Cited by 76Advanced Drug Delivery SystemsDrug Solubulity and Delivery SystemsNanoparticle-Based Drug Delivery

Improvement in antihypertensive and antianginal effects of felodipine by enhanced absorption from PLGA nanoparticles optimized by factorial design

Shah, Umang, Joshi, Garima, Sawant, Krutika·2014·Materials Science and Engineering: C

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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Crossref · 10.1016/j.msec.2013.10.038

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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”

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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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