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Crystalline-phase nano cubosome functionalized with biopolymers: development as a drug carrier and in vivo studies in zebrafish (Danio rerio)

Grant number: 21/00971-2
Support Opportunities:Regular Research Grants
Duration: July 01, 2021 - December 31, 2023
Field of knowledge:Biological Sciences - Biophysics - Biophysics of Processes and Systems
Principal Investigator:Omar Mertins
Grantee:Omar Mertins
Host Institution: Escola Paulista de Medicina (EPM). Universidade Federal de São Paulo (UNIFESP). Campus São Paulo. São Paulo , SP, Brazil
Associated researchers: Angelina Angelova ; Karin Do Amaral Riske ; Patrick Mathews Delgado ; Rumiana Dimova ; Watson Loh
Associated grant(s):22/13397-5 - Functionalized cubosome as bioactive delivery system for oral application, AP.R SPRINT


The efficient oral administration of drugs and bioactive substances, especially anti-cancer agents, represents a scientific and technological challenge due to the resulting low bioavailability. To overcome this challenge, nano-structured and functionalized materials such as systems for carrying and controlled release represent technology of high interest. In this proposal, we will develop a nano-particulated and bioconjugated carrier with lipid and biocompatible polysaccharides as a material with a high capacity for encapsulating bioactives due to its internal structure of crystalline topology. Bioconjugate nano cubosomes will have a pH-responsive property in order to optimize structural characteristics with the oral administration route and thus favor intestinal mucus adhesion to provide the release of carried drug directly into the intestinal mucosa and thus favor their absorption. The proposal intends to move forward on two fronts. Initially, the production and characterization of the functionalized cubosome with internal crystalline structure will be extensively studied by modern physicochemical techniques to optimize the structure. Then, the characteristics of drug encapsulation and release and the physical interaction with a biological membrane model will be studied. In parallel, the aim is to test the functionalized cubosomes in vivo through oral administration in zebrafish. Histological, hematological and immunofluorescence studies will be carried out to assess the potential application of the material as a carrier of drugs and bioactive agents for oral administration. (AU)

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Scientific publications (4)
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
MATHEWS, PATRICK D.; MERTINS, OMAR; ANGELOV, BORISLAV; ANGELOVA, ANGELINA. Cubosomal lipid nanoassemblies with pH-sensitive shells created by biopolymer complexes: A synchrotron SAXS study. Journal of Colloid and Interface Science, v. 607, n. 1, p. 440-451, . (19/13147-6, 21/00971-2, 18/21727-0)
RAMIREZ, CARLOS A. B.; CARRIERO, MATEUS M.; LEOMIL, FERNANDA S. C.; DE SOUSA, RICARDO MORO L.; DE MIRANDA, ANTONIO; MERTINS, OMAR; MATHEWS, PATRICK D.. Complexation of a Polypeptide-Polyelectrolytes Bioparticle as a Biomaterial of Antibacterial Activity. PHARMACEUTICS, v. 14, n. 12, p. 15-pg., . (21/00971-2)
PIMENTA, BARBARA V.; MADRID, RAFAEL R. M.; MATHEWS, PATRICK D.; RISKE, KARIN A.; LOH, WATSON; ANGELOV, BORISLAV; ANGELOVA, ANGELINA; MERTINS, OMAR. Interaction of polyelectrolyte-shell cubosomes with serum albumin for triggering drug release in gastrointestinal cancer. JOURNAL OF MATERIALS CHEMISTRY B, v. 11, n. 11, p. 14-pg., . (21/00971-2, 16/13368-4)
RAMIREZ, CARLOS A. B.; MATHEWS, PATRICK D.; MADRID, RAFAEL R. M.; GARCIA, IRENE T. S.; RIGONI, VERA L. S.; MERTINS, OMAR. Antibacterial polypeptide-bioparticle for oral administration: Powder formulation, palatability and in vivo toxicity approach. BIOMATERIALS ADVANCES, v. 153, p. 15-pg., . (21/00971-2, 15/23948-5)

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