Apigenin-Loaded Stealth Liposomes: Development and Pharmacokinetic Studies for Enhanced Plasma Retention of Drug in Cancer Therapy

• Published in: Topics in catalysis Vol. 67; no. 1-4; pp. 46 - 58
• Main Authors: Shetti, Priya, Jalalpure, Sunil S., Patil, Archana S., Kaur, Kirtanjot
• Format: Journal Article
• Language: English
• Published: New York Springer US 01.01.2024; Springer Nature B.V
• Subjects: Anticancer properties; Bioavailability; Catalysis; Characterization and Evaluation of Materials; Chemistry; Chemistry and Materials Science; Effectiveness; Entrapment; Ethanol; Industrial Chemistry/Chemical Engineering; Liposomes; Original Paper; Particle size; Pharmacokinetics; Pharmacy; Physical Chemistry; Solubility; Stability; Zeta potential; Plasma therapy; DSPE-PEG 2000; Breast cancer; Design expert; Stealth liposomes
• ISSN: 1022-5528; 1572-9028
• DOI: 10.1007/s11244-023-01818-3

Apigenin belongs to the class of compounds known as flavones. It possesses significant antioxidant, anti-inflammatory, and antitumor potential in various preclinical studies. Despite being a potent anticancer molecule, it suffers from significant pharmacokinetic limitations. As per Biopharmaceutical classification system, Apigenin has been categorized as a Class II drug. It has high permeability but low solubility which leads to lower bioavailability. To increase its bioavailability, it has to raise its solubility. Thus, the present work aimed to develop novel Apigenin loaded stealth liposomes to enhance its solubility, plasma residence time and better therapeutic efficacy. Apigenin loaded stealth liposomes (APISL) were prepared by utilizing the ethanol injection technique. The formulation was statistically optimized by DOE and evaluated for particle size, zeta potential, entrapment efficiency, morphology, in-vitro drug release study, in-vivo pharmacokinetic study and stability study. Among all of the preparations, the optimized stealth liposomal batch (APISL-L8) produced the best outcomes, with smallest particle size, the highest percent entrapment efficiency and the highest drug release percent at 48 h. The optimized Apigenin loaded stealth liposomes L8 was found to show higher percent drug release than the plain Apigenin as per Higuchi release model. According to in-vivo experiments, stealth liposomes had a longer exposure period in comparison to pure drug solution. When compared to standard drug, investigations revealed that Apigenin-loaded stealth liposomes demonstrated better plasma retention time and stability. Thus, the result reveals that, the Apigenin-loaded stealth liposome demonstrated an improved bioavailability with enhanced antitumor efficacy in the treatment of breast cancer. Graphical Abstract