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Appl Biochem Biotechnol ; 167(5): 1365-76, 2012 Jul.
Article in English | MEDLINE | ID: mdl-22415787

ABSTRACT

Pectins (Pec) of 33 to 74 % esterification degree were tested with doxorubicin (Dox), a very high toxic drug widely used in cancer therapies. Pec with 35 and 55 % DE were selected because of the Dox binding higher than Pec microspheres of 35 and 55 % obtained by ionotropic gelation with Ca⁺² have 88 and 66 % Dox loading capacity. Kinetic Dox release showed more than 80.0 and about 30.0 % free drug from 35 % and 55 % Pec formulations at pH 7.4, and 37 °C after 1-h incubation, respectively. Besides, Dox release decrease to 12 % in 55 % Pec microsphere formulation after 1-year storage at 4 °C. FTIR analysis of Pec-Dox complex showed hipsochromic shifts for the σ(C=O), δ(N-H) and σ(C-C) vibrational modes compared to Dox spectrum suggesting strong interaction between the drug cargo and the matrix. Rheological studies of Pec and Pec-Dox samples flow behavior exhibited a shear-thinning nature. Fifty-five percent of Pec showed higher viscosity than the viscosity for 35 % Pec in all range of temperatures analyzed, and decreased when the temperature is raised. Besides, Pec-Dox complexes have higher viscosity values than those of the corresponding Pec samples, and viscosity curves as function of shear rate for 35 % Pec-Dox are above the curves of 55 % Pec-Dox. In both cases, the results are confirming significant interaction between the cargo and the matrix, which also was established in viscoelastic dynamic analysis.


Subject(s)
Antineoplastic Agents/chemistry , Doxorubicin/chemistry , Drug Carriers/chemistry , Hydrogels/chemistry , Pectins/chemistry , Administration, Oral , Antineoplastic Agents/administration & dosage , Antineoplastic Agents/metabolism , Capsules , Doxorubicin/administration & dosage , Doxorubicin/metabolism , Kinetics , Microspheres , Rheology
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