Development of enoxaparin sodium polymeric microparticles for colon-specific delivery

Authors

  • Dana Hales
  • Maxime Casteran
  • Anne Sapin-Minet
  • Ioan Tomuţa
  • Marcela Achim
  • Laurian Vlase
  • Philippe Maincent

DOI:

https://doi.org/10.15386/cjmed-442

Keywords:

microparticles, colonic delivery, enoxaparin, Eudragit® FS 30D, Eudragit® RS PO

Abstract

Background and aims. Recent studies have shown that low molecular weight heparins are effective in the treatment of inflammatory bowel disease. Therefore, there is considerable interest in the development of an oral colonic delivery pharmaceutical system allowing targeted release of heparin in the inflamed tissue. The objective of this study was to prepare microparticles for the oral administration and colonic release of enoxaparin and to evaluate the influence of certain formulation factors on their characteristics.

Methods. Microparticles were prepared by water/oil/water double emulsion technique followed by solvent evaporation. The influence of several formulation factors on the characteristics of microparticles were evaluated. The formulation factors were alginate concentration in the inner aqueous phase, polymer (Eudragit® FS 30D and Eudragit® RS PO) concentration in the organic phase and ratios between the two polymers. The microparticles were characterized in terms of morphology, size, entrapment efficiency and enoxaparin release.

Results. The results showed that increasing sodium alginate percentage reduced the encapsulation efficiency of enoxaparin and accelerated enoxaparin release. Regarding the influence of the two polymers, reducing polymer concentration in the organic phase led to a smaller size of microparticles, a lower entrapment efficiency and an important retardation of enoxaparin release. The formulation prepared with Eudragit® FS 30D limited the release to a maximum of 3% in gastric simulated environment, a specific characteristic of oral systems for colonic delivery, and fulfilled our objective to delay the release.

Conclusions. Microparticles prepared with Eudragit® FS 30D represent a suitable and potential oral system for the colonic delivery of enoxaparin.

Author Biographies

Dana Hales, University of Medicine and Pharmacy „Iuliu Haţieganu” Cluj-Napoca

Faculty of Pharmacy,

Department of Pharmaceutical Technology and Biopharmacy,

Maxime Casteran, Université de Lorraine

CITHEFOR, EA 3452

Anne Sapin-Minet, Université de Lorraine

CITHEFOR, EA 3452,

Ioan Tomuţa, University of Medicine and Pharmacy „Iuliu Haţieganu” Cluj-Napoca

Faculty of Pharmacy

Department of Pharmaceutical Technology and Biopharmacy

Marcela Achim, University of Medicine and Pharmacy „Iuliu Haţieganu” Cluj-Napoca

Faculty of Pharmacy

Department of Pharmaceutical Technology and Biopharmacy

Laurian Vlase, University of Medicine and Pharmacy „Iuliu Haţieganu” Cluj-Napoca

Faculty of Pharmacy

Department of Pharmaceutical Technology and Biopharmacy

Philippe Maincent, Université de Lorraine

CITHEFOR, EA 3452

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Published

2015-06-19

How to Cite

1.
Hales D, Casteran M, Sapin-Minet A, Tomuţa I, Achim M, Vlase L, Maincent P. Development of enoxaparin sodium polymeric microparticles for colon-specific delivery. Med Pharm Rep [Internet]. 2015 Jun. 19 [cited 2025 Oct. 5];88(3):357-65. Available from: https://medpharmareports.com/index.php/mpr/article/view/442

Issue

Section

Original Research