Development and Characterization of Calcium-Alginate Beads of Apigenin: In Vitro Antitumor, Antibacterial, and Antioxidant Activities

Abstract

The objective of this work was to develop sustained-release Ca-alginate beads of apigenin using sodium alginate, a natural polysaccharide. Six batches were prepared by applying the ionotropic gelation technique, wherein calcium chloride was used as a crosslinking agent. The beads were evaluated for particle size, drug loading, percentage yield, and in vitro drug release. Particle size was found to decrease, and drug entrapment efficiency was enhanced with an increase in the polymer concentration. The dissolution study showed sustained drug release from the apigenin-loaded alginate beads with an increase in the polymer proportion. Based on the dissolution profiles, BD6 formulation was optimized and characterized for FTIR, DSC, XRD, and SEM, results of which indicated successful development of apigenin-loaded Ca alginate beads. MTT assay demonstrated a potential anticancer effect against the breast cancer MCF-7 cell lines. The antimicrobial activity exhibited effective inhibition in the bacterial and fungal growth rate. The DPPH measurement revealed that the formulation had substantial antioxidant activity, with EC50 value slightly lowered compared to pure apigenin. A stability study demonstrated that the BD6 was stable with similar (f2) drug release profiles in harsh condition. In conclusion, alginate-based beads could be used for sustaining the drug release of poorly water-soluble apigenin while also improving in vitro antitumor, antimicrobial, and antioxidant activity.

Selected strategies to fight pathogenic bacteria

“…Usage of alginate has several advantages including ease of preparation, biocompatibility, biodegradability, and absence of toxicity 322 . Alginate-based beads were reported to be useful for sustaining the release of poorly water-soluble flavones 323 .…”

A review on the synthesis and development of alginate hydrogels for wound therapy

“…Drugs can be mixed and dispersed with raw materials, and then fixed by polymer skeleton in the gelation process of the system, so that drugs are successfully uniformly loaded in hydrogels. 139 Sodium alginate hydrogel can load peptides, borax, aloe solution, vitamin E, cyclic adenosine monophosphate and Raphanus sativus L. seed extract in a relatively simple way. 56,90,[140][141][142] Some researchers used sodium alginate oxidized by iodized salt to react with gelatin in situ to form a hydrogel, and introduced borax and cyclic adenosine monophosphate before gel formation.…”

Phytochemicals, Biological Activities, Molecular Mechanisms, and Future Prospects of Plantago asiatica L.

“…Apigenin (1) has significant effects against various pathogenic bacterial strains like Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella typhimurium, and Proteus mirabilis, as well as antifungal activity for Candida albicans. 84,85 Similarly, luteolin (2) is a novel therapeutic drug for infectious lung diseases caused by S. aureus. 86,87 The relevant data of the antibacterial activity are summarized in Table 4 on the basis of previous studies of the major active components of P. asiatica.…”

“…P. asiatica , a natural antibiotic, contains a variety of naturally antibacterial and anti-inflammatory ingredients, which eliminates the body’s dysentery, typhoid bacteria, and Staphylococcus aureus , thereby preventing inflammation in the body. Apigenin ( 1 ) has significant effects against various pathogenic bacterial strains like Escherichia coli , Staphylococcus aureus , Pseudomonas aeruginosa , Salmonella typhimurium , and Proteus mirabilis , as well as antifungal activity for Candida albicans . , Similarly, luteolin ( 2 ) is a novel therapeutic drug for infectious lung diseases caused by S. aureus . , The relevant data of the antibacterial activity are summarized in Table on the basis of previous studies of the major active components of P. asiatica .…”