Water-soluble and -insoluble polymers as binders for pellet preparation by extrusion/spheronization

Zoubari, Gaith; Ali, Rebaz; Dashevskiy, Andriy

doi:10.1016/j.jddst.2018.10.030

Cited by 12 publications

(6 citation statements)

References 16 publications

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“…It is used for waterproofing in pharmaceutical coating processes ( Rowe et al, 2009 ). EC is a colourless, odourless and tasteless polymer ( Zoubari et al, 2019 ) primarily used in oral drug formulation as a hydrophobic coating agent or as a matrix former for tablets and granules to modify the release of drug and so forth ( Rowe et al, 2009 , Azoury et al, 1988 ). ERS is a copolymer of ethyl acrylate, methyl methacrylate and a low content of methacrylic acid ester.…”

Section: Introductionmentioning

confidence: 99%

Doxycycline hyclate-loaded in situ forming gels composed from bleached shellac, Ethocel, and Eudragit RS for periodontal pocket delivery

Senarat

Lwin

Mahadlek

et al. 2021

Saudi Pharmaceutical Journal

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Polymeric material plays an important role as a matrix former in the modulation of drug release of antimicrobial-loaded in situ forming gel (ISG) for efficient periodontitis treatment. This study was conducted to compare three polymers, namely bleached shellac (BS), Ethocel (EC) and Eudragit RS (ERS), as matrix formers of doxycycline hyclate (DH)-loaded solvent exchange-induced ISG. All prepared ISGs, except 25% EC ISG, exhibited the Newtonian flow behaviour. Transformation from solution into matrix-like was achieved rapidly within 5 min. Increasing the amount of these polymers extended the release of DH. DH-loaded EC and ERS ISG systems exhibited high antimicrobial activity, and all ISGs were effective in inhibiting the growth of Staphylococcus aureus , Escherichia coli , Streptococcus mutans , Porphyromonas gingivalis and Candida albicans . By comparison, the DH-loaded ERS ISG, through the solvent exchange mechanism, was found to be ease in injection with low viscosity and sustained the release with higher concentration, meanwhile, it also exhibited interesting in vitro degradability and antimicrobial activities. Therefore, the DH-loaded ERS ISG exhibited a potential use for localized periodontal drug delivery system for the treatment periodontitis.

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Section: Introductionmentioning

confidence: 99%

Doxycycline hyclate-loaded in situ forming gels composed from bleached shellac, Ethocel, and Eudragit RS for periodontal pocket delivery

Senarat

Lwin

Mahadlek

et al. 2021

Saudi Pharmaceutical Journal

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show abstract

“…Alternatively, the release controlling polymer can be incorporated into the beads as a binder that can potentially control drug release, with or without a thin coating. These matrix pellet systems have advantages over coated pellets, due to their easier production and higher resistance to mechanical stress that can damage the shell [ 36 ].…”

Section: Resultsmentioning

confidence: 99%

Chitosan and Sodium Alginate Implementation as Pharmaceutical Excipients in Multiple-Unit Particulate Systems

et al. 2022

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This study aimed to prepare and evaluate pellets containing acyclovir as a model drug. Pellets were prepared by the extrusion–spheronization process. Aqueous solutions of natural marine polymers (sodium alginate, chitosan) were compared to semi-synthetic hydroxypropyl methylcellulose (HPMC) in the role of binders. The study focused on the characterization of the pellet properties that are crucial for the formulation of the final dosage form, such as in multi-unit pellet system (MUPS) tablets or hard gelatin capsules filled with the pellets. Finally, the mentioned dosage forms were tested for drug dissolution. The morphology of pellets observed by scanning electron microscopy correlated with the shape evaluation performed by dynamic image analysis. Sodium alginate pellets exhibited the lowest value of sphericity (0.93), and many elongated rods and dumbbells were observed in this batch. Chitosan pellets had the highest value of sphericity (0.97) and were also less rough on the surface. The pellets maintained a constant surface geometry during the dissolution studies; they only reduced in size. The most significant reduction in size and weight was assessed after 2 h of dissolution testing. This fact was in line with the drug release from pellets in capsules or MUPS tablets, which was massive during the first hour, in both cases. The dissolution profiles of all of the batches were comparable.

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“…This encapsulation technique has been shown to have better cellular absorption and anticancer activity than non-encapsulated alphamangostin [33]. The use of cellulose derivates is to absorb large amounts of water, due to its large surface area, high porosity, and low fragility [55]. Cellulose also has an affinity in the formation of complexes with drugs and can reduce the crystallization of drugs in forming an amorphous matrix [56], and in doing so, demonstrates the efficacy of the treatment in mice after oral administration.…”

Section: Nanoparticle Technologymentioning

confidence: 99%

Methods for Improving Alpha-Mangostin Solubility: A Review

2021

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Solubility is an important parameter to achieve for the bioavailability of a drug to reach the therapeutic windows. Garcinia mangostana Linn is a plant with great potency for the development of natural medicine. Alpha-mangostin is one of the secondary metabolites of G. mangostana and has been reported to have several pharmacological activities. The Biopharmaceutics Classification System (BCS) is a system that classifies drugs based on their solubility and permeability. Due to its low solubility but high permeation, alpha-mangostin is categorized into class II of the Biopharmaceutics Classification System. Therefore, the determination of dosage forms and modification of solubility enhancers is limited due to its physical properties, as mentioned above. This disadvantage requires new methods to improve its solubility to administer alpha-mangostin, especially for oral administration. Here, we discuss the development of the methods to increase alpha-mangostin solubility to be applied to formulate a dosage form to reach a useful plasma level for medication.

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Water-soluble and -insoluble polymers as binders for pellet preparation by extrusion/spheronization

Cited by 12 publications

References 16 publications

Doxycycline hyclate-loaded in situ forming gels composed from bleached shellac, Ethocel, and Eudragit RS for periodontal pocket delivery

Doxycycline hyclate-loaded in situ forming gels composed from bleached shellac, Ethocel, and Eudragit RS for periodontal pocket delivery

Chitosan and Sodium Alginate Implementation as Pharmaceutical Excipients in Multiple-Unit Particulate Systems

Methods for Improving Alpha-Mangostin Solubility: A Review

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