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AAPS PharmSciTech

, Volume 19, Issue 7, pp 2961–2970 | Cite as

Labrasol-Enriched Nanoliposomal Formulation: Novel Approach to Improve Oral Absorption of Water-Insoluble Drug, Carvedilol

  • Samaneh Ghassemi
  • Azadeh Haeri
  • Soraya Shahhosseini
  • Simin Dadashzadeh
Research Article
  • 44 Downloads

Abstract

The purpose of the current study was to develop a novel liposomal formulation to improve the oral bioavailability of carvedilol, a Biopharmaceutics Classification System class II with poor aqueous solubility and extensive presystemic metabolism. Conventional and various surfactant-enriched carvedilol-loaded liposomes were prepared by thin film hydration technique and physicochemical properties of liposomes (including size, encapsulation efficiency, release behavior, and morphology) were evaluated. To assess the oral bioavailability, in vivo studies were carried out in eight groups of male Wistar rats (n = 6) and the drug plasma concentration was determined. Conventional and surfactant containing liposomes showed average particle size of 76–104 nm with a narrow size distribution, high encapsulation efficiency (80%≤) and a sustained release profile in simulated intestinal fluid. Compared to the suspension, conventional and Labrasol containing liposomes significantly improved the oral bioavailability and peak plasma concentration of carvedilol. Biocompatibility studies (cell cytotoxicity and histopathological analyses) showed that the enhancing effect might be achieved without any apparent toxicity in the intestine. Decreased oral absorption of carvedilol nanovesicles by using a chylomicron flow blocker indicated contribution of lymphatic transport in nanocapsules absorption. The results reported the successful development of biocompatible Labrasol-enriched carvedilol nanoliposomal formulation with a significant oral enhancement capability.

Graphical Abstract

KEY WORDS

carvedilol nanoliposomes surfactants Labrasol oral bioavailability rat 

Notes

Funding information

This study was supported by a grant from Shahid Beheshti University of Medical Sciences.

Compliance with Ethical Standards

Conflict of Interest

The authors report no conflicts of interest.

Supplementary material

12249_2018_1118_MOESM1_ESM.docx (15 kb)
ESM 1 (DOCX 15 kb)

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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  1. 1.Department of Pharmaceutics, School of PharmacyShahid Beheshti University of Medical SciencesTehranIran
  2. 2.Department of Pharmaceutical Chemistry, School of PharmacyShahid Beheshti University of Medical SciencesTehranIran
  3. 3.Pharmaceutical Sciences Research CenterShahid Beheshti University of Medical SciencesTehranIran

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