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AAPS PharmSciTech

, Volume 19, Issue 8, pp 3751–3762 | Cite as

Bioavailability Enhancement of Aripiprazole Via Silicosan Particles: Preparation, Characterization and In vivo Evaluation

  • Azza A. Mahmoud
  • Alaa H. Salama
  • Rehab N. Shamma
  • Faten Farouk
Research Article
  • 49 Downloads

Abstract

The aim of this study was to design a novel carrier for enhancing the bioavailability of the poorly water-soluble drug, aripiprazole (ARP). Silicosan, the applied carrier, was obtained by chemical interaction between tetraethyl orthosilicate (TEOS) and chitosan HCl. Different ARP-loaded silicosan particles were successfully prepared in absence and presence of one of the following surfactants; Tween 80, Poloxamer 407 and cetyltrimethylammonium bromide (CTAB). The prepared ARP-loaded silicosan particles were thoroughly investigated for their structures using FTIR, XRD, and DSC analysis as well as their particle size, zeta potential, flowability, drug content, and in vitro drug release efficiencies. The prepared ARP-loaded silicosan particles were characterized by amorphous structure, high drug entrapment efficiency and a remarkable improvement in the release of aripiprazole in simulated gastric fluid. SEM and EDX revealed that the morphology and silica atom content in the prepared ARP-loaded silicosan particles were affected by the used surfactant in their formulations. The selected ARP-loaded silicosan particles were subjected to in vivo study using rabbits. The obtained pharmacokinetic results showed that the relative bioavailability for orally administered ARP-loaded silicosan particles (SC-2-CTAB) was 66% higher relative to the oral suspension (AUC0-10h was 16.38 ± 3.21 and 27.23 ± 2.35 ng.h/mL for drug powder and SC-2-CTAB formulation, respectively). The obtained results suggested the unique-structured silicosan particles to be used as successful vehicle for ARP.

KEY WORDS

aripiprazole tetraethyl orthosilicate surfactant dissolution bioavailability 

Notes

Compliance with Ethical Standards

All animal experiments were approved by the Research Ethics Committee (REC) for Animal Subject Research at the Faculty of Pharmacy, Cairo University, Egypt and operated according to the National Institutes of Health guide for the care and use of Laboratory animals (NIH Publications No. 8023, revised 1978).

Conflict of Interest

The authors declare that there is no conflict of interest.

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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  1. 1.Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences and Pharmaceutical IndustriesFuture University in EgyptCairoEgypt
  2. 2.Department of Pharmaceutical Technology, Pharmaceutical and Drug Industries Research DivisionNational Research CentreCairoEgypt
  3. 3.Department of Pharmaceutics, Faculty of PharmacyAhram Canadian University6th of October CityEgypt
  4. 4.Department of Pharmaceutics and Industrial Pharmacy, Faculty of PharmacyCairo UniversityCairoEgypt
  5. 5.Department of Pharmaceutical Chemistry, Faculty of PharmacyAhram Canadian University6th of October CityEgypt

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