Improvement in antihypertensive and antianginal effects of felodipine by enhanced absorption from PLGA nanoparticles optimized by factorial design
Abstract
Objective of the present investigation was to enhance the bioavailability of felodipine by targeting the M cells of Peyer's patches using PLGA nanoparticles (NPs). Felodipine exhibits poor bioavailability due to limited aqueous solubility and extensive first pass metabolism. NPs were prepared using nanoprecipitation and optimized by 3(2) factorial design. Particle size (PS) and entrapment efficiency (% EE) were dependent on Drug/PLGA ratio (X1) and Pluronic F-68 (X2) concentration. % EE, PS and Zeta potential for optimized batch were 91.56±3.21%, 161.3±2.23 nm and -25.7±2.52 mV respectively. DSC, XRD and FTIR studies confirmed compatibility of PLGA and drug. TEM image confirmed the spherical shape. The in vitro and ex vivo studies using rat stomach and intestinal segment confirmed sustained release from NPs. Pharmacodynamic studies in rats showed control of blood pressure and ECG changes for extended duration. Hence, NPs can be a suitable alternative to the current available therapy in hypertension and angina by enhancing the bioavailability.
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Felodipine encapsulated in PLGA NPs showed improved antihypertensive effects because of increased solubility and bioavailability.
“Furthermore, felodipine (calcium-channel blocker) encapsulated in PLGA NPs showed improved antihypertensive effects because of the increased solubility and bioavailability of the drug.140”
From Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles (2019) · cites this paper as [140]
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Retracted
- Authors
- Shah, U., Joshi, G., & Sawant, K.
- Affiliations
- Maharaja Sayajirao University of Baroda (IN)
- Corresponding author
- Sawant, Krutika
- Venue
- Materials Science and Engineering: C
- Publisher
- Elsevier BV
- Published
- 2014-02
- Volume
- 35
- Pages
- 153-163
- ISSN
- 0928-4931 (ISSN-L)
- OpenAlex
- W2043851849
- Cited by
- 76
- References
- 43
- Citations by year
- 2026: 1 · 2025: 7 · 2024: 9 · 2023: 8 · 2022: 9 · 2021: 6 · 2020: 9 · 2019: 10 · 2018: 2 · 2017: 3 · 2016: 5 · 2015: 4 · 2014: 3
- FWCI
- 2.41
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Materials Science and Engineering C (publishedVersion)
- PubMed (publishedVersion)
- Funders
- University Grants Commission
- Topics
- 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
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- felodipine, PLGA nanoparticles, Peyer's patches, M cells, bioavailability enhancement, antihypertensive effect, antianginal effect, nanoprecipitation, factorial design optimization, sustained drug release, oral drug delivery, first-pass metabolism, poloxamer 188, encapsulation efficiency, particle size
- MeSH terms
- Absorption, Polylactic Acid-Polyglycolic Acid Copolymer, Administration, Oral, Angina, Unstable, Animals, Antihypertensive Agents, Cardiotonic Agents, Diffusion, Drug Synergism, Factor Analysis, Statistical, Hypertension, Male, Polyglycolic Acid, Vasodilator Agents, Drug Design, Felodipine, Treatment Outcome, Rats, Sprague-Dawley, Lactic Acid, Rats, Nanocapsules
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