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Solid Dispersion of Ursolic Acid in Gelucire 50/13: a Strategy to Enhance Drug Release and Trypanocidal Activity
- Source :
- Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual), Universidade de São Paulo (USP), instacron:USP
- Publication Year :
- 2012
- Publisher :
- Springer Science and Business Media LLC, 2012.
-
Abstract
- Solid dispersions (SDs) are an approach to increasing the water solubility and bioavailability of lipophilic drugs such as ursolic acid (UA), a triterpenoid with trypanocidal activity. In this work, Gelucire 50/13, a surfactant compound with permeability-enhancing properties, and silicon dioxide, a drying adjuvant, were employed to produce SDs with UA. SDs and physical mixtures (PMs) in different drug/carrier ratios were characterized and compared using differential scanning calorimetry, hot stage microscopy, Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), particle size, water solubility values, and dissolution profiles. Moreover, LLC-MK2 fibroblast cytotoxicity and trypanocidal activity evaluation were performed to determine the potential of SD as a strategy to improve UA efficacy against Chagas disease. The results demonstrated the conversion of UA from the crystalline to the amorphous state through XRD. FTIR experiments provided evidence of intermolecular interactions among the drug and carriers through carbonyl peak broadening in the SDs. These findings helped explain the enhancement of water solubility from 75.98 μg/mL in PMs to 293.43 μg/mL in SDs and the faster drug release into aqueous media compared with pure UA or PMs, which was maintained after 6 months at room temperature. Importantly, improved SD dissolution was accompanied by higher UA activity against trypomastigote forms of Trypanosoma cruzi, but not against mammalian fibroblasts, enhancing the potential of UA for Chagas disease treatment.
- Subjects :
- Trypanosoma cruzi
Biological Availability
Pharmaceutical Science
Aquatic Science
Permeability
Fats
Surface-Active Agents
chemistry.chemical_compound
Differential scanning calorimetry
X-Ray Diffraction
Ursolic acid
Spectroscopy, Fourier Transform Infrared
Drug Discovery
Organic chemistry
Chagas Disease
Particle Size
Solubility
Dissolution
Ecology, Evolution, Behavior and Systematics
Trypanocidal agent
Drug Carriers
Aqueous solution
Calorimetry, Differential Scanning
Ecology
Chemistry
Water
ÁCIDOS
General Medicine
Fibroblasts
Silicon Dioxide
Trypanocidal Agents
Triterpenes
Bioavailability
Drug carrier
Oils
Agronomy and Crop Science
Research Article
Nuclear chemistry
Subjects
Details
- ISSN :
- 15309932
- Volume :
- 13
- Database :
- OpenAIRE
- Journal :
- AAPS PharmSciTech
- Accession number :
- edsair.doi.dedup.....958fc3d557a3bf9973dfaa028180e4f3