scholarly journals Photoactivatable Surface-Functionalized Diatom Microalgae for Colorectal Cancer Targeted Delivery and Enhanced Cytotoxicity of Anticancer Complexes

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 480 ◽  
Author(s):  
Joachim Delasoie ◽  
Philippe Schiel ◽  
Sandra Vojnovic ◽  
Jasmina Nikodinovic-Runic ◽  
Fabio Zobi

Systemic toxicity and severe side effects are commonly associated with anticancer chemotherapies. New strategies based on enhanced drug selectivity and targeted delivery to cancer cells while leaving healthy tissue undamaged can reduce the global patient burden. Herein, we report the design, synthesis and characterization of a bio-inspired hybrid multifunctional drug delivery system based on diatom microalgae. The microalgae’s surface was chemically functionalized with hybrid vitamin B12-photoactivatable molecules and the materials further loaded with highly active rhenium(I) tricarbonyl anticancer complexes. The constructs showed enhanced adherence to colorectal cancer (CRC) cells and slow release of the chemotherapeutic drugs. The overall toxicity of the hybrid multifunctional drug delivery system was further enhanced by photoactivation of the microalgae surface. Depending on the construct and anticancer drug, a 2-fold increase in the cytotoxic efficacy of the drug was observed upon light irradiation. The use of this targeted drug delivery strategy, together with selective spatial–temporal light activation, may lead to lower effective concentration of anticancer drugs, thereby reducing medication doses, possible side effects and overall burden for the patient.

2020 ◽  
Author(s):  
Joachim Delasoie ◽  
Philippe Schiel ◽  
Sandra Vojnovic ◽  
Jasmina Nikodinovic-Runic ◽  
Fabio Zobi

Design, synthesis and characterization of a bio-inspired hybrid multifunctional drug delivery system based on diatom microalgae. The microalgae’s surface was chemically functionalized with hybrid vitamin B<sub>12</sub>-photoactivable molecules and the materials further loaded with highly active rhenium(I) tricarbonyl anticancer complexes. The constructs showed enhanced adherence to colorectal cancer (CRC) cells via transcobalamin (II) receptors and slow release of the chemotherapeutic drugs. The overall toxicity of the hybrid multifunctional drug delivery system was further enhanced by photoactivation of the microalgae surface. Depending on the construct and anticancer drug, a 2-fold increase in the cytotoxic efficacy of the drug was observed upon light irradiation.


2020 ◽  
Author(s):  
Joachim Delasoie ◽  
Philippe Schiel ◽  
Sandra Vojnovic ◽  
Jasmina Nikodinovic-Runic ◽  
Fabio Zobi

Design, synthesis and characterization of a bio-inspired hybrid multifunctional drug delivery system based on diatom microalgae. The microalgae’s surface was chemically functionalized with hybrid vitamin B<sub>12</sub>-photoactivable molecules and the materials further loaded with highly active rhenium(I) tricarbonyl anticancer complexes. The constructs showed enhanced adherence to colorectal cancer (CRC) cells via transcobalamin (II) receptors and slow release of the chemotherapeutic drugs. The overall toxicity of the hybrid multifunctional drug delivery system was further enhanced by photoactivation of the microalgae surface. Depending on the construct and anticancer drug, a 2-fold increase in the cytotoxic efficacy of the drug was observed upon light irradiation.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1412
Author(s):  
Murtada A. Oshi ◽  
Juho Lee ◽  
Jihyun Kim ◽  
Nurhasni Hasan ◽  
Eunok Im ◽  
...  

Cyclosporine A (CsA) is a potent immunosuppressant for treating ulcerative colitis (UC). However, owing to severe systemic side effects, CsA application in UC therapy remains limited. Herein, a colon-targeted drug delivery system consisting of CsA crystals (CsAc)-loaded, Eudragit S 100 (ES)-coated alginate microparticles (CsAc-EAMPs) was established to minimize systemic side effects and enhance the therapeutic efficacy of CsA. Homogeneously-sized CsAs (3.1 ± 0.9 μm) were prepared by anti-solvent precipitation, followed by the fabrication of 47.1 ± 6.5 μm-sized CsAc-EAMPs via ionic gelation and ES coating. CsAc-EAMPs exhibited a high drug loading capacity (48 ± 5%) and a CsA encapsulation efficacy of 77 ± 9%. The in vitro drug release study revealed that CsA release from CsAc-EAMPs was suppressed under conditions simulating the stomach and small intestine, resulting in minimized systemic absorption and side effects. Following exposure to the simulated colon conditions, along with ES dissolution and disintegration of alginate microparticles, CsA was released from CsAc-EAMPs, exhibiting a sustained-release profile for up to 24 h after administration. Given the effective colonic delivery of CsA molecules, CsAc-EAMPs conferred enhanced anti-inflammatory activity in mouse model of dextran sulfate sodium (DSS)-induced colitis. These findings suggest that CsAc-EAMPs is a promising drug delivery system for treating UC.


2021 ◽  
Vol 7 (2) ◽  
pp. 025-034
Author(s):  
Minakshee G. Nimbalwar ◽  
Bhushan R. Gudalwar ◽  
Wrushali A. Panchale ◽  
Ashish B. Wadekar ◽  
Jagdish V. Manwar ◽  
...  

Proniosomal drug delivery system is a stable provesicular system in nanotechnology to overcome the drawbacks associated with other vesicular systems. These are water-soluble pro-vesicular drug carriers coated with a non-ionic surfactant which on hydration give niosomes. The system is encapsulated and shows a systemic and targeted delivery of poorly soluble drugs with increased bioavailability and decreased side effects. Here we have covered characterizations and applications of the proniosomal drug delivery system.


2020 ◽  
Vol 8 (15) ◽  
pp. 4251-4265 ◽  
Author(s):  
Ram Pada Das ◽  
Beena Gobind Singh ◽  
Amit Kunwar

The study demonstrates the importance of the weight ratio of F127 and gelatin in forming size selective nanoconjugate through a thermal relaxation approach and its potential as an efficient drug delivery system of doxorubicin with reduced side effects.


2021 ◽  
Vol Volume 15 ◽  
pp. 557-576
Author(s):  
Hua-Feng Yin ◽  
Chun-Ming Yin ◽  
Ting Ouyang ◽  
Shu-Ding Sun ◽  
Wei-Guo Chen ◽  
...  

2013 ◽  
Vol 59 (5) ◽  
pp. 585-590 ◽  
Author(s):  
M.A. Sanzhakov ◽  
V.N. Prozorovskyi ◽  
O.M. Ipatova ◽  
E.G. Tikhonova ◽  
N.V. Medvedeva ◽  
...  

Low bioavailability of rifampicin, one of the main antituberculous drug, stimulates searches of its new optimized formulations. The present study has showen possibility of rifampicin embedding into nanoparticles from plant phosphatidylcholine (diameter of 20-30 nm). Addition of sodium oleate to the phospholipid system caused a 2-fold increase of the percent of rifampicin incorporation. After oral administration to rats, the maximal drug observed in plasma one hour after was 0.5 and 4.2 mkg/ml for free rifampicin for rifampicin in phospholipids-oleate nanoparticles, respectively. These levels were maintained for more than two hours of the experiment. High rifampicin bioavailability in the oleate containing phospholipid nanosystem suggests prospectivity of its pharmaceutical elaboration.


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