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Cited by 392Advanced Drug Delivery SystemsDrug Solubulity and Delivery SystemsNanoparticle-Based Drug Delivery

Positively charged nanoparticles for improving the oral bioavailability of cyclosporin-A

El-Shabouri, M.H·2002·International Journal of Pharmaceutics
DOI 10.1016/s0378-5173(02)00461-1
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Abstract

In this study, cyclosporin-A (Cy-A) a highly lipophilic, poorly absorbable drug can be prepared easily and reproducibly as positively and negatively charged nanoparticles with the aim of improving its bioavailability and reducing its inter- and intra-individual variability. The nanoparticles were prepared by emulsification solvent diffusion method, using lecithin and poloxamer 188 as emulsifiers, and chitosan HCl, gelatin-A or sodium glycocholate (SGC) as charge inducing agents. The prepared nanoparticles were evaluated with respect to particle size, zeta potential, drug content and encapsulation efficiency. The bioavailability Cy-A from nanoparticles in comparison with the currently available Cy-A microemulsion (Neoral) were assessed in beagle dogs. The results obtained revealed that, it was possible to prepare Cy-A as nanoparticles with size range of 104-148 nm. Chitosan HCl and gelatin-A nanoparticles exhibited +31.2 and +23.1 mV zeta potential, respectively; while SGC-nanoparticles exhibited -41.6 mV zeta potential. The in vivo results showed that, chitosan-nanoparticles gave the highest C(max) (2762.8 ng/ml) of Cy-A after 2.17 h (T(max)), while SGC-nanoparticles gave the lowest one (1202.4 ng/ml after 4.0 h). Furthermore, AUC(0-24) of Cy-A from chitosan-nanoparticles was markedly increased by about 2.6-fold when compared with SGC-nanoparticles and increased by about 1.8-fold when compared with the reference Neoral microemulsion. However, in case of gelatin-nanoparticles the AUC(0-24) of Cy-A increased by about 1.8 and 1.2-fold when compared with SGC-nanoparticles and the reference Neoral microemulsion, respectively. The relative bioavailability of Cy-A from chitosan-nanoparticles was increased by about 73%, and by about 18% from gelatin nanoparticles, while it was decreased by about 36% from SGC-nanoparticles.

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  • Positively charging PLGA particles, for example with positively charged stabilizers, increases epithelial penetration and systemic uptake of encapsulated slightly soluble drugs; these favorable characteristics are not found with anionic stabilizers.

    “However, positively charging PLGA particles, for example using positively charged stabilizers, increases the epithelial penetration and systemic uptake of encapsulated, slightly soluble drugs. These favorable characteristics are not found in particulate carriers prepared with anionic stabilizers [5,46].”

    From Use of lectin-functionalized particles for oral immunotherapy (2012) · cites this paper as [46]

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Authors
El-Shabouri, M. H.
Affiliations
Mansoura University (EG)
Corresponding author
El-Shabouri, M.H
Venue
International Journal of Pharmaceutics
Publisher
Elsevier BV
Published
2002-12
Volume
249
Issue
1-2
Pages
101-108
ISSN
0378-5173 (ISSN-L)
DOI
10.1016/s0378-5173(02)00461-1
OpenAlex
W2044872933
Cited by
392
References
38
Citations by year
2026: 8 · 2025: 19 · 2024: 28 · 2023: 26 · 2022: 21 · 2021: 24 · 2020: 23 · 2019: 18 · 2018: 19 · 2017: 15 · 2016: 20 · 2015: 13 · 2014: 14 · 2013: 16 · 2012: 32
FWCI
4.05
Type
journal article
Language
en
Open access
closed
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • International Journal of Pharmaceutics (publishedVersion)
  • PubMed (publishedVersion)
Funders
Mansoura University
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords
cyclosporine, positively charged nanoparticles, oral bioavailability, chitosan nanoparticles, gelatin nanoparticles, sodium glycocholate, zeta potential, relative bioavailability, poorly water-soluble drugs, drug delivery systems, beagle dogs
MeSH terms
Administration, Oral, Animals, Biological Availability, Dogs, Male, Cyclosporine, Nanotechnology

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