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Mohsin Kazi,1 Muhammad Farooq Khan,2 Fahd A Nasr,3 Mohammad Z Ahmed,3 Ali S Alqahtani,3 Meser M Ali,4 Mohammed S Aldughaim5 1Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, 11451, Kingdom of Saudi Arabia; 2Department of Zoology, College of Science, King Saud University, Riyadh, 11451, Kingdom of Saudi Arabia; 3Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh, 11451, Kingdom of Saudi Arabia; 4Department of Neurosurgery, Henry Ford Health, Detroit, MI, 48202, USA; 5Research Center, King Fahad Medical City, Riyadh Second Health Cluster, Riyadh, 11525, Kingdom of Saudi ArabiaCorrespondence: Mohsin Kazi; Mohammed S Aldughaim, Email mkazi@ksu.edu.sa; maldughaim@kfmc.med.saPurpose: Curcumin (CUR) and piperine (PP) are bioactive compounds with prominent pharmacological activities that have been investigated for the treatment of various diseases. The aim of the present study is to develop Bio-SNEDDS for CUR and PP as a combined delivery system for cancer therapy.Methods: CUR and PP loaded Bio-SNEDDSs with varying compositions of bioactive lipid oils, surfactants, and cosolvents were prepared at room temperature. Bio-SNEDDSs were characterized using a Zetasizer Nano particle size analyzer and further examined by transmission electron microscopy (TEM) for morphology. The in vivo toxicity of the preparations of Bio-SNEDDS was investigated in wild-type zebrafish embryos and cytotoxicity in THP-1 (human leukemia monocytic cells), Jurkat (human T lymphocyte cells) and HUVEC (non-cancerous normal) cells.Results: Bio-SNEDDSs were successfully developed with black seed oil, Imwitor 988, Transcutol P and Cremophor RH40 at a ratio of 20/20/10/50 (%w/w). The droplet size, polydispersity index and zeta potential of the optimized Bio-SNEDDS were found to be 42.13 nm, 0.59, and − 19.30 mV, respectively. Bio-SNEDDS showed a spherical structure evident by TEM analysis. The results showed that Bio-SNEDDS did not induce to

Abdelrahman Y Sherif,1,2 Gamaleldin I Harisa,1– 3 Fars K Alanazi,1,2 Fahd A Nasr,4 Ali S Alqahtani4 1Kayyali Chair for Pharmaceutical Industry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 2Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 3Department of Biochemistry and Molecular Biology, College of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt; 4Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh, Saudi ArabiaCorrespondence: Abdelrahman Y Sherif, Tel +966 500859725, Email ashreef@ksu.edu.saPurpose: The present study aimed to develop gefitinib-loaded solid lipid nanoparticles (GEF-SLN), and GEF-loaded PEGylated SLN (GEF-P-SLN) for targeting metastatic lung cancer through the lymphatic system.Methods: The prepared SLNs were characterized in terms of physicochemical properties, entrapment efficiency, and in-vitro release. Furthermore, ex-vivo permeability was investigated using the rabbit intestine. Cytotoxicity and apoptotic effects were studied against A549 cell lines as a model for lung cancer.Results: The present results revealed that the particle size and polydispersity index of the prepared formulations range from 114 to 310 nm and 0.066 to 0.350, respectively, with negative zeta-potential (− 14 to − 27.6). Additionally, SLN and P-SLN showed remarkable entrapment efficiency above 89% and exhibited sustained-release profiles. The permeability study showed that GEF-SLN and GEF-P-SLN enhanced the permeability of GEF by 1.71 and 2.64-fold, respectively, compared with GEF suspension. Cytotoxicity showed that IC50 of pure GEF was 3.5 μg/mL, which decreased to 1.95 and 1.8 μg/mL for GEF-SLN and GEF-P-SLN, respectively. Finally, the apoptotic study revealed that GEF-P-SLN decreased the number of living cells from 49.47 to 3.43 when compared with pure GEF.Conclusion: These results concluded that GEF-P-SLN is a promising approach to improving the therapeutic outcom

Abdelrahman Y Sherif,1,2 Gamaleldin I Harisa,1– 3 Fars K Alanazi,1,2 Fahd A Nasr,4 Ali S Alqahtani4 1Kayyali Chair for Pharmaceutical Industry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 2Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 3Department of Biochemistry and Molecular Biology, College of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt; 4Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh, Saudi ArabiaCorrespondence: Abdelrahman Y Sherif, Tel +966 500859725, Email ashreef@ksu.edu.saPurpose: The present study aimed to develop gefitinib-loaded solid lipid nanoparticles (GEF-SLN), and GEF-loaded PEGylated SLN (GEF-P-SLN) for targeting metastatic lung cancer through the lymphatic system.Methods: The prepared SLNs were characterized in terms of physicochemical properties, entrapment efficiency, and in-vitro release. Furthermore, ex-vivo permeability was investigated using the rabbit intestine. Cytotoxicity and apoptotic effects were studied against A549 cell lines as a model for lung cancer.Results: The present results revealed that the particle size and polydispersity index of the prepared formulations range from 114 to 310 nm and 0.066 to 0.350, respectively, with negative zeta-potential (− 14 to − 27.6). Additionally, SLN and P-SLN showed remarkable entrapment efficiency above 89% and exhibited sustained-release profiles. The permeability study showed that GEF-SLN and GEF-P-SLN enhanced the permeability of GEF by 1.71 and 2.64-fold, respectively, compared with GEF suspension. Cytotoxicity showed that IC50 of pure GEF was 3.5 μg/mL, which decreased to 1.95 and 1.8 μg/mL for GEF-SLN and GEF-P-SLN, respectively. Finally, the apoptotic study revealed that GEF-P-SLN decreased the number of living cells from 49.47 to 3.43 when compared with pure GEF.Conclusion: These results concluded that GEF-P-SLN is a promising approach

Sajid Hussain,1,2 Farhat Ullah,1 Muhammad Ayaz,1 Syed Adnan Ali Shah,3 Azhar-ul-Haq Ali Shah,4 Syed Majid Shah,1,2 Abdul Wadood,5 Waqar Aman,2 Riaz Ullah,6 Abdelaaty A Shahat,6,7 Fahd A Nasr6 1Department of Pharmacy, University of Malakand, Malakand, Pakistan; 2Department of Pharmacy, Kohat University of Science & Technology, Kohat, Pakistan; 3Research Institute of Natural Products for Drug Discovery (RiND), Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Shah Alam, Malaysia; 4Department of Chemistry, Kohat University of Science & Technology, Kohat, Pakistan; 5Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan, Pakistan; 6Department of Pharmacognosy (Medicinal Aromatic and Poisonous Plants Research Center), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; 7Chemistry of Medicinal Plants Department, National Research Centre, Dokki, Giza, EgyptCorrespondence: Sajid Hussain; Farhat UllahDepartment of Pharmacy, University of Malakand, Dir (L), Chakdara 18000, KPK, PakistanTel +92 3339178183; +92 3339361513Email hussain77pk2003@yahoo.com; farhataziz80@hotmail.comBackground: Cancer is one of the chronic health conditions worldwide. Various therapeutically active compounds from medicinal plants were the current focus of this research in order to uncover a treatment regimen for cancer. Anchusa arvensis (A. anchusa) (L.) M.Bieb. contains many biologically active compounds.Methods: In the current study, new ester 3-hydroxyoctyl -5- trans-docosenoate (compound-1) was isolated from the chloroform soluble fraction of A. anchusa using column chromatography. Using MTT assay, the anticancer effect of the compound was determined in human hepatocellular carcinoma cells (HepG-2) compared with normal epithelial cell line (Vero). DPPH and ABTS radical scavenging assays were performed to assess the antioxidant potential. The Molecular Operating Environment (MOE-2016) tool was used against tyrosine kinase.Results: The structur