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Development of solid formulations and entrapment of poor soluble active ingredients for topical and systemic applications

Grant number: 15/19651-7
Support type:Regular Research Grants
Duration: May 01, 2016 - June 30, 2018
Field of knowledge:Engineering - Chemical Engineering
Principal Investigator:Simone de Fátima Medeiros Sampaio
Grantee:Simone de Fátima Medeiros Sampaio
Home Institution: Escola de Engenharia de Lorena (EEL). Universidade de São Paulo (USP). Lorena , SP, Brazil
Assoc. researchers:Amilton Martins dos Santos ; Nicole Raymonde Demarquette
Associated grant(s):17/50126-1 - Triggered micelles for enhanced integration of chemotherapy and photodynamic therapy, AP.R SPRINT
Associated scholarship(s):18/05306-4 - Development of solid formulations and encapsulation of hydrophobic active principles for topical and systemic application, BP.TT


The developing of new carrier systems for active ingredients aim to modify the limiting physicochemical properties of drugs, improving thereby its pharmacodynamic (therapeutic effect potentiation), pharmacokinetics (control of the absorption and distribution on tissues) and reducing their toxic effects (local and systemic toxicity). The modification of the permeability and solubility of an active ingredient is a crucial factor to improve its administration and increase their bioavailability. In this context, the main objective of this project is to prepare solid formulations, from biocompatible and biodegradable polymers, to favor the administration and prolong the release of poor water soluble active ingredients. In a first step, micro and nanoparticles as well as nanofibers will be produced from homopolymers and polymer blends, via spray drying technique and electrospinning process. Then the incorporation of different hydrophobic active ingredients in the polymer matrices and their in vitro kinetics release will be carefully evaluated. Cytotoxicity assays will be performed to the formulations prepared during the developing of this project. It is expected with the implementation of this project, to develop materials capable of increasing the bioavailability and modify the pharmacokinetics of hydrophobic drugs for topical and systemic release. Studies carried out in this project will contribute to an advance in terms of synthesis and knowledge of the properties of new materials with potential for future applications in manufacturing various drug systems, aimed to reduce the number of doses required for a given treatment, the occurrence of side effects and, consequently, to increase the patient compliance. (AU)