The antihypertensive effect of orally administered nifedipine‐loaded nanoparticles in spontaneously hypertensive rats
Open accessAbstract
The therapeutic use of nifedipine is limited by the rapidity of the onset of its action and its short biological half‐life. In order to produce a form devoid of these disadvantages we made nanoparticles of nifedipine from three different polymers, poly‐ɛ‐caprolactone (PCL), polylactic and glycolic acid (1:1) copolymers (PLAGA), and Eudragit RL/RS (Eudragit). Nifedipine in polyethylene glycol 400 (PEG) solution was used as a control. The average diameters of the nanoparticles ranged from 0.12 to 0.21 μm; the encapsulation ratio was 82% to 88%. In spontaneously hypertensive rats (SHR), the initial rapid fall in systolic arterial blood pressure following oral administration of nifedipine in PEG solution (from 193 ± 3 to 102 ± 2 mmHg) was not seen following administration of the same dose in Eudragit nanoparticles (from 189 ± 2 to 156 ± 2 mmHg); with PCL and PLAGA nanoparticles the initial fall in blood pressure was significantly reduced (nadirs PCL 124 ± 2 and PLAGA 113 ± 2 mmHg). Ten hours following administration, blood pressure in rats administered the nifedipine/PEG preparation had returned to normal (183 ± 3 mmHg) whereas that of animals given nifedipine in nanoparticles (PCL 170 ±3, PLAGA 168 ± 2, Eudragit 160 ±3 mmHg) was still significantly reduced. All of the nanoparticle dosage forms decreased C max and increased T max and the mean residence time (MRT) values. Relative bioavailability was significantly increased with Eudragit nanoparticles compared to the nifedipine/PEG solution. There was an inverse linear correlation between the fall in blood pressure and plasma nifedipine concentration with all preparations. The nanoparticle nifedipine preparations represent sustained release forms with increased bioavailability, a less pronounced initial antihypertensive effect and a long‐lasting action.
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Nifedipine encapsulated in PLGA, PCL, and eudragit nanoparticles produced significant and sustained reduction in blood pressure.
“In another study, Kim et al. reported a significant and sustained reduction in blood pressure using nifedipine encapsulated in PLGA, PCL, and eudragit nanoparticles.143”
From Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles (2019) · cites this paper as [143]
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- Authors
- Kim, Y. I., Fluckiger, L., Hoffman, M., Lartaud‐Idjouadiene, I., Atkinson, J., & Maincent, T.
- Affiliations
- Université Henri Poincaré (FR)
- Corresponding author
- Maincent, Thilippe
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 1997-01
- Volume
- 120
- Issue
- 3
- Pages
- 399-404
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- PMC
- PMC1564474
- OpenAlex
- W2087338639
- Cited by
- 61
- References
- 23
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 2 · 2023: 4 · 2022: 4 · 2021: 7 · 2020: 3 · 2019: 5 · 2018: 4 · 2017: 3 · 2016: 4 · 2014: 1 · 2012: 2
- FWCI
- 2.25
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- British Journal of Pharmacology (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- nifedipine, nanoparticles, antihypertensive effect, sustained drug release, polycaprolactone, Eudragit, oral bioavailability, blood pressure, spontaneously hypertensive rats, drug delivery, plasma concentration
- MeSH terms
- Polylactic Acid-Polyglycolic Acid Copolymer, Acrylic Resins, Animals, Antihypertensive Agents, Blood Pressure, Calcium Channel Blockers, Caprolactam, Chemistry, Physical, Dialysis, Half-Life, Hypertension, Male, Microspheres, Nifedipine, Particle Size, Polyglycolic Acid, Polymers, Rats, Inbred SHR, Lactic Acid, Area Under Curve, Rats, Chemical Phenomena
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