Docosahexaenoic acid-mediated, targeted and sustained brain delivery of curcumin microemulsion
Shinde RL, Devarajan PV
Drug delivery · 61 citations
Review labels
Neutral facts our review recorded about how this study was done. They describe method, never whether we like the result.
How it was studied
- Design
- Animal study (classified by our AI screen)
- Studied in
- People, plus animal or lab work
- Main outcome
- Mechanisms only
Who paid for it
- Funding
- Independent funding
- Government
- University Grants Commission
Based on 1 listed funder(s) and full-text disclosure statement.
Publication
- Published
- 2017-01-01 · Drug Deliv · vol. 24 · issue 1 · pp. 152–161
- Publisher
- Taylor & Francis
- Cited
- 88 citations · more than 95% of similar papers · 4.2× the field average
- Impact
- Top 10% most cited in its field
- References
- 51 works
- Access
- Open access (journal) · CC-BY
- Research areas
- RNA Interference and Gene Delivery · Curcumin's Biomedical Applications · Advanced Drug Delivery Systems
- Keywords
- Curcumin, Nasal administration, Pharmacology, Docosahexaenoic acid, Cmax, IC50, Cytotoxicity, Chemistry, Drug delivery, In vivo, Medicine, Bioavailability, In vitro, Biochemistry, Fatty acid, Polyunsaturated fatty acid, Biology, Biotechnology, Organic chemistry
- MeSH
- blood-brain barrier, brain, cell line, tumor, animals, humans, rats, rats, sprague-dawley, glioblastoma, brain neoplasms, curcumin, docosahexaenoic acids, emulsions, delayed-action preparations, drug delivery systems, administration, intranasal, chemistry, pharmaceutical, male
2 authors
From IN
- Rajshree L. ShindeInstitute of Chemical Technology
- Padma V. Devarajan · correspondingInstitute of Chemical Technology
Abstract
We disclose microemulsions (ME) of curcumin (CUR) with docosahexaenoic acid (DHA)-rich oil (CUR DHA ME) for targeted delivery to the brain. MEs of CUR (5 mg/mL) with and without DHA-rich oil (CUR Capmul ME) suitable for intravenous and intranasal administration exhibited negative zeta potential, globule size max than CUR solution. Furthermore, high and sustained concentration was demonstrated even at 24 h, which was 8- and 2-fold higher than CUR solution and CUR Capmul ME, respectively. Brain concentrations following intranasal administration were, however, substantially higher as evident from higher Cmax and AUC and sustained compared to corresponding intravenous formulations signifying nose to brain targeting. The high brain concentration of CUR DHA ME is ascribed to the targeting efficiency enabled by DHA-mediated transport across the blood-brain barrier (BBB). Histopathological and nasal toxicity confirmed safety of the MEs. Concentration-dependent cytotoxicity in vitro, on human glioblastoma U-87MG cell line was observed with CUR DHA MEs and with the blank DHA ME, implying anticancer potential of DHA. The dramatically low IC50 value of CUR DHA ME (3.755 ± 0.24 ng/mL) is therefore attributed to the synergistic effect of CUR and DHA in the ME. The CUR concentration achieved with CUR DHA ME at 24 h which translated to >66-fold(intranasal) and >21-fold (intravenous) the IC50 value in the U-87MG cell line suggests great promise of CUR DHA ME for therapy of brain cancer by both routes.
Abstract via Europe PMC. Copyright remains with the authors or publisher (CC BY).
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