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Hyaluronic acid funcionalizated-liposomes for abiraterone incorporation: development, characterization and stability study

Grant number: 19/26044-0
Support type:Scholarships in Brazil - Scientific Initiation
Effective date (Start): July 01, 2020
Effective date (End): August 31, 2021
Field of knowledge:Health Sciences - Pharmacy - Pharmaceutical Technology
Principal researcher:Maria Palmira Daflon Gremião
Grantee:Felipe Tita de Lima
Home Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

Prostate cancer is one of the neoplasms that most affects the male population in Brazil and worldwide, which classifies it a serious public health problem. Abiraterone stands out among the most promising antineoplastics drugs due to its efficacy and control of adverse effects compared to other agents. However, despite numerous clinical advantages, abiraterone, like other chemotherapeutic agents, has low water solubility, toxicity and does not act exclusively on neoplastic cells, which results in a significant range of adverse effects for patients. However, toxicity induced by abiraterone treatment is a problem that can be minimized by incorporating the drug into nanostructured systems, as these systems have the ability to deliver the drug directly to the target site, both passively (by the effect of increased permeability and retention) and actively (through surface vectorization with site specific ligands). Among these systems, liposomes stand out as one of the most consolidated nanocarriers, as they have great capacity to encapsulate both hydrophilic and lipophilic drugs (such as abiraterone). One of the possibilities of conjugation is hyaluronic acid, since this molecule is the natural ligand of the CD44 receptor, overexpressed in prostate cancer cells. Thus, hyaluronic acid anchored to the carrier surface would bind specifically to the CD44 target receptor, releasing abiraterone selectively, sparing healthy cells. This work aims to characterize the systems by particle size, polydispersity index, zeta potential, abiraterone encapsulation efficiency and infrared spectroscopy. Additionally, the efficiency of conjugation of hyaluronic acid to liposomes will be evaluated by nuclear magnetic resonance, as well as the morphological analysis of these systems will be observed by transmission electron microscopy.

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