Taste masking of paracetamol encapsulated in chitosan-coated alginate beads

Almurisi, Samah Hamed; Doolaanea, Abd Almonem; Akkawi, Muhammad Eid; Chatterjee, Bappaditya; Sarker, Zaidul Islam

doi:10.1016/j.jddst.2020.101520

Cited by 34 publications

(17 citation statements)

References 33 publications

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“…Medical application of SAG was reported by Veerubhotla et al in their research of a 3D printed hydrogel-based cardiovascular stent [ 13 ]. Alginate-based beads have been widely investigated for the sustained and targeted delivery of various drugs in order to enhance bioavailability [ 14 , 15 , 16 , 17 ]. A natural source of phytochemicals has been explored to extend the medicinal applications in the treatment of a variety of human diseases and disorders.…”

Section: Introductionmentioning

confidence: 99%

Development and Characterization of Calcium-Alginate Beads of Apigenin: In Vitro Antitumor, Antibacterial, and Antioxidant Activities

et al. 2021

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The objective of this work was to develop sustained-release Ca-alginate beads of apigenin using sodium alginate, a natural polysaccharide. Six batches were prepared by applying the ionotropic gelation technique, wherein calcium chloride was used as a crosslinking agent. The beads were evaluated for particle size, drug loading, percentage yield, and in vitro drug release. Particle size was found to decrease, and drug entrapment efficiency was enhanced with an increase in the polymer concentration. The dissolution study showed sustained drug release from the apigenin-loaded alginate beads with an increase in the polymer proportion. Based on the dissolution profiles, BD6 formulation was optimized and characterized for FTIR, DSC, XRD, and SEM, results of which indicated successful development of apigenin-loaded Ca alginate beads. MTT assay demonstrated a potential anticancer effect against the breast cancer MCF-7 cell lines. The antimicrobial activity exhibited effective inhibition in the bacterial and fungal growth rate. The DPPH measurement revealed that the formulation had substantial antioxidant activity, with EC50 value slightly lowered compared to pure apigenin. A stability study demonstrated that the BD6 was stable with similar (f2) drug release profiles in harsh condition. In conclusion, alginate-based beads could be used for sustaining the drug release of poorly water-soluble apigenin while also improving in vitro antitumor, antimicrobial, and antioxidant activity.

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Section: Introductionmentioning

confidence: 99%

Development and Characterization of Calcium-Alginate Beads of Apigenin: In Vitro Antitumor, Antibacterial, and Antioxidant Activities

et al. 2021

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“…The hydrogel structure of alginate nanoparticles usually has large pores that facilitate the movement of water-soluble small molecules out from the particles. For example, EE of paracetamol in alginate beads dropped rapidly from 33.92 ± 1.12% at 10 min gelation time to as low as 5 ± 1.32% at 30 min [ 76 ]. Similar findings were reported for macromolecules, such as whey protein, in which the EE achieved was below 60% [ 47 ].…”

Section: Resultsmentioning

confidence: 99%

Electrosprayed Alginate Nanoparticles as CRISPR Plasmid DNA Delivery Carrier: Preparation, Optimization, and Characterization

et al. 2020

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Therapeutic gene editing is becoming more feasible with the emergence of the Clustered Regularly Interspaced Short Palindromic Repeats (CRISPR)/CRISPR-associated protein (Cas) system. However, the successful implementation of CRISPR/Cas9-based therapeutics requires a safe and efficient in vivo delivery of the CRISPR components, which remains challenging. This study presents successful preparation, optimization, and characterization of alginate nanoparticles (ALG NPs), loaded with two CRISPR plasmids, using electrospray technique. The aim of this delivery system is to edit a target gene in another plasmid (green fluorescent protein (GFP)). The effect of formulation and process variables were evaluated. CRISPR ALG NPs showed mean size and zeta potential of 228 nm and −4.42 mV, respectively. Over 99.0% encapsulation efficiency was achieved while preserving payload integrity. The presence of CRISPR plasmids in the ALG NPs was confirmed by Attenuated Total Reflectance-Fourier Transform Infrared Spectroscopy. The tests revealed that the nanoparticles were cytocompatible and successfully introduced the Cas9 transgene in HepG2 cells. Nanoparticles-transfected HepG2 was able to edit its target plasmid by introducing double-strand break (DSB) in GFP gene, indicating the bioactivity of CRISPR plasmids encapsulated in alginate nanoparticles. This suggests that this method is suitable for biomedical application in vitro or ex vivo. Future investigation of theses nanoparticles might result in nanocarrier suitable for in vivo delivery of CRISPR/Cas9 system.

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“…An important aspect in an effervescent preparation is the drug solubilization in the liquid medium after effervescence, ensuring an adequate bioavailability. Paracetamol, chosen as a model drug, has high aqueous solubility (14.2 mg/mL [ 47 ]), even so, after 5 min, only 50% of the dose was dissolved in water at 25 °C from the raw material ( Figure 7 a), probably due to the slow dissolution of its crystals and the low wetting of the solid particles. Hence, simply mixing the effervescent components with the drug, despite the effervescence reaction, does not improve this result.…”

Section: Resultsmentioning

confidence: 99%

Hot-Melt Extrusion as an Advantageous Technology to Obtain Effervescent Drug Products

et al. 2020

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Here, we assessed the feasibility of hot-melt extrusion (HME) to obtain effervescent drug products for the first time. For this, a combined mixture design was employed using paracetamol as a model drug. Extrudates were obtained under reduced torque (up to 0.3 Nm) at 100 °C to preserve the stability of the effervescent salts. Formulations showed vigorous and rapid effervescent disintegration (<3 min), adequate flow characteristics, and complete solubilization of paracetamol instantly after the effervescent reaction. Formulations containing PVPVA in the concentration range of 15–20% m/m were demonstrated to be sensitive to accelerated aging conditions, undergoing marked microstructural changes, since the capture of water led to the agglomeration and loss of their functional characteristics. HPMC matrices, in contrast, proved to be resistant to storage conditions in high relative humidity, showing superior performance to controls, including the commercial product. Moreover, the combined mixture design allowed us to identify significant interactions between the polymeric materials and the disintegrating agents, showing the formulation regions in which the responses are kept within the required levels. In conclusion, this study demonstrates that HME can bring important benefits to the elaboration of effervescent drug products, simplifying the production process and obtaining formulations with improved characteristics, such as faster disintegration, higher drug solubilization, and better stability.

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Taste masking of paracetamol encapsulated in chitosan-coated alginate beads

Cited by 34 publications

References 33 publications

Development and Characterization of Calcium-Alginate Beads of Apigenin: In Vitro Antitumor, Antibacterial, and Antioxidant Activities

Development and Characterization of Calcium-Alginate Beads of Apigenin: In Vitro Antitumor, Antibacterial, and Antioxidant Activities

Electrosprayed Alginate Nanoparticles as CRISPR Plasmid DNA Delivery Carrier: Preparation, Optimization, and Characterization

Hot-Melt Extrusion as an Advantageous Technology to Obtain Effervescent Drug Products

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