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Fabrication, characterization and in vitro evaluation of silibinin nanoparticles: an attempt to enhance its oral bioavailability

Authors Sahibzada MUK, Sadiq A, Khan S, Faidah HS, Naseemullah, Khurram M, Amin MU, Haseeb A

Received 4 February 2017

Accepted for publication 13 April 2017

Published 15 May 2017 Volume 2017:11 Pages 1453—1464


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 3

Editor who approved publication: Dr Qiongyu Guo

Muhammad Umar Khayam Sahibzada,1,2 Abdul Sadiq,1 Shahzeb Khan,1 Hani S Faidah,3 Naseemullah,1 Muhammad Khurram,4 Muhammad Usman Amin,5 Abdul Haseeb6

1Department of Pharmacy, University of Malakand, Chakdara, Lower Dir, 2Department of Pharmacy, Sarhad University of Science and Information Technology, Peshawar, Khyber Pakhtunkhwa, Pakistan; 3Department of Microbiology, Faculty of Medicine, Umm Al Qura University, Makkah, Saudi Arabia; 4Department of Pharmacy, Shaheed Benazir Bhutto University, Sheringal, Upper Dir, 5Department of Pharmacology, KMU Institute of Medical Sciences, Kohat, Khyber Pakhtunkhwa, Pakistan; 6Department of Clinical Pharmacy, College of Pharmacy, Umm Al Qura University, Makkah, Saudi Arabia

Background: Silibinin has gained in importance in the past few decades as a hepatoprotector and is used widely as oral therapy for toxic liver damage, liver cirrhosis, and chronic inflammatory liver diseases, as well as for the treatment of different types of cancers. Unfortunately, it has low aqueous solubility and inadequate dissolution, which results in low oral bioavailability.
Materials and methods: In this study, nanoparticles (NPs) of silibinin, which is a hydrophobic drug, were manufactured using two cost-effective methods. Antisolvent precipitation with a syringe pump (APSP) and evaporative precipitation of nanosuspension (EPN) were used. The prepared NPs were characterized using different analytical techniques such as scanning electron microscopy (SEM), fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray powder diffractometry (XRD) and were sifted for their bioavailability through in vitro dissolution and solubility studies. Moreover, the prepared NPs were evaluated for antimicrobial activity against a battery of bacteria and yeast.
Results: DSC and XRD studies indicated that the prepared NPs were amorphous in nature, with more solubility and dissolution compared to the crystalline form of this drug. NPs prepared through the EPN method had better results than those prepared using the APSP method. Antimicrobial activities of the NPs were improved compared to the unprocessed drugs, while having comparable activities to standard antimicrobial drugs.
Conclusion: Results indicate that the NPs have significantly increased solubility, dissolution rate, and antimicrobial activities due to the conversion of crystalline structure into amorphous form.

Keywords: silibinin, nanoparticles, antimicrobial activity, solubility, dissolution

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