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Published on: January 5, 2017
Cortisone-loaded stearoyl ascorbic acid based nanostructured lipid carriers alleviate inflammatory changes in
Rakesh Kumar Mishra1, Anas Ahmad2, Ajay Kumar1
1Institute of Nano Science and Technology, Habitat Centre, Phase - 10, Sector 64, Mohali, Punjab 160062, India.
This study developed novel nanostructured lipid carriers (NLCs) loaded with cortisone (CRT) to treat ulcerative colitis. The CRT-loaded NLCs effectively reduced inflammation and disease severity in mice, offering a promising therapeutic strategy.
Area of Science:
- Nanotechnology
- Pharmacology
- Gastroenterology
Background:
- Ulcerative colitis is a chronic inflammatory bowel disease affecting the colon and rectum.
- Cortisone (CRT), a corticosteroid, has limited clinical potency due to physicochemical properties.
- Developing advanced drug delivery systems is crucial for managing inflammatory conditions like colitis.
Purpose of the Study:
- To assess the therapeutic efficacy of cortisone-loaded nanostructured lipid carriers (NLCs) in a mouse model of DSS-induced colitis.
- To formulate and characterize NLCs using safe, USFDA-approved materials for improved cortisone delivery.
- To evaluate the impact of CRT-loaded NLCs on inflammatory markers and colon histoarchitecture.
Main Methods:
- Formulation and characterization of 6-o-stearoyl ascorbic acid (SAA) based NLCs encapsulating cortisone (CRT).
- Assessment of NLCs' physical properties including hydrodynamic diameter, encapsulation efficacy, and morphology (TEM, AFM, SEM).
- Evaluation of blank NLCs' cytocompatibility and the therapeutic effect of CRT-loaded NLCs in DSS-induced colitis mice, measuring disease activity index, weight variation, colon damage, and inflammatory markers.
Main Results:
- Successfully prepared CRT-loaded NLCs with an average diameter of 182 nm and 81.14% encapsulation efficacy, exhibiting spherical morphology.
- Blank NLCs demonstrated cytocompatibility up to 500 μg/ml.
- CRT-loaded NLCs significantly ameliorated colitis symptoms, including reduced disease activity index and weight loss.
- Histological analysis showed improved colon architecture, restored goblet cells and mucin secretion, and suppressed pro-inflammatory cytokines.
- Treatment with CRT-loaded NLCs downregulated key inflammatory enzymes such as cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS).
Conclusions:
- CRT-loaded SAA-NLCs represent a viable and effective nanocarrier system for managing ulcerative colitis.
- The developed NLCs improve cortisone's therapeutic potential by enhancing its delivery and efficacy.
- This nanotechnology-based approach offers a promising strategy to overcome the limitations of conventional cortisone therapy for inflammatory bowel diseases.
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