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Characterization of lidocaine:hydroxypropyl-β-cyclodextrin inclusion complex
Authors:Carolina Morales Moraes  Priscila Abrami  Daniele Riberio de Araujo  Angélica F. A. Braga  Michelle Georges Issa  Humberto G. Ferraz  Eneida de Paula  Leonardo Fernandes Fraceto
Affiliation:1. Departamento de Farmácia, Universidade de Sorocaba, Rod. Raposo Tavares, km 92,5 CEP, Sorocaba, SP, 18023-000, Brazil
2. Departamento de Bioquímica, Instituto de Biologia, Universidade Estadual de Campinas (UNICAMP), Campinas, SP, Brazil
3. Departamento de Anestesiologia, F.C. Médicas, UNICAMP, Campinas, SP, Brazil
4. Departamento de Farmácia, F.C. Farmacêuticas, Universidade de S?o Paulo (USP), Sao Paulo, SP, Brazil
Abstract:An inclusion complex was prepared between the local anesthetic lidocaine (LDC) and hydroxypropyl-β-CD (HP-β-CD). The complex was characterized by thermal analysis (differential scanning calorimetry, DSC), UV absorption and high-pressure liquid chromatography (HPLC). DSC results were indicative of complexation, due to the loss of the characteristic endothermic peak of LDC (77 °C). Phase-solubility diagrams allowed the determination of the association constant between LDC and HP-β-CD (35.7 ± 4.7 M−1). The rate of LDC release decreased after complexation and thermodynamic parameters from the HPLC studies (ΔG° = −2.65 kJ/mol) revealed that a stable complex was formed.
Keywords:Lidocaine  HP-β  -CD  HPLC  Association constant  Thermodynamic parameters
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