ArticleJournal of controlled release : official journal of the Controlled Release Society2017
Intranasal delivery of N-terminal modified leptin-pluronic conjugate for treatment of obesity.
Article in Journal of controlled release : official journal of the Controlled Release Society, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
14 citing papers in PubMed, 37 citations in OpenAlex.
- Whispering Through the Barrier: Signaling Interfaces for Peripheral Regulation of Brain Function in Obesity.Journal of neurochemistry · 2025Review
- Nasal Residence Depending on the Administered Dosage Form: Impact of Formulation Type on the In Vivo Nasal Retention Time of Drugs in Rats.Pharmaceutics · 2025Article
- Leptin signaling in the dorsomedial hypothalamus couples breathing and metabolism in obesity.Cell reports · 2023Article
- Anti-Obesity Drug Delivery Systems: Recent Progress and Challenges.Pharmaceutics · 2023Review
- Regulation of Metabolic Health by an "Olfactory-Hypothalamic Axis" and Its Possible Implications for the Development of Therapeutic Approaches for Obesity and T2D.Cellular and molecular neurobiology · 2022Review
- Biomaterial-Based Therapeutic Strategies for Obesity and Its Comorbidities.Pharmaceutics · 2022Review
- Novel Noninvasive Approaches to the Treatment of Obesity: From Pharmacotherapy to Gene Therapy.Endocrine reviews · 2022Review
- Using nanotechnology to deliver biomolecules from nose to brain - peptides, proteins, monoclonal antibodies and RNA.Drug delivery and translational research · 2022Article
- Leptin in Leanness and Obesity: JACC State-of-the-Art Review.Journal of the American College of Cardiology · 2021Review
- Remodeling adipose tissue inflammasome for type 2 diabetes mellitus treatment: Current perspective and translational strategies.Bioengineering & translational medicine · 2020Review
- Polymeric Carriers for Controlled Drug Delivery in Obesity Treatment.Trends in endocrinology and metabolism: TEM · 2019Review
- Drug Delivery Strategies for the Treatment of Metabolic Diseases.Advanced healthcare materials · 2019Review
- Leptin Signaling in the Control of Metabolism and Appetite: Lessons from Animal Models.Journal of molecular neuroscience : MN · 2018Review
- Surface-Modified Nanocarriers for Nose-to-Brain Delivery: From Bioadhesion to Targeting.Pharmaceutics · 2018Review
Corrections and comments
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Authors and funding
10 authors at 5 institutions in 2 countries.
Funding
Abstract
Leptin is an adipocyte-secreted hormone that is delivered via a specific transport system across the blood-brain barrier (BBB) to the brain where it acts on the hypothalamus receptors to control appetite and thermogenesis. Peripheral resistance to leptin due to its impaired brain delivery prevents therapeutic use of leptin in overweight and moderately obese patients. To address this problem, we modified the N-terminal amine of leptin with Pluronic P85 (LepNP85) and administered this conjugate intranasally using the nose-to-brain (INB) route to bypass the BBB. We compared this conjugate with the native leptin, the N-terminal leptin conjugate with poly(ethylene glycol) (LepNPEG5K), and two conjugates of leptin with Pluronic P85 attached randomly to the lysine amino groups of the hormone. Compared to the random conjugates of leptin with P85, LepNP85 has shown higher affinity upon binding with the leptin receptor, and similarly to native hormone activated hypothalamus receptors after direct injection into brain. After INB delivery, LepNP85 conjugate was transported to the brain and accumulated in the hypothalamus and hippocampus to a greater extent than the native leptin and LepNPEG5K and activated leptin receptors in hypothalamus at lower dose than native leptin. Our work suggests that LepNP85 can access the brain directly after INB delivery and confirms our hypothesis that the improvement in brain accumulation of this conjugate is due to its enhanced brain absorption. In conclusion, the LepNP85 with optimized conjugation chemistry is a promising candidate for treatment of obesity.
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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.