title: Preparation and evaluation of lidocaine hydrochloride in cyclodextrin inclusion complexes for development of stable gel in association with chlorhexidine gluconate for urogenital use.
abstract: Inclusions of lidocaine hydrochloride in cyclodextrins were prepared to obtain stable complexes compatible for association with chlorhexidine in a new gel formulation for use in urogenital applications. Two cyclodextrins, β-cyclodextrin and methyl-β-cyclodextrin, were used for encapsulating lidocaine hydrochloride through solubilization and kneading techniques. The lidocaine-cyclodextrin complexes were characterized by ultraviolet spectroscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. The results revealed that the techniques generated good yields of inclusion products that maintained the functional properties of lidocaine. In addition, the inclusion products obtained improved the compatibility of lidocaine hydrochloride with chlorhexidine in solution and a gel formulation. The gel formulation displayed desirable rheological and physicochemical properties. The results presented here are the first description of the inclusion of lidocaine with cyclodextrins, which improves compatibility with chlorhexidine in formulations for simultaneous delivery.
authors.affiliation: Departamento de Medicamentos, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
authors.forename: Luiz Francisco Jones
authors.initials: LF
authors.lastname: Soares da Silva
authors.forename: Flavia Almada
authors.initials: FA
authors.lastname: do Carmo
authors.forename: Vinicius Raphael
authors.initials: VR
authors.lastname: de Almeida Borges
authors.forename: Lidiane Mota
authors.initials: LM
authors.lastname: Monteiro
authors.forename: Carlos Rangel
authors.initials: CR
authors.lastname: Rodrigues
authors.forename: Lúcio Mendes
authors.initials: LM
authors.lastname: Cabral
authors.forename: Valeria Pereira
authors.initials: VP
authors.lastname: de Sousa
mesh_terms: D000704:Analysis of Variance; D002710:Chlorhexidine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D003505:Cyclodextrins / Q000737:chemistry*; D004355:Drug Stability; D055119:Elastic Modulus; D005782:Gels / Q000737:chemistry*; D008012:Lidocaine / Q000737:chemistry* / Q000493:pharmacokinetics; D016014:Linear Models; D008954:Models, Biological; D015203:Reproducibility of Results; D014622:Vaginal Creams, Foams, and Jellies / Q000737:chemistry; D014783:Viscosity
chemical_list: D003505:Cyclodextrins; D005782:Gels; D014622:Vaginal Creams, Foams, and Jellies; D008012:Lidocaine; C010882:chlorhexidine gluconate; D002710:Chlorhexidine