A β–Sitosterol Encapsulated Biocompatible Alginate/Chitosan Polymer Nanocomposite for the Treatment of Breast Cancer

Obaid Afzal, Md Habban Akhter, Irfan Ahmad, Khursheed Muzammil, Adam Dawria, Mohammad Zeyaullah, Abdulmalik S. A. Altamimi, Habibullah Khalilullah, Shehla Nasar Mir Najib Ullah, Mohammad Akhlaquer Rahman, Abuzer Ali, Naiyer Shahzad, Mariusz Jaremko, Abdul-Hamid M. Emwas, Ibrahim Abdel Aziz Ibrahim

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

Abstract

β–sitosterol is the most abundant type of phytosterol or plant sterol and can be found in various plant dietary sources including natural oils, soy products, and nuts. Numerous studies have demonstrated the potential therapeutic and clinical applications of β–sitosterol including lowering low-density lipoprotein and cholesterol levels, scavenging free radicals in the body, and interestingly, treating and preventing cancer. This study focuses on synthesizing and characterizing β–sitosterol encapsulated Alginate/Chitosan nanoparticles (β–sito–Alg/Ch/NPs) and evaluating their effectiveness in breast cancer treatment and their pharmacokinetic profile in vivo. The synthesized NPs, which incurred a mean size of 25 ± 1 nm, were extensively characterized in vitro for various parameters including surface charge and morphology. The NPs were further analyzed using DSC, FT-IR, thermogravimetry and X-ray diffraction studies. The release of β–sito from NPs was carried out in a bio-relevant medium of pH 7.4 and pH 5.5 and samples were drawn off and analyzed under time frames of 0, 8, 16, 32, 64, 48, 80, and 96 h, and the best kinetic release model was developed after fitting drug release data into different kinetic models. The metabolic activity of MCF-7 cells treated with the prepared formulation was assessed. The radical scavenging potential of β–sito–Alg/Ch/NPs was also studied. The pharmacokinetic parameters including Cmax, Tmax, half-life (t1/2), and bioavailability were measured for β–sito–Alg/Ch/NPs as compared to β–sito–suspension. The β–sito–Alg/Ch/NPs stability was assessed at biological pH 7.4. The % drug release in PBS of pH 7.4 reportedly has shown 41 ± 6% vs. 11 ± 1% from β–sito–Alg/Ch/NPs and β–sito–suspension. In acidic pH 5.5 mimicking the tumor microenvironment has shown 75 ± 9% vs. 12 ± 4% drug release from β–sito–Alg/Ch/NPs and β–sito–suspension. When compared to the β–sito–suspension, the β–sito–Alg/Ch/NPs demonstrated greater cytotoxicity (p < 0.05) and ~3.41-fold higher oral bioavailability. Interestingly, this work demonstrated that β–sito–Alg/Ch/NPs showed higher cytotoxicity due to improved bioavailability and antioxidant potential compared to the β–sito–suspension.
Original languageEnglish (US)
Pages (from-to)1711
JournalPharmaceutics
Volume14
Issue number8
DOIs
StatePublished - Aug 16 2022

Bibliographical note

KAUST Repository Item: Exported on 2022-09-14
Acknowledgements: The authors extend their appreciation to the Deanship of Scientific Research at King Khalid University, KSA, for funding this work through a research group program under grant number RGP. 2/233/43. The APC was funded by King Abdullah University of Science and Technology (KAUST), Thuwal Jeddah, Saudi Arabia

ASJC Scopus subject areas

  • Pharmaceutical Science

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