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

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A Correction to this article was published on 17 June 2023

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Abstract

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.

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Acknowledgements

The authors are thankful to Aktin chemicals, China for providing the drug bas gift sample. Authors are also thankful to KAHER’s BSRC, Belagavi for providing the facility.

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Authors and Affiliations

  1. KAHER’s Dr. Prabhakar Kore Basic Science Research Center, KLE Academy of Higher Education and Research, Nehru Nagar, Belagavi, 590010, Karnataka, India

    Priya Shetti & Sunil S. Jalalpure

  2. Department of Pharmacognosy, KLE College of Pharmacy Belagavi, KLE Academy of Higher Education and Research, Nehru Nagar, Belagavi, 590010, Karnataka, India

    Priya Shetti, Sunil S. Jalalpure, Archana S. Patil & Kirtanjot Kaur

  3. Department of Pharmaceutics, KLE College of Pharmacy Belagavi, KLE Academy of Higher Education and Research, Nehru Nagar, Belagavi, 590010, Karnataka, India

    Archana S. Patil

  4. PG Department of Chemistry, Sri Guru Gobind Singh College, Sector 26, Chandigarh, 160019, India

    Kirtanjot Kaur

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  1. Priya Shetti
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  2. Sunil S. Jalalpure
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Contributions

PPS contributed for experimental work and manuscript preparation, SSJ contributed in hypothesis and finalization of manuscript. ASP worked on DOE software and in compilation of data. The manuscript was written through contributions of all authors. All authors have given approval to the final version of the manuscript.

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Correspondence to Sunil S. Jalalpure.

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The authors declare no competing interests.

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This study involved animals and ethical approval was obtained by the Institutional Animal Ethical Committee – Reg.No221/Po/Re/S/2000/CPCSEA.

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Shetti, P., Jalalpure, S.S., Patil, A.S. et al. Apigenin-Loaded Stealth Liposomes: Development and Pharmacokinetic Studies for Enhanced Plasma Retention of Drug in Cancer Therapy. Top Catal 67, 46–58 (2024). https://doi.org/10.1007/s11244-023-01818-3

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