ArticleDrug delivery and translational research2022
Nanostructured lipid carriers of isradipine for effective management of hypertension and isoproterenol induced myocardial infarction.
Article in Drug delivery and translational research, 2022. 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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Who cites it
6 citing papers in PubMed, 13 citations in OpenAlex.
- Application of nanotherapy in cardiovascular diseases featuring novel pharmacological mechanisms and drug delivery strategies.Discover nano · 2026Review
- Nanoparticles-based phototherapy systems: molecular mechanisms and clinical applications.Signal transduction and targeted therapy · 2026Review
- Review
- In vivo evaluation of nanostructured lipid carrier systems (NLCs) in mice bearing prostate cancer tumours.Drug delivery and translational research · 2023Article
- Neurogenic Hypertension, the Blood-Brain Barrier, and the Potential Role of Targeted Nanotherapeutics.International journal of molecular sciences · 2023Review
- mRNA therapy for myocardial infarction: A review of targets and delivery vehicles.Frontiers in bioengineering and biotechnology · 2022Review
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The objective of the present paper is to formulate nanostructured lipid carriers (NLCs) of a calcium channel blocker, isradipine, to enhance its oral bioavailability and prolong its antihypertensive effect apart from evaluating efficacy of the formulation in isoproterenol induced myocardial infarction in rats. Formulation was optimized using quality by design (QbD)-based approach. Three factors i.e., total lipid concentration (%), homogenization pressure (bar), and number of cycles were optimized through Box-Behnken design to estimate their effect on critical quality attributes (CQAs) viz., size (nm), % entrapment efficiency, and in vitro % drug release which were found to be 80.9 ± 1.7 nm, 83.51 ± 2.15%, and 83.3 ± 3.86% after 24 h, respectively. In vivo pharmacokinetic study indicated 4.207 and 1.907 times increase in the oral bioavailability of optimized nanostructured lipid carrier without and with cycloheximide (lymphatic transport inhibitor), respectively. Treatment with ISO (isoproterenol) significantly diverges the levels of antioxidant marker, TBARS (thiobarbituric acid), and ultrastructure of the cardiac tissue indicating significant myocardial damage. Pretreatment of nanostructured lipid carrier of isradipine (ISD-NLCs) significantly prevented the antioxidant status and ultrastructural changes in the heart. In conclusion, this study confirms that optimized NLCs can substantially improve oral bioavailability of isradipine and presents a promising strategy in the management of hypertension for longer duration of time apart from demonstrating its preclinical efficacy in cardioprotection.
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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.