scholarly journals Co-Loading of Temozolomide and Curcumin into a Calix[4]arene-Based Nanocontainer for Potential Combined Chemotherapy: Binding Features, Enhanced Drug Solubility and Stability in Aqueous Medium

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2930
Author(s):  
Rossella Migliore ◽  
Nicola D’Antona ◽  
Carmelo Sgarlata ◽  
Grazia M. L. Consoli
Keyword(s):  
Isothermal Titration Calorimetry ◽  
Anticancer Drugs ◽  
Drug Loading ◽  
Building Blocks ◽  
Critical Micellar Concentration ◽  
Titration Calorimetry ◽  
Drug Solubility ◽  
New Paradigm ◽  
Drug Combination Therapy ◽  
Low Solubility

The co-delivery of anticancer drugs into tumor cells by a nanocarrier may provide a new paradigm in chemotherapy. Temozolomide and curcumin are anticancer drugs with a synergistic effect in the treatment of multiform glioblastoma. In this study, the entrapment and co-entrapment of temozolomide and curcumin in a p-sulfonato-calix[4]arene nanoparticle was investigated by NMR spectroscopy, UV-vis spectrophotometry, isothermal titration calorimetry, and dynamic light scattering. Critical micellar concentration, nanoparticle size, zeta potential, drug loading percentage, and thermodynamic parameters were all consistent with a drug delivery system. Our data showed that temozolomide is hosted in the cavity of the calix[4]arene building blocks while curcumin is entrapped within the nanoparticle. Isothermal titration calorimetry evidenced that drug complexation and entrapment are entropy driven processes. The loading in the calixarene-based nanocontainer enhanced the solubility and half-life of both drugs, whose medicinal efficacy is affected by low solubility and rapid degradation. The calixarene-based nanocontainer appears to be a promising new candidate for nanocarrier-based drug combination therapy for glioblastoma.

scholarly journals COMPARATIVE EVALUATION OF THE RELEASE PROPERTIES OF VERAPAMIL HCL AND CARBAMAZEPINE FROM MICROCRYSTALLINE CELLULOSE II PELLETS

2017 ◽  
Vol 9 (10) ◽  
pp. 182
Author(s):  
John Rojas ◽  
David Correa
Keyword(s):  
Microcrystalline Cellulose ◽  
Drug Loading ◽  
Product Yield ◽  
Immediate Release ◽  
Cellulose Ii ◽  
Drug Solubility ◽  
Microscopy Analysis ◽  
Pelletization Aid ◽  
Verapamil Hcl ◽  
Low Solubility

Objective: To study microcrystalline cellulose II (MCCII) as new pelletization aid for a high and low solubility drugs such as verapamil. HCl and carbamazepine, respectively.Methods: Approximately, 30 g of MCCII and drug mixtures were hydrated passed through a # 20 mesh sieved and spheronizated at a frequency of 6 Hz and residence time of 480 s. A microscopy analysis was used to evaluate the shape and size descriptors. Pellets properties such as compressibility, friability, density, flowability and product yield were also evaluated. Drug release properties were tested according to the USP specifications and compared to those of MCCI.Results: The wetting level of the excipients depended on drug loading and drug solubility. Thus, a high drug loading (>50%) rendered pellets having a low yield, flowability and caused a detriment on size descriptors. Likewise, the regular morphology and strength of MCCII-based pellets was highly affected by increasing drug loads. Verapamil. HCl pellets were less friable and compressible and showed better flowability than carbamazepine pellets. Regardless of drug loading and drug solubility, MCCII-based pellets released more than 80% of verapamil. HCl within 10 min, whereas released more than 75% of carbamazepine within 15 min. Conversely, MCCI pellets had a satisfactory verapamil. HCl release, but ~30% carbamazepine release within 1h.Conclusion: MCCII proved to be a better excipient than MCCI to yield beads having optimal pellet characteristics and rendered an immediate release profile for verapamil. HCl and carbamazepine.

Present trends in the encapsulation of anticancer drugs

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Xavier Montané ◽  
Karolina Matulewicz ◽  
Karolina Balik ◽  
Paulina Modrakowska ◽  
Marcin Łuczak ◽  
...  
Keyword(s):  
Carbon Nanotubes ◽  
Drug Toxicity ◽  
Recent Progress ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
The Body ◽  
Inorganic Nanoparticles ◽  
Hybrid Nanoparticles ◽  
Traditional Medicines ◽  
Low Solubility

Abstract Different nanomedicine devices that were developed during the recent years can be suitable candidates for their application in the treatment of various deadly diseases such as cancer. From all the explored devices, the nanoencapsulation of several anticancer medicines is a very promising approach to overcome some drawbacks of traditional medicines: administered dose of the drugs, drug toxicity, low solubility of drugs, uncontrolled drug delivery, resistance offered by the physiological barriers in the body to drugs, among others. In this chapter, the most important and recent progress in the encapsulation of anticancer medicines is examined: methods of preparation of distinct nanoparticles (inorganic nanoparticles, dendrimers, biopolymeric nanoparticles, polymeric micelles, liposomes, polymersomes, carbon nanotubes, quantum dots, and hybrid nanoparticles), drug loading and drug release mechanisms. Furthermore, the possible applications in cancer prevention, diagnosis, and cancer therapy of some of these nanoparticles have been highlighted.

scholarly journals Thermodynamic characterization of calcium-milk protein interaction by isothermal titration calorimetry

2009 ◽  
Vol 89 (3-4) ◽  
pp. 257-267 ◽  
Author(s):  
Latha-Selvi Canabady-Rochelle ◽  
Christian Sanchez ◽  
Michel Mellema ◽  
Sylvie Banon
Keyword(s):  
Isothermal Titration Calorimetry ◽  
Protein Interaction ◽  
Milk Protein ◽  
Titration Calorimetry ◽  
Thermodynamic Characterization
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