  
Meng Gao ◽  
Runhao Zhang ◽  
Jingchen Gao ◽  

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1654
Lorenzo Marsili ◽  
Michele Dal Bo ◽  
Federico Berti ◽  
Giuseppe Toffoli

Microgels can be considered soft, porous and deformable particles with an internal gel structure swollen by a solvent and an average size between 100 and 1000 nm. Due to their biocompatibility, colloidal stability, their unique dynamicity and the permeability of their architecture, they are emerging as important candidates for drug delivery systems, sensing and biocatalysis. In clinical applications, the research on responsive microgels is aimed at the development of “smart” delivery systems that undergo a critical change in conformation and size in reaction to a change in environmental conditions (temperature, magnetic fields, pH, concentration gradient). Recent achievements in biodegradable polymer fabrication have resulted in new appealing strategies, including the combination of synthetic and natural-origin polymers with inorganic nanoparticles, as well as the possibility of controlling drug release remotely. In this review, we provide a literature review on the use of dual and multi-responsive chitosan-grafted-poly-(N-vinylcaprolactam) (CP) microgels in drug delivery and oncological applications.

2021 ◽  
Biswajit Roy ◽  
Rakesh Mengji ◽  
Samrat Roy ◽  
Bipul Pal ◽  
Avijit Jana ◽  

In recent times, organelle-targeted drug delivery systems gained tremendous attention due to the site specific delivery of active drug molecules resulting in enhanced bioefficacy. In this context, the phototriggered drug delivery system (DDS) for releasing an active molecule is superior as it provides spatial and temporal control over the release. So far, near infrared (NIR) light responsive organelle targeted DDS has not yet been developed. Hence, we introduced a two-photon NIR-light responsive lysosome targeted ʽAIE + ESIPTʼ active single component DDS based on naphthalene chromophore. The Two-photon absorption cross-section of our DDS is 142 GM at 850 nm. The DDS was converted into pure organic nanoparticles for biological applications. Our nano-DDS is capable of selective targeting, AIE-luminogenic imaging, and drug release within the lysosome. In vitro studies using cancerous cell lines showed that our single component photoresponsive nanocarrier exhibited enhanced cytotoxicity and real-time monitoring ability of the drug release.

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