Preparation, Characterization, and Evaluation of Physcion Nanoparticles for Enhanced Oral Bioavailability: An Attempt to Improve Its Antioxidant and Anticancer Potential

Fazli Khuda; Irum Zahir; Atif Ali Khan Khalil; Sajid Ali; Naveed Ullah; Ahmed H Albariqi; Mi-Jeong Ahn; Muhammad Shafique; Sultan Mehtap Büyüker; Saud Almawash

doi:10.1021/acsomega.3c04821

Preparation, Characterization, and Evaluation of Physcion Nanoparticles for Enhanced Oral Bioavailability: An Attempt to Improve Its Antioxidant and Anticancer Potential

ACS Omega. 2023 Sep 11;8(37):33955-33965. doi: 10.1021/acsomega.3c04821. eCollection 2023 Sep 19.

Authors

Affiliations

¹ Department of Pharmacy, University of Peshawar, Peshawar 25120, Pakistan.
² Department of Pharmacognosy, Institute of Pharmacy, Lahore College for Women University, Lahore 54000, Pakistan.
³ Department of Biotechnology, Abdul Wali Khan University, Mardan 23200, Pakistan.
⁴ Department of Pharmacy, University of Swabi, Swabi 23430, Pakistan.
⁵ Department of Pharmaceutics, College of Pharmacy, Jazan University, Jazan 45142, Saudi Arabia.
⁶ College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju 52828, Republic of Korea.
⁷ Department of Pharmaceutical Sciences, College of Pharmacy, Shaqra University, Shaqra 11961, Saudi Arabia.
⁸ Department of Pharmacy Services, Üsküdar University, İstanbul 34662, Turkey.

Abstract

This study aims to enhance the dissolution rate of a poorly water-soluble drug physcion by producing its nanoparticles (NPs) using an antisolvent precipitation with a syringe pump (APSP) method and to assess its antioxidant and cytotoxic potential. The NPs were prepared using a simple and cost-effective APSP method and subsequently characterized by different analytical techniques including dynamic light scattering (DLS), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and X-ray powder diffractometry (XRD). They were also subjected to solubility and dissolution studies, and different parameters such as dissolution efficiency (DE), mean dissolution time (MDT), and difference (f₁) and similarity factors (f₂) were determined. Furthermore, physcion and its NPs were investigated for antioxidant and cytotoxic effects using various in vitro assays. SEM and DLS analysis indicated that the average size of physcion NPs was 110 and 195 ± 5.6 nm, respectively. The average ζ-potential and polydispersibility index (PDI) of the prepared NPs were -22.5 mV and 0.18, respectively, showing excellent dispersibility. XRD confirmed the amorphous nature of physcion NPs. The solubility and dissolution rates of NPs were significantly higher than those of the original powder. The antioxidant potential studied by the (DPPH), FRAP, and H₂O₂ assays was greater for physcion NPs than that for the raw powder. The IC₅₀ values of physcion NPs against the aforementioned models were 57.56, 22.30, and 22.68 μg/mL, respectively. Likewise, the cytotoxic potential investigated through the MTT assay showed that physcion NPs were more cytotoxic to cancer cell lines A549 (IC₅₀ 4.12 μg/mL), HepG2 (IC₅₀ 2.84 μg/mL), and MDA-MB-231 (IC₅₀ 2.97 μg/mL), while it had less effect on HPAEpiC (IC₅₀ 8.68 μg/mL) and HRPTEpiC (IC₅₀ 10.71 μg/mL) normal human epithelial cells. These findings have proved that the APSP method successfully produced physcion NPs with enhanced solubility, dissolution rate, and antioxidant and cytotoxic activities.