Didanosine-loaded chitosan microspheres optimized by surface-response methodology: A modified "Maximum Likelihood Classification'' approach formulation for reverse transcriptase inhibitors

Author(s)

da Silva, Classius Ferreira ; Severino, Patricia ; Martins, Fernanda ; Santana, Maria Helena A. ; Souto, Eliana B.

• Document type: Journal article
• Source: BIOMEDICINE & PHARMACOTHERAPY; v. 70, p. 7-pg., 2015-03-01.

Abstract

Didanosine-loaded chitosan microspheres were developed applying a surface-response methodology and using a modified Maximum Likelihood Classification. The operational conditions were optimized with the aim of maintaining the active form of didanosine (ddI), which is sensitive to acid pH, and to develop a modified and mucoadhesive formulation. The loading of the drug within the chitosan microspheres was carried out by ionotropic gelation technique with sodium tripolyphosphate (TPP) as cross-linking agent and magnesium hydroxide (Mg(OH)(2)) to assure the stability of ddI. The optimization conditions were set using a surface-response methodology and applying the "Maximum Likelihood Classification'', where the initial chitosan concentration, TPP and ddI concentration were set as the independent variables. The maximum ddI-loaded in microspheres (i.e. 1433 mg of ddI/g chitosan), was obtained with 2% (w/v) chitosan and 10% TPP. The microspheres depicted an average diameter of 11.42 mu m and ddI was gradually released during 2 h in simulated enteric fluid. (C) 2015 Elsevier Masson SAS. All rights reserved. (AU)

• FAPESP's process: 08/00421-8 - Incorporation and immunological evaluation of tumor antigens incorporated in solid lipid nanoparticles and solid lipid nanocarriers
• Grantee: Patricia Severino
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 11/20801-2 - Polymixin B load in solid lipid nanoparticles for incorporation in mucoadhesive hydrogels for oral mucositis treatment
• Grantee: Patricia Severino
• Support Opportunities: Scholarships in Brazil - Post-Doctoral