Curcumin-loaded self-nanomicellizing solid dispersion system: part I: development, optimization, characterization, and oral bioavailability

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dc.contributor.authorParikh, A.
dc.contributor.authorKathawala, K.
dc.contributor.authorSong, Y.
dc.contributor.authorZhou, X.F.
dc.contributor.authorGarg, S.
dc.date.issued2018
dc.description.abstractCurcumin (CUR) is considered as one of the most bioactive molecules ever discovered from nature due to its proven anti-inflammatory and antioxidant in both preclinical and clinical studies. Despite its proven safety and efficacy, the clinical translation of CUR into a useful therapeutic agent is still limited due to its poor oral bioavailability. To overcome its limitation and enhance oral bioavailability by improving its aqueous solubility, stability, and intestinal permeability, a novel CUR formulation (NCF) was developed using the self-nanomicellizing solid dispersion strategy. From the initial screening of polymers for their potential to improve the solubility and stability, Soluplus (SOL) was selected. The optimized NCF demonstrated over 20,000-fold improvement in aqueous solubility as a result of amorphization, hydrogen bonding interaction, and micellization determined using differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, Fourier transform infrared spectroscopy, nuclear magnetic resonance, dynamic light scattering, and transmission electron microscopy. Moreover, the greater stabilizing effect in alkaline pH and light was observed. Furthermore, significant enhancement of dissolution and permeability of CUR across everted sacs of rat small intestine were noticed. Pharmacokinetic studies demonstrated that the oral bioavailability of CUR was increased 117 and 17-fold in case of NCF and physical mixture of CUR and SOL compared to CUR suspension. These results suggest NCF identified as a promising new approach for repositioning of CUR for pharmaceutical application by enhancing the oral bioavailability of CUR. The findings herein stimulate further in vivo evaluations and clinical tests of NCF.
dc.description.statementofresponsibilityAnkit Parikh, Krishna Kathawala, Yunmei Song, Xin-Fu Zhou and Sanjay Garg
dc.identifier.citationDrug Delivery and Translational Research, 2018; 8(5):1389-1405
dc.identifier.doi10.1007/s13346-018-0543-3
dc.identifier.issn2190-393X
dc.identifier.issn2190-3948
dc.identifier.orcidZhou, X.F. [0000-0002-8687-0175]
dc.identifier.urihttps://hdl.handle.net/2440/132715
dc.language.isoen
dc.publisherSpringer
dc.rights© 2018, Controlled Release Society
dc.source.urihttps://doi.org/10.1007/s13346-018-0543-3
dc.subjectIntestine, Small
dc.subject.meshIntestine, Small
dc.subject.meshAnimals
dc.subject.meshRats
dc.subject.meshCurcumin
dc.subject.meshAdministration, Oral
dc.subject.meshDrug Compounding
dc.subject.meshDrug Stability
dc.subject.meshBiological Availability
dc.subject.meshMicelles
dc.subject.meshParticle Size
dc.subject.meshPermeability
dc.subject.meshNanostructures
dc.subject.meshMale
dc.titleCurcumin-loaded self-nanomicellizing solid dispersion system: part I: development, optimization, characterization, and oral bioavailability
dc.typeJournal article
pubs.publication-statusPublished

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