Attenuation of lipid levels in triton induced hyperlipidemia rats through rosuvastatin calcium nanoparticles: Pharmacokinetic and pharmacodynamic studies

Dudhipala, NR; Ettireddy, SR; Puchakayala, GR

doi:10.1016/j.chemphyslip.2021.105081

Cited by 7 publications

(4 citation statements)

References 48 publications

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“…To assess the generality of this method, the scope of quinoxalin-2(1H)-ones was firstly investigated (Scheme 2). A variety of N-substituted quinoxalin-2(1H)-ones, such as alkyl (3)(4)(5), ring alkyl (6), phenyl (7), benzyl (8), 2-oxo-2-phenylethyl (9), naphthyl (10) and ester (11)(12)(13), were all smoothly converted to the coupling products in 61-89% yields. The product 12 could be easily transformed into the antitumor agent, which demonstrated the practicability of this protocol.…”

Section: Resultsmentioning

confidence: 99%

“…[1][2][3][4] Introducing an aryl group into the framework of heterocycles is a long-standing research topic since it often results in changes in their physicochemical properties or biological activities (Scheme 1a). [5][6][7][8] So far, a number of synthetic strategies have been developed. The classical approach involves transitionmetal-catalyzed cross-coupling reactions, such as Suzuki-Miyaura, 9,10 Negishi, 11 Hiyama, 12,13 and Stille 14 reactions (Scheme 1b).…”

Section: Introductionmentioning

confidence: 99%

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Divergent C(sp²)–H arylation of heterocycles via organic photoredox catalysis

Ren

Cui

et al. 2022

Green Chem.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Divergent C(sp²)–H arylation of heterocycles via organic photoredox catalysis

Ren

Cui

et al. 2022

Green Chem.

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“…However, an insignificant change in ZP was observed (p > 0.05). The freezedrying process could modify the PS and the shape of the SLNs [50]. The increase in PS and PDI is due to nanoparticles aggregation due to lyophilization.…”

Section: Lyophilizationmentioning

confidence: 99%

Cyclodextrin Complexed Lipid Nanoparticles of Irbesartan for Oral Applications: Design, Development, and In Vitro Characterization

Dudhipala¹,

Ettireddy²,

Youssef

et al. 2021

Molecules

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Irbesartan (IR) is an angiotensin II receptor antagonist drug with antihypertensive activity. IR bioavailability is limited due to poor solubility and first-pass metabolism. The current investigation aimed to design, develop, and characterize the cyclodextrin(s) (CD) complexed IR (IR-CD) loaded solid lipid nanoparticles (IR-CD-SLNs) for enhanced solubility, sustained release behavior, and subsequently improved bioavailability through oral administration. Based on phase solubility studies, solid complexes were prepared by the coacervation followed by lyophilization method and characterized for drug content, inclusion efficiency, solubility, and in vitro dissolution. IR-CD inclusion complexes demonstrated enhancement of solubility and dissolution rate of IR. However, the dissolution efficiency was significantly increased with hydroxypropyl-βCD (HP-βCD) inclusion complex than beta-CD (βCD). SLNs were obtained by hot homogenization coupled with the ultrasonication method with IR/HP-βCD inclusion complex loaded into Dynasan 112 and glycerol monostearate (GMS). SLNs were evaluated for physicochemical characteristics, in vitro release, differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), and physical stability at room temperature for two months. The optimized SLNs formulation showed particle size, polydispersity index, zeta potential, assay, and entrapment efficiency of 257.6 ± 5.1 nm, 0.21 ± 0.03, −30.5 ± 4.1 mV, 99.8 ± 2.5, and 93.7 ± 2.5%, respectively. IR-CD-SLN and IR-SLN dispersions showed sustained release of IR compared to the IR-CD inclusion complexes. DSC results complimented PXRD results by the absence of IR endothermic peak. Optimized IR-CD complex, IR-SLN, and IR-CD-SLN formulations were stable for two months at room temperature. Thus, the current IR oral formulation may exhibit improved oral bioavailability and prolonged antihypertensive activity, which may improve therapeutic outcomes in the treatment of hypertension and heart failure.

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“…The mobile phase used was buffer (1.0 ml orthophosphoric into 1,000 ml water):acetonitrile:methanol (50:25:25, v/v). The flow rate was 1.0 ml/min and injection volume was 100 µl with a total run time of 20 min [ 29 ]. Additionally, the assessment of lipid profile was measured at the day 15 and the day 30 (the end of the experiment).…”

Section: Methodsmentioning

confidence: 99%

Development and assessment of nano drug delivery systems for combined delivery of rosuvastatin and ezetimibe

Metwally,

El-Zawahry,

Ali

et al. 2024

Korean J Physiol Pharmacol

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Worldwide, cardiovascular disease is the main cause of death, which accordingly increased by hyperlipidemia. Hyperlipidemia therapy can include lifestyle changes and medications to control cholesterol levels. Statins are the medications of the first choice for dealing with lipid abnormalities. Rosuvastatin founds to control high lipid levels by hindering liver production of cholesterol and to achieve the targeted levels of low-density lipoprotein cholesterol, another lipid lowering agents named ezetimibe may be used as an added therapy. Both rosuvastatin and ezetimibe have low bioavailability which will stand as barrier to decrease cholesterol levels, because of such depictions, formulations of this combined therapy in nanotechnology will be of a great assistance. Our study demonstrated preparations of nanoparticles of this combined therapy, showing their physical characterizations, and examined their behavior in laboratory conditions and vivo habitation. The mean particle size was uniform, polydispersity index and zeta potential of formulations were found to be in the ranges of (0.181–0.72) and (–13.4 to –6.24), respectively. Acceptable limits of entrapment efficiency were affirmed with appearance of spherical and uniform nanoparticles. In vitro testing showed a sustained release of drug exceeded 90% over 24 h. In vivo study revealed an enhanced dissolution and bioavailability from loaded nanoparticles, which was evidenced by calculated pharmacokinetic parameters using triton for hyperlipidemia induction. Stability studies were performed and assured that the formulations are kept the same up to one month. Therefore, nano formulations is a suitable transporter for combined therapy of rosuvastatin and ezetimibe with improvement in their dissolution and bioavailability.

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Attenuation of lipid levels in triton induced hyperlipidemia rats through rosuvastatin calcium nanoparticles: Pharmacokinetic and pharmacodynamic studies

Cited by 7 publications

References 48 publications

Divergent C(sp²)–H arylation of heterocycles via organic photoredox catalysis

Divergent C(sp²)–H arylation of heterocycles via organic photoredox catalysis

Cyclodextrin Complexed Lipid Nanoparticles of Irbesartan for Oral Applications: Design, Development, and In Vitro Characterization

Development and assessment of nano drug delivery systems for combined delivery of rosuvastatin and ezetimibe

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Attenuation of lipid levels in triton induced hyperlipidemia rats through rosuvastatin calcium nanoparticles: Pharmacokinetic and pharmacodynamic studies

Cited by 7 publications

References 48 publications

Divergent C(sp2)–H arylation of heterocycles via organic photoredox catalysis

Divergent C(sp2)–H arylation of heterocycles via organic photoredox catalysis

Cyclodextrin Complexed Lipid Nanoparticles of Irbesartan for Oral Applications: Design, Development, and In Vitro Characterization

Development and assessment of nano drug delivery systems for combined delivery of rosuvastatin and ezetimibe

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Product

Resources

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Divergent C(sp²)–H arylation of heterocycles via organic photoredox catalysis

Divergent C(sp²)–H arylation of heterocycles via organic photoredox catalysis