Combinatorial delivery of Ribociclib and green tea extract mediated nanostructured lipid carrier for oral delivery for the treatment of breast cancer synchronising in silico, in vitro, and in vivo studies

Ali, Sartaj; Annu, .; Alam, Meraj; Biswas, Largee; Yar, Mohammad Shahar; Mir, Showkat R.; Verma, Anita; Baboota, Sanjula; Ali, Javed

doi:10.1080/1061186x.2022.2104292

Cited by 9 publications

(6 citation statements)

References 68 publications

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“…To determine the crystallinity of the samples, different slits were set at 49 kilovolts. The scan was conducted from 5 to 80 degrees at two theta positions at 25 ± 2 °C with 65-70% humidity [34].…”

Section: Powdered X-ray Diffraction (Pxrd)mentioning

confidence: 99%

“…The sediment part is also separable, containing lipid-based components such as diglycerides, triglycerides, and insoluble fatty acids. The amount of ERVN was calculated in each layer, i.e., the aqueous layer and the lipidic layer [34].…”

Section: In-vitro Lipolysismentioning

confidence: 99%

“…The sharp characteristic peak of ERVN was missing in the ERVN-TPGS-loaded nanocarriers, indicating the absence of ERVN could be due to the encapsulation of ERVN inside the lipid matrix or might have changed it to an amorphous form. Sartaj and associates demonstrated the ribociclibloaded NLC, where the specific peak of the ribociclib was absent in the XRD of drug-loaded nanocarriers, attributing ribociclib entrapped in nanocarriers [34].…”

Section: Powder X-ray Diffraction (Pxrd)mentioning

confidence: 99%

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Fabrication of TPGS decorated Etravirine loaded lipid nanocarriers as a neoteric oral bioavailability enhancer for lymphatic targeting

Muheem,

Wasim,

Aldosari

et al. 2023

Preprint

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Etravirine (ERVN) is a potential NNRTI (non-nucleoside reverse transcriptase inhibitor) in treating HIV infection. It possesses extremely low oral bioavailability. The present research aims to optimize the formulation and characterization of TPGS-enriched ERVN-loaded lipid-based nanocarriers (LNCs) for HIV-infected patients. The formulation, ERVN-TPGS-LNCs, was optimized by CCRD using a modified-solvent evaporation process. Various characterization parameters of LNCs were evaluated, including globule size of 121.56 ± 2.174 nm, PDI of 0.172 ± 0.042, the zeta potential of -7.32 ± 0.021 mV, %EE of 94.42 ± 8.65% of ETR and %DL was 8.94 ± 0.759% of ERVN and spherical shape was revealed by TEM. PXRD was also performed to identify the crystallinity of the sample. In-vitro drug release showed % a cumulative drug release of 79.77 ± 8.35% at pH 1.2 and 83.23 ± 9.11% at pH 6.8, respectively, at the end of 48h compared to pure drug suspension (ERVN-S). Further, the intestinal permeation study and confocal microscope showed approximately ~3-fold and ~2-fold increased permeation in ERVN-TPGS-LNCs and ERVN-LNCs across the gut sac compared to ERVN-S. Hemolysis compatibility and lipolysis studies were performed to predict the in-vivo fate of the formulation. The pharmacokinetic study revealed a 3.13-fold increment in the relative bioavailability, which agrees with the ex-vivo studies, and lymphatic uptake was validated by using cycloheximide (CYHD) along with designed formulation, which leads to lowering AUC of ERVN-TPGS-LNCs. Thus, this study ensures that ERVN-TPGS-LNCs take lymphatic uptake to minimize the first-pass metabolism followed by improved oral bioavailability of EVN. Thus, the enhanced bioavailability of ERVN can reduce the high dose of ERVN to minimize the adverse effects related to dose-related burden.

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Section: Powdered X-ray Diffraction (Pxrd)mentioning

confidence: 99%

Section: In-vitro Lipolysismentioning

confidence: 99%

Section: Powder X-ray Diffraction (Pxrd)mentioning

confidence: 99%

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Fabrication of TPGS decorated Etravirine loaded lipid nanocarriers as a neoteric oral bioavailability enhancer for lymphatic targeting

Muheem,

Wasim,

Aldosari

et al. 2023

Preprint

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“…22 Nevertheless, only one LC-MS/MS analytical assay was reported for measuring ribociclib in rat plasma, which was limited by a relatively narrow calibration curve of 5-500 ng/mL, long run time of 13 min, and not utilizing a deuterated internal standard. 18 Also, other investigations that quantified ribociclib in rat plasma were either based on an LC/MS assay that did not show validation parameters in rat plasma 9,22 or a high-performance liquid chromatography HPLC method with ultraviolet (UV) detection that was not validated for ribociclib in rats. 10 Furthermore, some of the reported LC-MS/MS analytical assays had poor sensitivity 13,15,19 and narrow calibration curves, 14,16 which may limit their applicability for preclinical studies performed in rats.…”

Section: Introductionmentioning

confidence: 99%

“…Because of its moderate permeability and the feature of permeability‐controlled absorption, a physiologically based biopharmaceutics modeling revealed that ribociclib formulation optimization would be important to enhance its pharmacokinetics 8 . Formulations based on nanostructured lipidic carriers were recently developed for ribociclib to enhance its solubility, permeability, bioavailability potentially, and targeted therapy effect 9,10 . However, validating new ribociclib formulations requires performing preclinical pharmacokinetic studies in vivo, such as in rats.…”

Section: Introductionmentioning

confidence: 99%

Simple and rapid quantification of ribociclib in rat plasma by protein precipitation and LC‐MS/MS: An application to pharmacokinetics of ribociclib nanoparticles in rats

Alshogran,

Al‐Shdefat,

Hailat

2023

J Mass Spectrom

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Ribociclib is a cyclin‐dependent kinase (CDK4/6) inhibitor and is a standard of care for treating metastatic breast cancer. The drug has moderate oral bioavailability and exhibits permeability‐controlled absorption. Novel formulations to enhance ribociclib pharmacokinetics are being developed and tested in rats. This requires developing analytical assays for quantifying ribociclib monitoring in rat plasma. We present a fully validated, sensitive, and simple LC‐MS/MS method for measuring ribociclib in rat plasma. Ribociclib‐D6 was utilized as an internal standard, and a simple protein precipitation procedure with acetonitrile was used in sample preparation. Excellent assay linearity was observed over a standard curve concentration of 1.008–1027.624 ng/mL. Acceptable intra‐ and inter‐day accuracy and reproductivity were demonstrated for ribociclib quality controls (bias and CV% within ±15%). Complete extraction recovery of ribociclib was achieved, and a negligible matrix effect of analyte to internal standard ratio was observed. Ribociclib was stable at various conditions, including bench‐top, freeze–thaw, and short‐term stability. Overall, the presented method is simple, sensitive, accurate, and precise and was successfully applied to quantify ribociclib in plasma samples from a pharmacokinetic study of ribociclib suspension and nanoparticle formulation in rats.

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Application of nanoparticles in breast cancer treatment: a systematic review

Bourang,

Noruzpour,

Jahanbakhsh Godekahriz

et al. 2024

Naunyn-Schmiedeberg's Arch Pharmacol

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Combinatorial delivery of Ribociclib and green tea extract mediated nanostructured lipid carrier for oral delivery for the treatment of breast cancer synchronising in silico, in vitro, and in vivo studies

Cited by 9 publications

References 68 publications

Fabrication of TPGS decorated Etravirine loaded lipid nanocarriers as a neoteric oral bioavailability enhancer for lymphatic targeting

Fabrication of TPGS decorated Etravirine loaded lipid nanocarriers as a neoteric oral bioavailability enhancer for lymphatic targeting

Simple and rapid quantification of ribociclib in rat plasma by protein precipitation and LC‐MS/MS: An application to pharmacokinetics of ribociclib nanoparticles in rats

Application of nanoparticles in breast cancer treatment: a systematic review

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