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
• Start date: July 01, 2021
• End date: 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
• City of the host institution: São Paulo
• Associated researchers: Angelina Angelova ; Karin Do Amaral Riske ; Patrick Mathews Delgado ; Rumiana Dimova ; Watson Loh
• Associated research grant(s): 24/00718-3 - 13th International Colloids Conference, AR.EXT; 22/13397-5 - Functionalized cubosome as bioactive delivery system for oral application, AP.R SPRINT

Abstract

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)

Scientific publications

(7)

(The scientific publications listed on this page originate from the Web of Science or SciELO databases. Their authors have cited FAPESP grant or fellowship project numbers awarded to Principal Investigators or Fellowship Recipients, whether or not they are among the authors. This information is collected automatically and retrieved directly from those bibliometric databases.)

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, FEB 2022. (19/13147-6, 21/00971-2, 18/21727-0)

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., 2023-02-03. (21/00971-2, 16/13368-4)

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., 2022-12-01. (21/00971-2)

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., 2023-10-01. (21/00971-2, 15/23948-5)

GARCIA, BIANCA B. M.; MERTINS, OMAR; DA SILVA, EMERSON R.; HAN, SANG W.. Influence of the degree of arginine substitution on chitosan-N-arginine-based chitosomes: Insights for improved gene delivery systems. JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, v. 92, p. 10-pg., 2024-01-25. (20/06913-1, 21/00971-2, 15/20206-8, 22/04361-7, 23/03903-3)

GARCIA, BIANCA B. M.; DOUKA, STEFANIA; MERTINS, OMAR; MASTROBATTISTA, ENRICO; HAN, SANG W.. Efficacy of Chitosan-N-Arginine Chitosomes in mRNA Delivery and Cell Viability Enhancement. ACS APPLIED BIO MATERIALS, v. N/A, p. 11-pg., 2024-11-19. (20/06913-1, 22/04361-7, 23/03903-3, 21/00971-2)

MADRID, RAFAEL R. M.; MATHEWS, PATRICK D.; PRAMANIK, SHREYA; MANGIAROTTI, AGUSTIN; FERNANDES, RODRIGO; ITRI, ROSANGELA; DIMOVA, RUMIANA; MERTINS, OMAR. Hybrid crystalline bioparticles with nanochannels encapsulating acemannan from Aloe vera: Structure and interaction with lipid membranes. Journal of Colloid and Interface Science, v. 673, p. 13-pg., 2024-06-14. (21/00971-2, 22/12376-4)