Obtenção de Nanopartículas Poliméricas a Base de Goma do Cajueiro Acetilada e Goma do Angico para Incorporação do Alendronato de Sódio

Abstract

Osteoporosis is a disease characterized by low bone mass and bone tissue deterioration, with the occurrence of fracture as its main clinical manifestation. Bisphosphonates are considered as the first-line pharmacological treatment for this condition. Among the bisphosphonates, alendronate sodium (ALD) stands out as the drug commonly used due to its effectiveness in reducing the incidence of fractures. However, its prolonged use has been associated with the emergence of side effects, particularly gastrointestinal problems. In this context, the need for new therapeutic alternatives that increase the benefits of ALD to patients becomes evident. Therefore, polymeric nanoparticles (NPPs) have been proposed as promising systems for drug delivery, drawing attention due to their therapeutic potential. Thus, the present study aimed to develop polymeric nanoparticles using two natural polymers as a vehicle for incorporation of ALD, in addition to characterizing and evaluating its effects on erythrocytes. For the characterization of the gums and the drug, infrared spectroscopy (FT-IR) readings were performed. The nanoparticles were synthesized at room temperature, under constant agitation at 15.000rpm for 30 minutes, using acetylated cashew gum (GAC) at 0.1% and 0.05% and DMSO 5%, forming the organic phase. For the aqueous phase, 10mg of angico gum (GA) was used as a surfactant and sodium alendronate at different concentrations: 5, 10 and 15mg, both diluted in distilled water. After formulated, the particles were characterized regarding size, polydispersion index and Zeta potential using the dynamic light scattering (DLS) technique and regarding drug quantification and incorporation efficiency using a UV-visible spectrophotometer with readings at 260nm. The hemolytic activity was evaluated against

human erythrocytes using nanoencapsulated ALD, as well as in its free form (15mg). The FT- IR analyses showed that the cashew gum, modified with acetic anhydride, presented an

intense absorption band in the 1750cm-1

region, specific for acetylation. The GA spectrum

showed bands at 1022cm-1

, characteristic of polysaccharides, confirming its composition. In addition, the ALD FT-IR demonstrated drug-specific bands (phosphate groups at 1544cm-1 and P-OH at 1022cm-1

). Through the DLS analyses, it was observed that the diameter of the formulated NPPs varied between 303.2nm – NPPs without the presence of ALD – and 59.62nm – for the NPPs formulated with 15mg of ALD. Furthermore, the Zeta potential of NPPs showed values between -25.9mV and -28.9mV. The incorporation efficiency assay demonstrated that the 0.05% GAC NPPs containing 5mg of ALD incorporated a total of 68.47%, while the formulations 0.1% GAC containing 5mg of ALD incorporated a total of 87.97%. The hemolysis test revealed that NPPs containing ALD were able to reverse the hemolytic activity caused by nanoformulations containing only the polymers, as well as the hemolytic activity caused by the drug in its free form. However, further investigations must be made for a better characterization of nanoparticles.