Selection and Control of Process Conditions Enable the Preparation of Curcumin-Loaded Poly(lactic-co-glycolic acid) Nanoparticles of Superior Performance

Author(s)

da Silva Feltrin, Felipe ; D'Angelo, Natalia Aimee ; de Oliveira Guarnieri, Joao Paulo ; Lopes, Andre Moreni ; Lancellotti, Marcelo ; Lona, Liliane Maria Ferrareso

• Document type: Journal article
• Source: ACS APPLIED MATERIALS & INTERFACES; v. 15, n. 22, p. 14-pg., 2023-05-23.

Abstract

Curcumin (CUR) is one natural bioactive compound acknowledgedfordiverse therapeutic activities, but its use is hindered by its poorbioavailability, fast metabolism, and susceptibility to pH variationsand light exposure. Thus, the encapsulation in poly-(lactic-co-glycolic acid), or PLGA, has been successfully used toprotect and enhance CUR absorption in the organism, making CUR-loadedPLGA nanoparticles (NPs) promising drug delivery systems. However,few studies have focused beyond CUR bioavailability, on the environmentalvariables involved in the encapsulation process, and whether theycould help obtain NPs of superior performance. Our study evaluatedpH (3.0 or 7.0), temperature (15 or 35 degrees C), light exposure, andinert atmosphere (N-2) incidence in the encapsulation ofCUR. The best outcome was at pH 3.0, 15 degrees C, without light incidence,and without N-2 usage. This best nanoformulation showedNP size, zeta potential, and encapsulation efficiency (EE) of 297nm, -21 mV, and 72%, respectively. Moreover, the CUR in vitro release at pH values 5.5 and 7.4 suggested differentpotential applications for these NPs, one of which was demonstratedby the effective inhibition of multiple bacteria (i.e., Gram-negative, Gram-positive, and multi-resistant) in the minimalinhibition concentration assay. Besides, statistical analyses confirmeda significant impact of temperature on the NP size; in addition, temperature,light, and N-2 affected the EE of CUR. Thus, the selectionand control of process variables resulted in higher CUR encapsulationand customizable outcomes, ultimately enabling more economical processesand providing future scale-up guidelines. (AU)

• FAPESP's process: 18/12831-8 - In situ synthesis of biodegradable polymers using nanocrystalline and microfibrillated cellulose and lignin with no functionalization
• Grantee: Liliane Maria Ferrareso Lona
• Support Opportunities: Regular Research Grants
• FAPESP's process: 21/09341-1 - Alternative functional polymeric materials with potential application to the treatment and proliferation of diseases
• Grantee: Liliane Maria Ferrareso Lona
• Support Opportunities: Regular Research Grants
• FAPESP's process: 20/03727-2 - Polymersomes development aiming at the co-encapsulation of drugs for application in cancer therapy
• Grantee: Natalia Aimee D'Angelo
• Support Opportunities: Scholarships in Brazil - Master
• FAPESP's process: 18/10799-0 - Combinatorial therapy using polymersomes decorated with transferrin and incorporated into chitosan hydrogels as smart drug delivery systems for melanoma tumor cells
• Grantee: André Moreni Lopes
• Support Opportunities: Scholarships in Brazil - Young Researchers
• FAPESP's process: 17/10789-1 - Combinatorial therapy using polymersomes decorated with transferrin and incorporated into chitosan hydrogels as smart drug delivery systems for melanoma tumor cells
• Grantee: André Moreni Lopes
• Support Opportunities: Research Grants - Young Investigators Grants