ArticlePharmaceutical research2014
CNS delivery and pharmacokinetic evaluations of DALDA analgesic peptide analog administered in Nano-sized oil-in-water emulsion formulation.
Article in Pharmaceutical research, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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The trial behind it
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Who cites it
6 citing papers in PubMed, 15 citations in OpenAlex.
- DHA-SBT-1214 Taxoid Nanoemulsion and Anti-PD-L1 Antibody Combination Therapy Enhances Antitumor Efficacy in a Syngeneic Pancreatic Adenocarcinoma Model.Molecular cancer therapeutics · 2019Article
- Challenging the CNS Targeting Potential of Systemically Administered Nanoemulsion Delivery Systems: a Case Study with Rapamycin-Containing Fish Oil Nanoemulsions in Mice.Pharmaceutical research · 2019Article
- Biodistribution and Pharmacokinetic Evaluations of a Novel Taxoid DHA-SBT-1214 in an Oil-in-Water Nanoemulsion Formulation in Naïve and Tumor-Bearing Mice.Pharmaceutical research · 2018Article
- Nanoemulsion formulation of a novel taxoid DHA-SBT-1214 inhibits prostate cancer stem cell-induced tumor growth.Cancer letters · 2017Article
- Mathematical Modeling and Experimental Validation of Nanoemulsion-Based Drug Transport across Cellular Barriers.Pharmaceutical research · 2017Article
- Analgesic efficacy and safety of DALDA peptide analog delivery to the brain using oil-in-water nanoemulsion formulation.Pharmaceutical research · 2014Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
Abstract
purposeAlthough neuro-active peptides are highly potent as central nervous system (CNS) therapeutics, their systemic delivery across the blood-brain barrier (BBB) is limited due to lack of permeability in the brain and rapid systemic metabolism. In this study, we aimed at enhancing the brain delivery and stability of chemically modified [D-Arg(2), Lys(4)]-dermorphin-(1-4)-amide)] (DALDA) peptide to achieve prolonged analgesic effects.
methodsThe C8-DALDA peptide analog was encapsulated in an oil-in-water nanoemulsion formulation made specifically with oils rich in omega-3 rich polyunsaturated fatty acid (PUFA) to enhance CNS availability. The nanoemulsion formulation was administered systemically in CD-1 mice and qualitative and quantitative biodistribution was evaluated. We have also examined the effect of curcumin, which is known to down-regulate efflux transporters and inhibit systemic metabolism, on the pharmacokinetic properties of the peptide.
resultsQualitative and quantitative biodistribution and pharmacokinetic studies in mice clearly demonstrated improved plasma and brain exposure of modified DALDA when administered in nanoemulsion, thereby providing an exciting opportunity towards improved efficacy and/or lowered dose of the peptide. The various dosing regimens tested for modified DALDA solution and curcumin nanoemulsion directed towards a novel combination strategy for improved systemic delivery of peptides across the BBB.
conclusionsEncapsulation of the drug in PUFA nanoemulsion is an effective strategy for delivery of peptides. This work provides a novel combination strategy for improved delivery of peptides to the brain.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.