Development of mucoadhesives solid dispersion and polymeric nanoparticles of zidovudine and biological interaction evaluation with intestnal mucosa

• Grant number: 13/01670-0
• Support type: Scholarships in Brazil - Doctorate
• Effective date (Start): December 01, 2013
• Effective date (End): July 30, 2015
• Field of knowledge: Health Sciences - Pharmacy - Pharmaceutical Technology
• Principal researcher: Maria Palmira Daflon Gremião
• Grantee: Liliane Neves Pedreiro
• Home Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
• Associated scholarship(s): 14/08044-0 - Bioavailability and pharmacokinetics of zidovudine mucoadhesive solid dispersions and polymeric nanoparticles in rats, BE.EP.DR

Abstract

Zidovudine, azidothymidine (AZT) is the drug most used alone or in combination with other antiretroviral agents for the treatment of AIDS (Acquired Immunodeficiency Syndrome), caused by HIV (human immunodeficiency virus). The low bioavailability of AZT is the major challenge to be overcome to optimize their performance on oral therapy, since its high rate of hepatic metabolism and low permeability result in the need for administration of high doses of the drug, which often achieve plasma levels toxic causing serious adverse effects and, moreover, is still substrate efflux mechanism mediated by P-glycoprotein in the gut. Solid dispersions are an important technological strategy for improving the effectiveness of drugs, therapeutic alternatives constituting pharmacologically more efficient. Already nanoparticles are small solid particles which aim to delivery of low doses of potent drugs, reduced drug concentration in sites other than the target organ or tissue and protect labile compounds before and after administration, to exert its pharmacological action. In oral administration, the small size of the nanoparticles favors gastrointestinal absorption of the drug by improving its bioavailability. Depending on the polymer used in the preparation of the nanoparticles, they may also have mucoadhesive properties. In addition, drug delivery systems with mucoadhesive properties allow intimate contact of the drug with the mucosa and increase its residence time at a specific site can improve the bioavailability of drugs by being able to keep the drug for longer in contact with the intestinal mucosa. This project proposes the development of solid dispersions and polymeric nanoparticles for zidovudine release and therefore, the evaluation and comparison of the mode of absorption of the drug from these systems, and biological interaction with the intestinal mucosa.

Academic Publications

(References retrieved automatically from State of São Paulo Research Institutions)

PEDREIRO, Liliane Neves. Extratos padronizados para o tratamento de doenças crônicas : Serjania marginata Casar. (Sapindaceae). 2015. Doctoral Thesis - Universidade Estadual Paulista "Júlio de Mesquita Filho" Faculdade de Ciências Farmacêuticas..