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Budesonide Loaded PLGA Nanoparticles for Targeting the Inflamed Intestinal Mucosa—Pharmaceutical Characterization and Fluorescence Imaging

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Abstract

Purpose

The purpose of this study was to evaluate the specifically targeted efficiency of budesonide loaded PLGA nanoparticles for the treatment of inflammatory bowel disease (IBD).

Methods

The nanoparticles were prepared by an oil/water (O/W) emulsion evaporation technique. The nanoparticles were characterized for their size, shape and in vitro drug release profile. Solid state characterization was carried out by differential scanning calorimetry (DSC) and X-ray Power diffraction (XPRD). In order to evaluate the targeted efficiency of nanoparticles, a particle localization study in the healthy and in the inflamed colon was determined in vivo. These data were complemented by cryo-sections.

Results

Nanoparticles were 200 ± 05 nm in size with a smooth and spherical shape. The encapsulation efficiency was around 85 ± 3.5%, which was find-out by both, direct and indirect methods. Release of budesonide from the nanoparticles showed a biphasic release profile with an initial burst followed by sustained release. XPRD data revealed that the drug in the polymer matrix existed in crystalline state. Nanoparticles accumulation in inflamed tissues was evaluated by in-vivo imaging system and it was found that particles are accumulated in abundance at the site of inflammation when compared to the healthy group.

Conclusion

The study demonstrates that the budesonide loaded PLGA nanoparticles are an efficient delivery system for targeted drug delivery to the inflamed intestinal mucosa.

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Abbreviations

AFM:

Atomic force microscopy

CD:

Crohn’s disease

DSC:

Differential scanning calorimetry

GIT:

Gastrointestinal tract

IBD:

Inflammatory bowel disease

O/W:

Oil/water

PBS:

Phosphate buffer saline

PDI:

Poly-dispersity index

PLGA:

Poly(lactic-co-glycolic acid)

PVA:

Poly-vinyl alcohol

SD:

Standard deviation

SEM:

Scanning electron microscope

UC:

Ulcerative colitis

XRD:

X-ray diffraction

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ACKNOWLEDGMENTS AND DISCLOSURES

Dr. Salman Khan is thanked here for his technical assistance.

Author information

Authors and Affiliations

  1. Department of Pharmacy, Quaid-i-Azam University, Islamabad, 45320, Pakistan

    Hussain Ali

  2. Biopharmaceutics and Pharmaceutical Technology, Saarland University, Campus A4.1, 66123, Saarbrücken, Germany

    Hussain Ali, Maike Windbergs & Claus-Michael Lehr

  3. Medical Clinic I, University Hospital Erlangen, Research Campus, 91052, Erlangen, Germany

    Benno Weigmann

  4. Department of Drug Delivery (DDEL), Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Saarland University, Campus E 8.1, 66123, Saarbrücken, Germany

    Eva-Maria Collnot, Maike Windbergs & Claus-Michael Lehr

  5. Department of Pharmacy, Kohat University of Science and Technology, Kohat, KPK, Pakistan

    Saeed Ahmad Khan

Authors
  1. Hussain Ali
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  2. Benno Weigmann
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  3. Eva-Maria Collnot
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  4. Saeed Ahmad Khan
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  5. Maike Windbergs
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  6. Claus-Michael Lehr
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Corresponding author

Correspondence to Claus-Michael Lehr.

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Ali, H., Weigmann, B., Collnot, EM. et al. Budesonide Loaded PLGA Nanoparticles for Targeting the Inflamed Intestinal Mucosa—Pharmaceutical Characterization and Fluorescence Imaging. Pharm Res 33, 1085–1092 (2016). https://doi.org/10.1007/s11095-015-1852-6

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  • DOI: https://doi.org/10.1007/s11095-015-1852-6

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