Development of a new ex vivo method for the assessment of drug intestinal permeability using frog intestinal epithelium (Rana catesbeiana)

• Grant number: 10/17240-6
• Support Opportunities: Regular Research Grants
• Start date: March 01, 2011
• End date: February 28, 2013
• Field of knowledge: Health Sciences - Pharmacy - Pharmaceutical Technology
• Principal Investigator: Vladi Olga Consiglieri
• Grantee: Vladi Olga Consiglieri
• Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil
• Associated researchers: Guilherme Diniz Tavares ; María Segunda Aurora Prado ; Talita Ferreira Monteiro ; Telma Mary Kaneko

Abstract

Effective treatment depends on the bioavailability of drugs, this feature related to the properties of permeability and solubility. The biopharmaceutical classification (SCB), based on these parameters, was proposed as a tool for the development of dosage forms, in order to assist in predicting the availability in vivo, since there are technical limitations, economic and ethical issues in clinical direct bioavailability. Thus, the evaluation of permeability and solubility of drugs, although indirectly, provides objective information about drug efficacy, and supplies easily reproducible models without exposing healthy volunteers to risks. Studies of in vitro/ex vivo permeability can be achieved through different techniques. However, there is a lack of standardized protocols, and many available data in the literature regarding this property are not reliable or conclusive. Thus, the aim of this is to propose a new ex vivo model of studying drug permeability using intestinal epithelium of Rana catesbeiana in Franz cells. Zidovudine, lamivudine, and acyclovir were selected as model drugs. The amount of drug permeated will be determined by the method of capillary electrophoresis equipped with detector diode array. The permeation parameters that should be determined are: cumulative amount of permeate drug, apparent permeability coefficient, absorption rate constant and permeability rate. These will be correlated to bioavailability data from previous studies. ANOVA and Tukey tests should be used to the evaluation of these results. (AU)