scholarly journals Biodegradable magnetic microspheres for drug targeting, temperature controlled drug release, and hyperthermia

2019 ◽  
Vol 5 (1) ◽  
pp. 161-164 ◽  
Author(s):  
Diana Zahn ◽  
Andreas Weidner ◽  
Katayoun Saatchi ◽  
Urs O. Häfeli ◽  
Silvio Dutz

AbstractMagnetic microspheres (MMS) used for magnetic drug targeting consist of magnetic nanoparticles (MNP) and a pharmaceutical agent embedded in a polymeric matrix material. The application of MNP for drug targeting enables guiding the MMS to a target area, imaging the position of the MMS with magnetic particle imaging, and finally inducing drug release. As latter takes place by degradation of the MMS or diffusion through the matrix, an increase in temperature, e.g. through magnetic hyperthermia, leads to an accelerated drug release. Here, MMS consisting of poly(lactic-coglycolic) acid (PLGA) with different monomer ratios were prepared by an oil-in-water emulsion evaporation method. The model drug Camptothecin (CPT) and magnetic multicore nanoparticles (MCNP) with a high specific heating rate were embedded into the microspheres. We obtained MMS in the preferred size range of 1 to 2 μm with a concentration of MCNP of 16wt%, a drug load of about 0.5wt% and an excellent heating performance of 161 W/gMMS. Investigations of the drug release behaviour showed an accelerated drug release when increasing the temperature from 20 °C to 37 °C or 43 °C by using a water bath. In addition, an increase in drug release of about 50% through magnetic heating of the MMS up to 44 °C compared to 37 °C was observed. By this, a magnetic hyperthermia induced CPT release from PLGA MMS is demonstrated for the very first time.

2015 ◽  
Vol 380 ◽  
pp. 285-294 ◽  
Author(s):  
Prabu Chakkarapani ◽  
Latha Subbiah ◽  
Selvamani Palanisamy ◽  
Arputha Bibiana ◽  
Fredrik Ahrentorp ◽  
...  

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Joseph C. Bear ◽  
P. Stephen Patrick ◽  
Alfred Casson ◽  
Paul Southern ◽  
Fang-Yu Lin ◽  
...  

RSC Advances ◽  
2015 ◽  
Vol 5 (29) ◽  
pp. 22365-22372 ◽  
Author(s):  
Yufang Zhu ◽  
Cuilian Tao

DNA-capped Fe3O4/SiO2 magnetic mesoporous silica (MMS) nanoparticles were developed for potential temperature controlled drug release and magnetic hyperthermia.


Pharmacology ◽  
2020 ◽  
Vol 105 (9-10) ◽  
pp. 541-549 ◽  
Author(s):  
Ahmed S. Ali ◽  
Abid A. Altayari ◽  
Lateef M. Khan ◽  
Sameer E. Alharthi ◽  
Osama A. Ahmed ◽  
...  

<b><i>Background/Aims:</i></b> Inflammatory bowel disease is a chronic or remitting/relapsing intestinal inflammation, which comprises Crohn’s disease and ulcerative colitis (UC). Severe UC is a life-threatening condition that requires corticosteroids (CS) as a first-line rescue therapy. Some patients are refractory to CS and may require alternative immunosuppressive therapy. Oral tacrolimus (FK506), an immunosuppressive agent, has been reported to be effective in the management of severe refractory UC, but it can cause serious adverse effects. This work aims to study the effect of tacrolimus delivered by a colon-targeted delivery system (CTDS) in a dextran sulfate sodium (DSS)-induced animal model of colitis. <b><i>Materials and Methods:</i></b> We developed and evaluated an oral CTDS of tacrolimus (FK506) loaded pH-dependent polymeric microspheres, composed of Eudragit® S100 as a pH-sensitive polymer using the oil-in-water emulsion method. The physicochemical properties and drug release profiles of these microparticles in gastrointestinal tract (GIT) conditions were examined. A DSS-induced colitis rat model was used to evaluate the potential remedial and in vivo distribution of microspheres. <b><i>Results:</i></b> The pH-microspheres prevented a burst drug release in acidic pH conditions and showed sustained release at a colonic pH. The in vivo distribution study in the rat GIT demonstrated that pH-microspheres were successfully delivered to the inflamed colon. Moreover, it also demonstrated a significant decrease of disease activity and expression of proinflammatory cytokines, such as tumor necrosis factor α, interleukin-1β (IL-1β), and IL-6, and minimized the histological and morphometric changes. <b><i>Conclusion:</i></b> The results confirmed the efficacy of tacrolimus (FK506) CTDs in the management of DSS-induced colitis.


Processes ◽  
2019 ◽  
Vol 7 (6) ◽  
pp. 365 ◽  
Author(s):  
Mine Diril ◽  
Yesim Karasulu ◽  
Miltiadis Toskas ◽  
Ioannis Nikolakakis

Self-emulsifying pellets (SEPs) of Atorvastatin Calcium (AtrCa) were developed and processed into tablets (SETs). Self-emulsifying drug delivery system (SEDDS) composed of oleic acid, Tween 20, Span 80 and N-Methyl-2-pyrolidone gave great solubility improvement and was used as oil in water emulsion for the preparation of SEPs. Due to the high 60% w/w SEDDS content required to achieve a therapeutic dose in the final tablet form, sonication was necessary to improve fluidity and stability. Colloidal silicon dioxide (CSD) and microcrystalline cellulose (MCC) were the solids in the pellet formulation employed at a ratio 7:3, which enabled production of pellets with high SEDDS content and acceptable friability as well. Emulsions were characterized physico-chemically, SEPs for physical properties and reconstitution, and tablets of compressed pellets for mechanical strength, disintegration into pellets and drug release. SEPs compressed with 30% MCC at 60 MPa gave tablets of adequate strength that disintegrated rapidly into pellets within 1 min. Emulsion reconstitution took longer than drug release due to adsorption of SEDDS on CSD, implying dissolution at the pellet surface in parallel to that from the dispersed droplets. Compared to the commercial tablet, drug release from the self-emulsifying forms was faster at pH 1.2 where the drug solubility is poor, but slower at pH 6.8 where the solubility is higher. Permeability and cytotoxicity were also studied using Caco-2 cells. The results showed that drug transport from the apical to basolateral compartment of the test well was 1.27 times greater for SEPs than commercial tablets, but 0.86 times lower in the opposite direction. Statistical analysis confirmed the significance of these results. Toxicity was slightly reduced. Therefore, the increased permeability in conjunction with the protection of the drug being dissolved in the SEDDS droplets, may reduce the overall effect of presystemic metabolism and enhance bioavailability.


2020 ◽  
Vol 21 (10) ◽  
pp. 3641 ◽  
Author(s):  
Beatriz D. Cardoso ◽  
Ana Rita O. Rodrigues ◽  
Bernardo G. Almeida ◽  
Carlos O. Amorim ◽  
Vítor S. Amaral ◽  
...  

Despite the promising pharmacological properties of curcumin, the transport and effective release of curcumin is still a challenge. The advances in functionalized nanocarriers for curcumin have also been motivated by the anticancer activity of this natural compound, aiming at targeted therapies. Here, stealth (aqueous and solid) magnetoliposomes containing calcium-substituted magnesium ferrite nanoparticles, CaxMg1−xFe2O4 (with x = 0.25, 0.50, 0.75) were developed as nanocarriers for curcumin. The magnetic nanoparticles exhibit superparamagnetic properties and crystalline structure, with sizes below 10 nm. The magnetoliposomes based on these nanoparticles have hydrodynamic diameters around or below 150 nm and a low polydispersity. The influence of an alternating magnetic field (AMF) on drug release over time was evaluated and compared with curcumin release by diffusion. The results suggest the potential of drug-loaded magnetoliposomes as nanocarriers that can be magnetically guided to the tumor sites and act as agents for a synergistic effect combining magnetic hyperthermia and controlled drug release.


2009 ◽  
Vol 151 ◽  
pp. 159-165 ◽  
Author(s):  
Shahin Bonakdar ◽  
Seyed Ali Poursamar ◽  
Mohammad Rafienia ◽  
Mohammad A. Shokrgozar ◽  
Afshin Farhadi ◽  
...  

Betamethasone acetate (BA) is a glucocorticoid steroid with anti-inflammatory and immunosuppressive properties which can be used in treatment of asthma and itching. In this research, polyvinyl alcohol nanospheres loaded by betamethasone acetate were prepared by oil in water emulsion method after which they were exposed to 1, 2 and 4 cycles of freeze-thawing (F-T) process including 24 hours freezing cycle at -25 °C and 24 hours thawing at ambient temperature. Nanospheres fabrication was confirmed by transmission electron microscopy and betamethasone release was analyzed by UV spectrophotometer at 245 nm. The results revealed that by increasing the number of F-T cycles the rate of drug release decreased. The effect of BA concentration was also investigated on human chondrosarcoma (sw 1353). The MTT assay was utilized to assess the cell proliferation. The results showed that these biocompatible nanospheres can be used for sustained release of such drugs for more than four months and drug release rate can be effectively controlled by implementing F-T cycles.


2021 ◽  
Vol 2 (1) ◽  
pp. 51-60
Author(s):  
Mostafa Yusefi ◽  
Kamyar Shameli ◽  
Siti Nur Amalina Mohamad Sukri

The activation of MNPs for hyperthermia therapy via an external alternating magnetic field is an interesting method in targeted cancer therapy. This mini-review explains new developments and implications of magnetic nanofluids mediated magnetic hyperthermia for their potential use in future clinical settings. The external alternating magnetic field generates heat in the tumor area to eliminate cancer cells. Depending on the tumor type and targeted area, several kinds of MNPs with different coating agents of various morphology and surface charge have been developed. The tunable physiochemical characteristics of MNPs enhance their heating capability. In addition, heating efficiency is strongly associated with the amount of the applied magnetic field and frequency. The great efforts have offered promising preclinical trials of magnetic hyperthermia via MNPs as a smart nanoagent. MNPs are very appropriate to be considered as a heating source in MHT and prospective research in this field will lead to tackle the problems from chemotherapy and introduce promising therapeutic techniques and nanodrug formulations for remotely controlled drug release and anticancer effects. This mini-review aims to pinpoint synthesis and structural analysis of various magnetic nanoparticles examined for magnetic hyperthermia therapy and controlled drug release in cancer treatment.


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