Formulation of Polymeric Multicomponent Systems Containing Cardiovascular APIs

Sha’at, Fawzia; Pavaloiu, Ramona Daniela; Salceanu, Daniela Crina; Hlevca, Cristina; Nechifor, Gheorghe

doi:10.37358/mp.18.1.4976

Cited by 5 publications

(7 citation statements)

References 15 publications

(19 reference statements)

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“…The nanoprecipitation method demonstrated the efficient capability of encapsulating such APIs inside PLGA NPs. In a previous study [15], formulations with AML-VAL loaded in a polymeric matrix of higher concentrations of PLGA were assessed and for which were demonstrated good EE(%). In this study we investigate formulations with a smaller amount of PLGA matrix in order to obtain better characteristics.…”

Section: Resultsmentioning

confidence: 99%

Evaluation of AML-VAL Nanoparticles as Combined Therapy in Cardiovascular Disease

Sha’at¹,

Pavaloiu²,

Salceanu³

et al. 2018

Mat.Plast.

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The main aim of this study was to investigate a mixture of two poorly water-soluble active pharmaceutical ingredients (APIs): an angiotensin II receptor antagonist (valsartan) and a calcium channel blocker (amlodipine besylate), chosen in a fixed-dose, in order to obtain new polymeric nanoparticles (NPs) for cardiovascular diseases treatment. NPs were prepared via nanoprecipitation method using poly (D,L-lactide-co-glycolide) (PLGA) as matrix and Pluronic F127 as stabilizer. Three formulations were investigated with different ratios of AML:VAL:PLGA (1:16:5, 1:16:7.5 and 1:16:10). Particle size, polydispersity index and zeta-potential analyses were performed to characterize and optimize the formulation. The in vitro drug release study was determined by using a dialysis membrane method under sink conditions. All NPs loaded with both APIs showed nano-size, negative potential, a high homogeneity and a slow drugs release in physiological environment.

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Section: Resultsmentioning

confidence: 99%

Evaluation of AML-VAL Nanoparticles as Combined Therapy in Cardiovascular Disease

Sha’at¹,

Pavaloiu²,

Salceanu³

et al. 2018

Mat.Plast.

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“…A mixture of two cardiovascular drugs-valsartan (an angiotensin II receptor antagonist drug) and amlodipine besylate (a calcium channel blocker)-was loaded in polymeric nanoparticles. The formulation of PLGA NPs loaded with valsartan-amlodipine (PLGA:valsartan:amlodipine besylate = 10:16:1) was established in prevoius studies [8,9] as optimal having high EE (%) for both drugs (91.98 ± 0.18% for valsartan and 82.54 ± 0.12% for amlodipine besylate, nano-metric particle size (140.4 ± 1.34 nm) and narrow dispersity (polydispersity index = 0.108 ± 0.03). The cellular uptake of polymeric nanoparticles was investigated by incubating adherent mouse embryo fibroblasts (NIH 3T3) with a suspension of PLGA NPs loaded with valsartanamlodipine.…”

Section: Resultsmentioning

confidence: 99%

“…PLGA NPs loaded with valsartan-amlodipine were synthesized via nanoprecipitation method according to previous reports [8,9]. Briefly, PLGA and cardiovascular drugs were dissolved in acetone (organic phase), while Pluronic-F127 was dissolved in distilled water (aqueous phase).…”

Section: Preparation Of Plga Nps Loaded With Valsartan-amlodipinementioning

confidence: 99%

Intracellular Uptake Study of Polymeric Nanoparticles Loaded with Cardiovascular Drugs Using Confocal Laser Scanning Microscopy

Păvăloiu

Sha’at

et al. 2020

The 24th International Electronic Conference on Synthetic Organic Chemistry

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Confocal laser scanning microscopy (CSLM) is a powerful microscopic tool that gives valuable morphological and functional information within cells and tissues. CLSM is non-invasive, with high-contrast scanning, a simple and fast sample preparation procedure as well as easy operation. The aim of this paper was to study the intracellular uptake of polymeric nanoparticles loaded with cardiovascular drugs using confocal laser scanning microscopy. Polymeric nanoparticles were prepared via nanoprecipitation method using poly(lactide-co-glycolide) (PLGA) as biodegradable polymeric matrix and Pluronic F127 as a stabilizer. A mixture of two cardiovascular drugs-valsartan (an angiotensin II receptor antagonist drug) and amlodipine besylate (a calcium channel blocker)-was loaded in polymeric nanoparticles. The prepared polymeric nanoparticles had sizes lower than 300 nm and narrow dispersity. The cellular uptake of polymeric nanoparticles was investigated by incubating adherent mouse embryo fibroblasts (NIH 3T3) with a suspension of nanoparticles (stained previously with phthalocyanine) at three different time points. Targeted cell compartments were labeled with two fluorophores: Rhodamine B (membrane stain) and Hoechst (nucleic acid stain). Live cell imaging was performed using a confocal microscope Zeiss LSM710 with Zeiss PALM microdissection system. The intracellular uptake of polymeric nanoparticles was revealed by confocal laser scanning microscopy for each incubation time. The results suggest a possible mechanism of endocytosis and clearly a vesicularbased accumulation of the nanoparticles in the cytoplasmatic compartments.

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“…Polymers selected to be used as a drug carrier should share following features: be biocompatible; do not interact with the drug; provide a platform for appropriate drug-eluting kinetics; behave biologically inert after the drug has been completely eluted, and be mechanically stable at longterm in the dynamics of coronary circulation milieu. Various permanent (biostable) and biodegradable polymers have been used on DES platforms with various results which are still in testing in clinical trials [7][8][9][10][11], (table 1).…”

Section: Experimental Part Des Versus Bmsmentioning

confidence: 99%

Aspects of Heart Failure in Patients with Ischemic Heart Disease after Percutaneous Coronary Revascularization with Polymer-coated Drug-Eluting Stents versus Bare-Metal Stents

Tudoran¹,

Tudoran²,

Ciocârlie³

et al. 2019

Mat.Plast.

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Percutaneous coronary revascularization (PCR) with polymer-coated drug-eluting stents (DES) or bare-metal stents (BMS) is considered the standard therapy in advanced ischemic heart disease (IHD). Despite revascularisation, many of these patients subsequently develop heart failure with reduced ejection fraction (HFrEF). We analysed 51 patients with IHD, treated by PCR and insertion of DES and/or BMS who later developed HFrEF. Patients with DES where more likely women, of younger age and a higher incidence of diabetes mellitus compared to patients with BMS who were generally men, of older age and had more frequently acute ST-elevation myocardial infarction (STEMI) as indication for PCR. Although patients with DES had more severe IHD, their EF was higher, possibly due to the benefits offered by the DES.

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Formulation of Polymeric Multicomponent Systems Containing Cardiovascular APIs

Cited by 5 publications

References 15 publications

Evaluation of AML-VAL Nanoparticles as Combined Therapy in Cardiovascular Disease

Evaluation of AML-VAL Nanoparticles as Combined Therapy in Cardiovascular Disease

Intracellular Uptake Study of Polymeric Nanoparticles Loaded with Cardiovascular Drugs Using Confocal Laser Scanning Microscopy

Aspects of Heart Failure in Patients with Ischemic Heart Disease after Percutaneous Coronary Revascularization with Polymer-coated Drug-Eluting Stents versus Bare-Metal Stents

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