Matrix systems for oral drug delivery: Formulations and drug release

Vasvári, Gábor; Kalmár, József; Veres, Péter; Vecsernyés, Miklós; Bácskay, Ildikó; Fehér, Pálma; Ujhelyi, Zoltán; Haimhoffer, Ádám; Rusznyák, Ágnes; Fenyvesi, Ferenc; Váradi, Judit

doi:10.1016/j.ddtec.2018.06.009

Cited by 33 publications

(17 citation statements)

References 140 publications

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“…Besides its numerous application as a dissolution retardant (40) in oral hydrophobic matrix systems, SA when neutralised with tetrabutylammonium hydroxide can be used to create foam from o/w emulsions (41). The authors states based on the results of the experiments that SA contributes to the easier foamability due to two of its property.…”

Section: Discussionmentioning

confidence: 99%

Development and Characterisation of Gastroretentive Solid Dosage Form Based on Melt Foaming

et al. 2019

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Dosage forms with increased gastric residence time are promising tools to increase bioavailability of drugs with narrow absorption window. Low-density floating formulations could avoid gastric emptying; therefore, sustained drug release can be achieved. Our aim was to develop a new technology to produce low-density floating formulations by melt foaming. Excipients were selected carefully, with the criteria of low gastric irritation, melting range below 70°C and well-known use in oral drug formulations. PEG 4000, Labrasol and stearic acid type 50 were used to create metronidazole dispersion which was foamed by air on atmospheric pressure using in-house developed apparatus at 53°C. Stearic acid was necessary to improve the foamability of the molten dispersion. Additionally, it reduced matrix erosion, thus prolonging drug dissolution and preserving hardness of the moulded foam. Labrasol as a liquid solubiliser can be used to increase drug release rate and drug solubility. Based on the SEM images, metronidazole in the molten foam remained in crystalline form. MicroCT scans with the electron microscopic images revealed that the foam has a closed-cell structure, where spherical voids have smooth inner wall, they are randomly dispersed, while adjacent voids often interconnected with each other. Drug release from all compositions followed Korsmeyer-Peppas kinetic model. Erosion of the matrix was the main mechanism of the release of metronidazole. Texture analysis confirmed that stearic acid plays a key role in preserving the integrity of the matrix during dissolution in acidic buffer. The technology creates low density and solid matrix system with micronsized air-filled voids.

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Section: Discussionmentioning

confidence: 99%

Development and Characterisation of Gastroretentive Solid Dosage Form Based on Melt Foaming

et al. 2019

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“…International Journal of Polymer Scienceadministration of AMD which is more convenient for patients. The prolonged release in the 6-8 h time interval is in accordance with optima pharmaceutical requirements for such formulations, to avoid the risk of AMD accumulation in the organism which should lead to the major toxic phenomena[65,66].…”

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confidence: 81%

Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone

Crețeanu

Pamfil²,

Vasile³

et al. 2019

International Journal of Polymer Science

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The aim of this study was to improve the solubility of amiodarone hydrochloride (AMD) and the drug release using its inclusion complexes with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complexes were prepared by coprecipitation and freeze-drying. The solubility enhancement of AMD/HP-β-CD inclusion complexes by 4–22 times was evaluated by the phase solubility method. The inclusion complexes were studied both in solution and in solid state by spectroscopic methods, dynamic light scattering (DLS) and zeta potential analysis, SEM, and DSC. The formulations of AMD/HP-β-CD inclusion complexes both as powdered form and as matrix tablets showed superior pharmacokinetic performance in improving loading and release properties in respect of those of the insoluble AMD drug. In vitro kinetic study reveals a complex mechanism of release occurring in three steps: the first one being attributed to a burst effect and the other two to different bonding existing in inclusion complexes. An in vivo test on matrix tablets containing Kollidon® and chitosan also reveals a multiple (at least two) peaks release diagram because of both structures of the inclusion complexes and also of different sites of absorption in biological media (digestive tract).

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“…In the past few decades, many efforts have been made to develop controlled drug release systems. These systems can regulate drug dissolution from a formulation in a controlled manner [ 36 ] and reduce the fluctuations of drug concentrations in the blood. These properties result in a decrease in the drug’s adverse effects [ 37 ].…”

Section: Resultsmentioning

confidence: 99%

PEGylated Mesoporous Silica Nanoparticles (MCM-41): A Promising Carrier for the Targeted Delivery of Fenbendazole into Prostrate Cancer Cells

et al. 2021

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Low water solubility and thus low bioavailability limit the clinical application of fenbendazole (FBZ) as a potential anticancer drug. Solubilizing agents, such as Mobil Composition of Matter Number 41 (MCM) as a drug carrier, can improve the water solubility of drugs. In this study, PEGylated MCM (PEG-MCM) nanoparticles (NPs) were synthesized and loaded with FBZ (PEG-MCM-FBZ) to improve its solubility and, as a result, its cytotoxicity effect against human prostate cancer PC-3 cells. The loading efficiency of FBZ onto PEG-MCM NPs was 17.2%. The size and zeta potential of PEG-MCM-FBZ NPs were 366.3 ± 6.9 nm and 24.7 ± 0.4 mV, respectively. They had a spherical shape and released the drug in a controlled manner at pH 1.2 and pH 6.2. PEG-MCM-FBZ were found to inhibit the migration of PC-3 cells, increase the cytotoxicity effects of FBZ against PC-3 cells by 3.8-fold, and were more potent by 1.4-fold, when compared to the non-PEGylated NPs. In addition, PEG-MCM-FBZ promoted the production of reactive oxygen species by 1.3- and 1.2-fold, respectively, when compared to FBZ and MCM-FBZ. Overall, the results demonstrate that PEG-MCM-FBZ NPs enhanced FBZ delivery to PC-3 cells; therefore, they have the potential to treat prostate cancer after a comprehensive in vivo study.

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Matrix systems for oral drug delivery: Formulations and drug release

Cited by 33 publications

References 140 publications

Development and Characterisation of Gastroretentive Solid Dosage Form Based on Melt Foaming

Development and Characterisation of Gastroretentive Solid Dosage Form Based on Melt Foaming

Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone

PEGylated Mesoporous Silica Nanoparticles (MCM-41): A Promising Carrier for the Targeted Delivery of Fenbendazole into Prostrate Cancer Cells

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