High amount of lecithin facilitates oral delivery of a poorly soluble pyrazoloquinolinone ligand formulated in lipid nanoparticles: Physicochemical, structural and pharmacokinetic performances

Mitrović, Jelena R.; Divović-Matović, Branka; Knutson, Daniel E; Petković, Miloš; Djorović, Djordje; Randjelović, Danijela; Dobričić, Vladimir; Đoković, Jelena; Lunter, Dominique Jasmin; Cook, James M.; Savić, Miroslav M.; Savić, Snežana

doi:10.1016/j.ijpharm.2023.122613

Cited by 5 publications

(2 citation statements)

References 42 publications

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“…In our opinion, nanostructured lipid carriers offer an additional opportunity to efficiently target brain tissue—not only after parenteral, but also oral administration (cf. [ 175 ] in press).…”

Section: Discussionmentioning

confidence: 99%

Parenteral Lipid-Based Nanoparticles for CNS Disorders: Integrating Various Facets of Preclinical Evaluation towards More Effective Clinical Translation

et al. 2023

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Contemporary trends in combinatorial chemistry and the design of pharmaceuticals targeting brain disorders have favored the development of drug candidates with increased lipophilicity and poorer water solubility, with the expected improvement in delivery across the blood–brain barrier (BBB). The growing availability of innovative excipients/ligands allowing improved brain targeting and controlled drug release makes the lipid nanocarriers a reasonable choice to overcome the factors impeding drug delivery through the BBB. However, a wide variety of methods, study designs and experimental conditions utilized in the literature hinder their systematic comparison, and thus slows the advances in brain-targeting by lipid-based nanoparticles. This review provides an overview of the methods most commonly utilized during the preclinical testing of liposomes, nanoemulsions, solid lipid nanoparticles and nanostructured lipid carriers intended for the treatment of various CNS disorders via the parenteral route. In order to fully elucidate the structure, stability, safety profiles, biodistribution, metabolism, pharmacokinetics and immunological effects of such lipid-based nanoparticles, a transdisciplinary approach to preclinical characterization is mandatory, covering a comprehensive set of physical, chemical, in vitro and in vivo biological testing.

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Section: Discussionmentioning

confidence: 99%

Parenteral Lipid-Based Nanoparticles for CNS Disorders: Integrating Various Facets of Preclinical Evaluation towards More Effective Clinical Translation

et al. 2023

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“…The Mitrovic team demonstrated the enhanced cellular uptake of loaded DK-I-60-3 oral lipid nanoparticles due to their increased affinity and bio-adhesion to the intestinal wall by pharmacokinetic studies. 9 Furthermore, the mixed micelles formed by lipid degradates and bile salts in vivo were found to enhance drug permeability and absorption. Therefore, pharmacokinetic research on lipid-based drug formulations should broaden their focus beyond the free drug itself and consider the dynamic changes occurring within the drug-lipid excipient mixtures in vivo.…”

Section: Introductionmentioning

confidence: 99%

Revealing Changes in Celecoxib Nanostructured Lipid Carrier’s Bioavailability Using Hyaluronic Acid as an Enhancer by HPLC-MS/MS

Zhu,

Chen,

Yang

et al. 2024

DDDT

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Purpose Oral drug administration is the most common and convenient route, offering good patient compliance but drug solubility limits oral applications. Celecoxib, an insoluble drug, requires continuous high-dose oral administration, which may increase cardiovascular risk. The nanostructured lipid carriers prepared from drugs and lipid excipients can effectively improve drug bioavailability, reduce drug dosage, and lower the risk of adverse reactions. Methods In this study, we prepared hyaluronic acid-modified celecoxib nanostructured lipid carriers (HA-NLCs) to improve the bioavailability of celecoxib and reduce or prevent adverse drug reactions. Meanwhile, we successfully constructed a set of FDA-compliant biological sample test methods to investigate the pharmacokinetics of HA-NLCs in rats. Results The pharmacokinetic analysis confirmed that HA-NLCs significantly enhanced drug absorption, resulting in an AUC 0-t 1.54 times higher than the reference formulation (Celebrex ® ). Moreover, compared with unmodified nanostructured lipid carriers (CXB-NLCs), HA-NLCs enhance the retention time and improve the drug’s half-life in vivo. Conclusion HA-NLCs significantly increased the bioavailability of celecoxib. The addition of hyaluronic acid prolonged the drug’s in vivo duration of action and reduced the risk of cardiovascular adverse effects associated with the frequent administration of oral celecoxib.

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QbD-driven development of phospholipid-embedded lipidic nanocarriers of raloxifene: extensive in vitro and in vivo evaluation studies

Pant,

Sharma,

Saini

et al. 2023

Drug Deliv. and Transl. Res.

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High amount of lecithin facilitates oral delivery of a poorly soluble pyrazoloquinolinone ligand formulated in lipid nanoparticles: Physicochemical, structural and pharmacokinetic performances

Cited by 5 publications

References 42 publications

Parenteral Lipid-Based Nanoparticles for CNS Disorders: Integrating Various Facets of Preclinical Evaluation towards More Effective Clinical Translation

Parenteral Lipid-Based Nanoparticles for CNS Disorders: Integrating Various Facets of Preclinical Evaluation towards More Effective Clinical Translation

Revealing Changes in Celecoxib Nanostructured Lipid Carrier’s Bioavailability Using Hyaluronic Acid as an Enhancer by HPLC-MS/MS

QbD-driven development of phospholipid-embedded lipidic nanocarriers of raloxifene: extensive in vitro and in vivo evaluation studies

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