Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment

• Published in: Pharmaceutics 2021-11, Vol.13 (12), p.1997
• Main Authors: Zafar, Ameeduzzafar, Alruwaili, Nabil K, Imam, Syed Sarim, Alsaidan, Omar Awad, Alkholifi, Faisal K, Alharbi, Khalid Saad, Mostafa, Ehab M, Alanazi, Abdullah S, Gilani, Sadaf Jamal, Musa, Arafa, Alshehri, Sultan, Rawaf, Alenazy, Alquraini, Ali
• Format: Article
• Language: English
• Subjects: antimicrobial activity; antioxidant; Bioavailability; Cancer therapies; Cellulose; Chemotherapy; Cytotoxicity; Drug delivery systems; genistein; Hydroxypropyl β cyclodextrin; Microwaves; Pharmaceutical industry; poloxamer
• ISSN: 1999-4923; 1999-4923
• DOI: 10.3390/pharmaceutics13121997

The current study was designed to prepare the inclusion complex Genistein (GS) using Hydroxypropyl β cyclodextrin (HP β CD) and poloxamer 188 (PL 188). The binary inclusion complex (GS BC) and ternary inclusion complex (GS TC) were developed by microwave irradiation technique and evaluated for a comparative dissolution study. Further, the samples were assessed for FTIR, DSC, XRD, and NMR for the confirmation of complex formation. Finally, antioxidant and antimicrobial studies and cytotoxicity studies on a breast cancer (MCF-7) cell line were conducted. The dissolution study result showed a marked increment in GS dissolution/release after incorporation in binary (GS: HP β CD, 1:1) and ternary (GS: HP β CD: PL 188; 1:1:0.5) inclusion complexes. Moreover, the ternary complex exhibited a significant enhancement ( < 0.05) in dissolution than did the binary complexes. This might be due to the presence of PL 188, which helps in solubility enhancement of GS. DSC, XRD and SEM evaluation confirmed the modification in the structure of GS. FTIR and NMR results indicated the formation of an inclusion complex. The antioxidant and antimicrobial activity results revealed that GS TC has shown significant ( < 0.05) higher activity than pure GS. The cytotoxicity study results also depicted concentration-dependent cytotoxicity. GS TC exhibited significantly ( < 0.05) high cytotoxicity to cancer cells (IC = 225 µg/mL) than pure GS (IC = 480 µg/mL). Finally, it was concluded that a remarkable enhancement in the dissolution was observed after the inclusion of GS in the ternary complex and it therefore has significant potential for the treatment of breast cancer.