Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Tran, Thao T.D.; Tran, Phuong Ha Lien

doi:10.3390/polym12081679

Cited by 8 publications

(5 citation statements)

References 110 publications

(166 reference statements)

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“…The prepared samples were scanned with a resolution of 4 cm -1 and a wave number range of 4000 to 400 cm -1 . 13,14 Differential Scanning Calorimetry (DSC) DSC was used to analyze the physical mixture (drug and polymer) and the resulting solid dispersion for their thermal behavior. The samples were heated to temperatures between 25 and 400°C while maintaining a pace of 10°C per minute to produce thermograms of the samples.…”

Section: Saturation Solubility Studymentioning

confidence: 99%

Solid Dispersion of Dolutegravir: Formulation Development, Characterization, and Pharmacokinetic Assessment

Bhairam¹,

Shukla²,

Gidwani³

et al. 2022

IJPQA

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A recently authorized antiviral drug called dolutegravir has solubility problems and could be a Biopharmaceutical Classification System (BCS) class II candidate. The current study aimed to improve dolutegravir’s solubility and efficiency by employing the solid dispersion method. Different ratios of hydrophilic polymeric carriers, including polyethylene glycol (PEG) 6000, polyvinyl pyrrolidone (PVP) (30K), and hydroxypropyl methylcellulose (HPMC), were used. Dolutegravir (DTG) and soluplus were produced as a solid dispersion at 1:5 ratio using the solvent evaporation method. A variety of techniques were utilized to describe the solid state, including powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and fourier transform infrared spectroscopy (FTIR). Produced solid dispersion did not reveal any physicochemical interactions between the DTG and soluplus, but the X-ray diffractogram clearly showed that the drug’s crystalline state had transformed to an amorphous state. DTG was released quickly from solid dispersion (92%) compared to pure drug (10.12%), physical mixture (22.06%), and commercially available DTG (62.90%). The formed solid dispersion’s drug release kinetics was in line with the Higuchi Model. Finally, the rapid drug release from the solid dispersion formulation showed higher Cmax (15.25 ± 0.40 μg/mL) compared to the physical mixture (5.11 ± 0.20 μg/mL) and pure drug (4.91 ± 0.73 μg/mL). DTG’s enhanced bioavailability in experimental wistar rats (AUC: 147.99 ± 23.86 μg/h/mL) further supported this when compared to the AUC of animals administered with physical mixture (52.35 ± 4.32 μg/h/mL) and pure drug (43.32 ± 3.13 μg/h/mL). Thus, it could be inferred that by employing the solid dispersion delivery system and the hydrophilic carrier, soluplus, the bioavailability and dissolution profile of DTG could both be improved, which could be expected to improve the drug’s effectiveness in treating Human immunodeficiency virus/Acquired immunodeficiency syndrome (HIV/AIDS).

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Section: Saturation Solubility Studymentioning

confidence: 99%

Solid Dispersion of Dolutegravir: Formulation Development, Characterization, and Pharmacokinetic Assessment

Bhairam¹,

Shukla²,

Gidwani³

et al. 2022

IJPQA

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“…Recently, extensive research has been conducted assessing the performance of pH-responsive, water-insoluble, and modified polyelectrolytes in controlled-release studies [ 136 , 137 ]. Controlled-release ASDs have been studied in order to reduce the required drug dose and, subsequently, improve patient compliance [ 138 ].…”

Section: Polyelectrolytes In Controlled-drug Release/colonic Targetingmentioning

confidence: 99%

Polyelectrolyte Matrices in the Modulation of Intermolecular Electrostatic Interactions for Amorphous Solid Dispersions: A Comprehensive Review

2021

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Polyelectrolyte polymers have been widely used in the pharmaceutical field as excipients to facilitate various drug delivery systems. Polyelectrolytes have been used to modulate the electrostatic environment and enhance favorable interactions between the drug and the polymer in amorphous solid dispersions (ASDs) prepared mainly by hot-melt extrusion. Polyelectrolytes have been used alone, or in combination with nonionic polymers as interpolyelectrolyte complexes, or after the addition of small molecular additives. They were found to enhance physical stability by favoring stabilizing intermolecular interactions, as well as to exert an antiplasticizing effect. Moreover, they not only enhance drug dissolution, but they have also been used for maintaining supersaturation, especially in the case of weakly basic drugs that tend to precipitate in the intestine. Additional uses include controlled and/or targeted drug release with enhanced physical stability and ease of preparation via novel continuous processes. Polyelectrolyte matrices, used along with scalable manufacturing methods in accordance with green chemistry principles, emerge as an attractive viable alternative for the preparation of ASDs with improved physical stability and biopharmaceutic performance.

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“…Examples of such polymers include polyvinylpyrrolidone (PVP), polyethylene glycol (PEG), hydroxypropyl methylcellulose (HPMC), and hydroxypropyl cellulose. 24,25 For this research, PVP has been chosen as the drug carrier. PVP finds widespread use in the pharmaceutical, biomedical, cosmetic, and food industries due to its biodegradable and hydrophilic properties.…”

Section: Introductionmentioning

confidence: 99%

“…Hydrophilic polymers are commonly used as carriers in the formation of solid dispersions due to their low toxicity, ability to reduce potential side effects, and ease of excretion. Examples of such polymers include polyvinylpyrrolidone (PVP), polyethylene glycol (PEG), hydroxypropyl methylcellulose (HPMC), and hydroxypropyl cellulose 24,25 . For this research, PVP has been chosen as the drug carrier.…”

Section: Introductionmentioning

confidence: 99%

Investigating the effect of polyvinylpyrrolidone matrix on surface characteristics and dissolution rate of anticancer drug dasatinib

Sokač,

Priselec,

Barač

et al. 2024

J of Applied Polymer Sci

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Dasatinib (DAS) is a second‐generation tyrosine kinase inhibitor used in the treatment of Philadelphia chromosome‐positive chronic myeloid leukemia and acute lymphoblastic leukemia. Nevertheless, this drug is hindered by poor gastrointestinal absorption and limited bioavailability, primarily attributable to its low aqueous solubility. To improve its properties, solid dispersions of DAS within a matrix of the hydrophilic polymer polyvinylpyrrolidone (PVP) are prepared by cogrinding in a vibrational ball mill at various drug‐to‐polymer ratios. The prepared solid dispersions are thoroughly characterized by several methods to verify the drug's amorphization and enhanced wettability as a result of successful mechanochemical activation. Fluidized bed melt granulation and traditional tableting are used to prepare tablets of 8 mm diameter with strictly defined aimed properties. Characterization of tablets includes testing their hardness, disintegration, and in vitro dissolution. The in vitro release profiles reveal a significant improvement in the release rate of DAS from tablets containing solid dispersion with the highest polymer ratio when compared with those containing untreated DAS or solid dispersions with a low polymer ratio. The results confirm the significant effect of the PVP ratio in solid dispersions on the surface characteristics and dissolution rate of DAS.

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Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Cited by 8 publications

References 110 publications

Solid Dispersion of Dolutegravir: Formulation Development, Characterization, and Pharmacokinetic Assessment

Solid Dispersion of Dolutegravir: Formulation Development, Characterization, and Pharmacokinetic Assessment

Polyelectrolyte Matrices in the Modulation of Intermolecular Electrostatic Interactions for Amorphous Solid Dispersions: A Comprehensive Review

Investigating the effect of polyvinylpyrrolidone matrix on surface characteristics and dissolution rate of anticancer drug dasatinib

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