Impact of drying on dissolution behavior of carvedilol-loaded sustained release solid dispersion: development and characterization

Halder, Shimul; Ahmed, Fairuza; Shuma, Madhabi Lata; Azad, M. A. K.; Kabir, Eva Rahman

doi:10.1016/j.heliyon.2020.e05026

Cited by 12 publications

(4 citation statements)

References 46 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Our finding of the kinetics profile ( Table 4 ) for the samples are also confirmed by the literature, as solid dispersions tend to fit well for both the Korsmeyer–Peppas and the zero-order model as well [ 39 , 61 , 62 ].…”

Section: Discussionsupporting

confidence: 88%

Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen

et al. 2023

View full text Add to dashboard Cite

Solid dispersions are typically binary systems with a hydrophilic matrix polymer and a lipophilic active substance. During formulation, the drug undergoes a crystalline to amorphous phase transition, which leads to a supersaturated solution providing enhanced bioavailability. The interaction of the active substance and the polymer is unique and influences the level of supersaturation. We aimed to investigate the relationship between low molecular weight polyethylene glycol derivates PEG 1000, 1500, and 2000 and ketoprofen regarding the effect of molecular weight. The physicochemical properties of solid dispersions prepared with hot melt homogenization and their respective physical mixtures were investigated with Fourier transform infrared spectroscopy, powder X-ray diffraction and scanning electron microscopy techniques. A phase solubility study was carried out in hydrochloric acid media which showed no difference between the three polymers, but the dissolution curves differed considerably. PEG 1000 had higher percentage of released drug than PEG 1500 and 2000, which had similar results. These results indicate that when multiple low molecular weight PEGs are suitable as matrix polymers of solid dispersions, the molecular weight has only limited impact on physicochemical characteristics and interactions and further investigation is needed to select the most applicable candidate.

show abstract

Section: Discussionsupporting

confidence: 88%

Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen

et al. 2023

View full text Add to dashboard Cite

show abstract

“…Carvedilol (CAR) is a non-selective third generation beta-blocker used to treat hypertension, congestive heart failure and angina pectoris [2]. Carvedilol is practically water insoluble; with a solubility value of 4.4 µg/mL in water, and it has a weak basic character (pKa value 6.8) [3]. Oral administration of CRV showed poor oral bioavailability (≈25%) due to high exposure to first-pass metabolism [4].…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of a Novel Mucoadhesive Carvedilol Nanosponge: A Promising Platform for Buccal Anti-Hypertensive Delivery

Khafagy

Lila

Sallam

et al. 2022

Gels

View full text Add to dashboard Cite

Carvedilol (CRV) is a non-selective third generation beta-blocker used to treat hypertension, congestive heart failure and angina pectoris. Oral administration of CRV showed poor bioavailability (25%), which might be ascribed to its extensive first-pass metabolism. Buccal delivery is known to boost drugs bioavailability. The aim of this study is to investigate the efficacy of bilosomes-based mucoadhesive carvedilol nanosponge for enhancing the oral bioavailability of CRV. The bilosomes were prepared, optimized and characterized for particle size, surface morphology, encapsulation efficiency and ex-vivo permeation studies. Then, the optimized formula was incorporated into a carboxymethyl cellulose/hydroxypropyl cellulose (CMC/HPC) composite mixture to obtain buccal nanosponge enriched with CRV bilosomes. The optimized bilosome formula (BLS9), showing minimum vesicle size, maximum entrapment, and highest cumulative in vitro release, exhibited a spherical shape with 217.2 nm in diameter, 87.13% entrapment efficiency, and sustained drug release for up to 24 h. In addition, ex-vivo drug permeation across sheep buccal mucosa revealed enhanced drug permeation with bilosomal formulations, compared to aqueous drug suspension. Consecutively, BLS9 was incorporated in a CMC/HPC gel and lyophilized for 24 h to obtain bilosomal nanosponge to enhance CRV buccal delivery. Morphological analysis of the prepared nanosponge revealed improved swelling with a porosity of 67.58%. The in vivo assessment of rats indicated that CRV-loaded nanosponge efficiently enhanced systolic/diastolic blood pressure, decreased elevated oxidative stress, improved lipid profile and exhibited a potent cardio-protective effect. Collectively, bilosomal nanosponge might represent a plausible nanovehicle for buccal delivery of CRV for effective management of hypertension.

show abstract

“…The sustained release performance of nanoparticles was measured using a RC1207DP dissolution tester (Tianjin, China) and ultraviolet spectrophotometer (UV spectrophotometer, T6, Pgeneral, Beijing, China) [ 28 , 29 ]. Firstly, 800 mL of phosphate buffer (pH = 7.4) was utilized as the dissolution media to ensure the internal environment.…”

Section: Methodsmentioning

confidence: 99%

Synthesis, Characterization, and Evaluation of Nanoparticles Loading Adriamycin Based on 2-Hydroxypropyltrimethyl Ammonium Chloride Chitosan Grafting Folic Acid

Zhang

et al. 2021

Polymers

View full text Add to dashboard Cite

Chitosan nanoparticles have been considered as potential candidates for drug loading/release in drug delivery systems. In this paper, nanoparticles (HACAFNP) loading adriamycin based on 2-hydroxypropyltrimethyl ammonium chloride chitosan grafting folic acid (HACF) were synthesized. The surface morphology of the novel nanoparticles was spherical or oval, and the nanoparticles exhibited a relatively small hydrodynamic diameter (85.6 ± 2.04 nm) and positive zeta potential (+21.06 ± 0.96 mV). The drug release of nanoparticles was assayed and represented a burst effect followed by a long-term steady release. Afterward, the antioxidant efficiencies of nanoparticles were assayed. In particular, the target nanoparticles exhibited significant enhancement in radical scavenging activities. Cytotoxicities against cancer cells (MCF-7, BGC-823, and HEPG-2) were estimated in vitro, and results showed nanoparticles inhibited the growth of cancer cells. It’s worth noting that the inhibition index of HACAFNP against BGC-823 cells was 71.19% with the sample concentration of 25 μg/mL, which was much higher than the inhibitory effect of ADM. It was demonstrated that the novel nanoparticles with dramatically enhanced biological activity, reduced cytotoxicity, and steady release could be used as the practical candidates for drug loading/release in a delivery system.

show abstract

Impact of drying on dissolution behavior of carvedilol-loaded sustained release solid dispersion: development and characterization

Cited by 12 publications

References 46 publications

Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen

Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen

Preparation and Characterization of a Novel Mucoadhesive Carvedilol Nanosponge: A Promising Platform for Buccal Anti-Hypertensive Delivery

Synthesis, Characterization, and Evaluation of Nanoparticles Loading Adriamycin Based on 2-Hydroxypropyltrimethyl Ammonium Chloride Chitosan Grafting Folic Acid

Contact Info

Product

Resources

About