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Electrosprayed Polymeric Nanospheres for Enhanced Solubility, Dissolution Rate, Oral Bioavailability and Antihyperlipidemic Activity of Bezafibrate

Authors
  • Sun, Ru1
  • Shen, Chengwu1
  • Shafique, Shumaila2
  • Mustapha, Omer2
  • Hussain, Talib3
  • Khan, Ikram Ullah4
  • Mehmood, Yasir4
  • Anwer, Khaleeq5
  • Shahzad, Yasser3
  • Yousaf, Abid Mehmood3
  • 1 Department of Pharmacy, Shandong Provincial Hospital, Shandong University, Jinan, Shandong, 250000
  • 2 Faculty of Pharmaceutical Sciences, Dow College of Pharmacy, Dow University of Health Sciences, Karachi, 74200 , (Pakistan)
  • 3 Department of Pharmacy, COMSATS University Islamabad, Lahore, 54000 , (Pakistan)
  • 4 Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad, 38000 , (Pakistan)
  • 5 Office of Chief Executive Officer, District Health Authority, Pakpattan, 57400 , (Pakistan)
Type
Published Article
Journal
International Journal of Nanomedicine
Publisher
Dove Medical Press
Publication Date
Jan 31, 2020
Volume
15
Pages
705–715
Identifiers
DOI: 10.2147/IJN.S235146
PMID: 32099359
PMCID: PMC6999775
Source
PubMed Central
Keywords
License
Green

Abstract

Background Bezafibrate is a BCS class II drug as it presents very low solubility in water; therefore, its bioavailability after oral administration is very poor. The aim of this work was to enhance solubility and dissolution rate of bezafibrate in water in order to enhance its oral bioavailability. Methods Several formulations were prepared using PVP K30 and Cremophor ELP employing the solvent-evaporation method and the electrospraying technique. Solubility, release rate, bioavailability in male Sprague Dawley rats, and lipid profile attributes in Wistar rats were assessed in comparison with bezafibrate plain powder. Solid-state characterization was carried out using X-ray diffraction (XRD) analysis, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy and scanning electron microscopy (SEM). Results All the formulations exerted positive effect towards the desired goal. In particular, the optimized formulation furnished about 14-fold enhanced solubility and 85.48 ± 10.16% drug was released in 10 min as compared with bezafibrate alone (4.06 ± 2.59%). The drug existed in the amorphous state in the prepared sample as confirmed by XRD and DSC, whilst no drug-excipient interactions were observed through FTIR analysis. Moreover, SEM revealed smooth-surfaced spherical particles of the optimized formulation. A 5.5-fold higher oral bioavailability was achieved with the optimized formulation in comparison with bezafibrate plain powder. Also, TG, LDL and TC were decreased, and HDL was increased considerably in HFD-treated rats. Conclusion The optimized formulation consisting of bezafibrate, PVP K30 and cremophor ELP (1/12/1.5, w/w/w) might be a capable drug delivery system for orally administering poorly water-soluble bezafibrate with improved bioavailability and antihyperlipidemic effects.

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