A Review on Solid Dispersion and Carriers Used Therein for Solubility Enhancement of Poorly Water Soluble Drugs

Tekade, Avinash R.; Yadav, Jyoti Narayan

doi:10.34172/apb.2020.044

Cited by 83 publications

(75 citation statements)

References 73 publications

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“…Whilst oral delivery remains the most common route for drug administration, most new active pharmaceutical ingredients are poorly water soluble and thus not well-absorbed after oral administration. Solid dispersion, defined as the dispersion of one or more active ingredient in a carrier or matrix at solid state, is an established platform technology to enhance the dissolution rate and improve the apparent solubility of a drug and, hence, increase the bioavailability of a range of poorly water soluble drugs [ 1 , 2 , 3 ]. Several classes of hydrophilic polymers have been used as carriers to prepare solid dispersions, including PVP [ 4 , 5 , 6 ] and its derivatives [ 7 , 8 , 9 ], polyethylene glycols [ 10 , 11 ], cellulose ethers [ 12 , 13 ] and poloxamers [ 14 , 15 ].…”

Section: Introductionmentioning

confidence: 99%

Mutual Effects of Hydrogen Bonding and Polymer Hydrophobicity on Ibuprofen Crystal Inhibition in Solid Dispersions with Poly(N-vinyl pyrrolidone) and Poly(2-oxazolines)

et al. 2021

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Poly(N-vinyl pyrrolidone) (PVP), poly(2-methyl-2-oxazoline) (PMOZ), poly(2-ethyl-2-oxazoline) (PEOZ), poly(2-n-propyl-2-oxazoline) (PnPOZ), and poly(2-isopropyl-2-oxazoline) (PiPOZ) were used to prepare solid dispersions with ibuprofen (IB), a model poorly-water soluble drug. Dispersions, prepared by solvent evaporation, were investigated using powder X-ray diffractometry, differential scanning calorimetry, and FTIR spectroscopy; hydrogen bonds formed between IB and all polymers in solid dispersions. PMOZ, the most hydrophilic polymer, showed the poorest ability to reduce or inhibit the crystallinity of IB. In contrast, the more hydrophobic polymers PVP, PEOZ, PnPOZ, and PiPOZ provided greater but similar abilities to reduce IB crystallinity, despite the differing polymer hydrophobicity and that PiPOZ is semi-crystalline. These results indicate that crystallinity disruption is predominantly due to hydrogen bonding between the drug molecules and the polymer. However, carrier properties affected drug dissolution, where PnPOZ exhibited lower critical solution temperature that inhibited the release of IB, whereas drug release from other systems was consistent with the degree of ibuprofen crystallinity within the dispersions.

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Section: Introductionmentioning

confidence: 99%

Mutual Effects of Hydrogen Bonding and Polymer Hydrophobicity on Ibuprofen Crystal Inhibition in Solid Dispersions with Poly(N-vinyl pyrrolidone) and Poly(2-oxazolines)

et al. 2021

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“…The product and carrier will instantly crystallize during the cooling phase of the eutectic mixture, so it is preferred over the monotectic mixture. 15,17 The reduced particle size increases the specific surface area, thus enhances the dissolution rate and bioavailability. 17…”

Section: First-generation Solid Dispersionmentioning

confidence: 99%

“…15,17 The reduced particle size increases the specific surface area, thus enhances the dissolution rate and bioavailability. 17…”

Section: First-generation Solid Dispersionmentioning

confidence: 99%

“…Although using more viscous polymers can impede the drug dissolution rate, it is often used to tackle the recrystallization drawback providing a more stable formulation suitable for manufacture. 17…”

Section: Second Generation Solid Dispersionmentioning

confidence: 99%

“…Loosening polymer chains is necessary to incorporate the drug molecules, as the effect of heat achieves this flexibility, whether by hot-melt extrusion or fusion method. 17 Many techniques are based on using solvents, such as solvent evaporation and co-precipitation methods. The used solvent has a dual role: besides converting the drug into a molecular state, the solvent creates weak inter-and intra-molecular cohesion polymer chain interactions, developing polymer interactions with different solvents.…”

Section: Mechanism Of Drug Incorporation and Release From Solid Dispersionmentioning

confidence: 99%

See 2 more Smart Citations

Solid Dispersion as a Technical Solution to Boost the Dissolution Rate and Bioavailability of Poorly Water-Soluble Drugs

Attia¹,

Hasan²,

Ghazy³

et al. 2021

IJPER

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Solid dispersion (SD) is one of the oldest and widely utilized techniques to improve the solubility of slowly dissolving drugs. A variety of pharmaceutically compatible additives using different emerging technology is used for preparing SDs. Multiple approaches were designed to prepare SDs by such as kneading, co-milling, fusion, solvent evaporation and various solvent-associated methods. The selection of appropriate preparation method and carrier is vital for producing a homogenous product affecting its stability and biological activity. Many attempts were recently carried out to improve the scalability of the applied approaches and the results were novel preparation methods such as KinetiSol, Electrospinning and Hot-melt extrusion. In the present review, drug carriers used to formulate SD were classified as small molecular weight carriers, large molecular weight named polymeric carriers and functionalized polymeric ones. Moreover, new attractive SD formulated using the newly emerged natural carriers recently joined the field of the pharmaceutical industry.

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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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A Review on Solid Dispersion and Carriers Used Therein for Solubility Enhancement of Poorly Water Soluble Drugs

Cited by 83 publications

References 73 publications

Mutual Effects of Hydrogen Bonding and Polymer Hydrophobicity on Ibuprofen Crystal Inhibition in Solid Dispersions with Poly(N-vinyl pyrrolidone) and Poly(2-oxazolines)

Mutual Effects of Hydrogen Bonding and Polymer Hydrophobicity on Ibuprofen Crystal Inhibition in Solid Dispersions with Poly(N-vinyl pyrrolidone) and Poly(2-oxazolines)

Solid Dispersion as a Technical Solution to Boost the Dissolution Rate and Bioavailability of Poorly Water-Soluble Drugs

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

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