Improvement in the water solubility of drugs with a solid dispersion system by spray drying and hot-melt extrusion with using the amphiphilic polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer and d-mannitol

Ogawa, Naoko; Hiramatsu, Tomoki; Suzuki, Ryôhei; Okamoto, Reiko; Shibagaki, Kohei; Fujita, Kosuke; Takahashi, Chisato; Kawashima, Yasunaru; Yamamoto, Hiromitsu

doi:10.1016/j.ejps.2017.09.014

Cited by 45 publications

(29 citation statements)

References 44 publications

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“…Spraydrying is known to trigger the formation of amorphous solid dispersions (41,42), a phenomenon that has been reported for IBU encapsulation with gelatin (31), acylated soy protein (16), or HPMCP-HP55 and Kollidon VA 64 (5). This change in crystalline form would be expected to increase solubility and, thus, the bioavailability of drugs poorly soluble in water (43).…”

Section: Crystalline State Of Encapsulated Ibumentioning

confidence: 94%

Spray-Dried Succinylated Soy Protein Microparticles for Oral Ibuprofen Delivery

et al. 2019

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The potential value of succinylated soy protein (SPS) as a wall material for the encapsulation of ibuprofen (IBU), a model hydrophobic drug, by spray-drying was investigated. A succinylation rate of 93% was obtained for soy protein isolate, with a molar ratio of 1/1.5 (NH 2 /succinic anhydride). The solubility profile at 37°C showed that this chemical modification decreased the solubility of the protein below its isoelectric point, whereas solubility increased in alkaline conditions. Various SPS/IBU ratios (90/10, 80/20, and 60/40) were studied and compared with the same ratio of soy protein isolate (SPI/IBU). High encapsulation efficiency was achieved (91-95%). Microparticles were spherical and between 4 and 8 μm in diameter. The spray-drying of protein/IBU solutions appeared to be beneficial, as it resulted in an amorphous solid dispersion of IBU within the microparticles, coupled with an increase in the thermal stability of IBU. In vitro release was evaluated in acidic (pH 1.2 in the presence of pepsin) and neutral (pH 6.8) conditions similar to those in the gastrointestinal (GI) tract. IBU was released significantly more slowly at pH 1.2, for both proteins. However, this slowing was particularly marked for SPS, for which rapid (within 2 h) and complete release was observed at pH 6.8. These results validate the hypothesis that SPS is suitable for use as a coating material for hydrophobic active pharmaceutical ingredients (APIs) due to its pH sensitivity, which should delay IBU release in the gastrointestinal tract.

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Section: Crystalline State Of Encapsulated Ibumentioning

confidence: 94%

Spray-Dried Succinylated Soy Protein Microparticles for Oral Ibuprofen Delivery

et al. 2019

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“…These advantages make it more suitable for preparation of SDs for oral drug delivery. Soluplus ® , a polyethylene glycol, polyvinyl acetate and polyvinylcaprolactame-based graft copolymer, has been extensively investigated for preparation of SDs [ 62 , 63 ]. Soluplus ® is a transparent solid excipient and can form solid solutions with many drugs [ 66 ].…”

Section: Solid Dispersion Techniquementioning

confidence: 99%

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

et al. 2018

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Over the past decades, a large number of drugs as well as drug candidates with poor dissolution characteristics have been witnessed, which invokes great interest in enabling formulation of these active ingredients. Poorly water-soluble drugs, especially biopharmaceutical classification system (BCS) II ones, are preferably designed as oral dosage forms if the dissolution limit can be broken through. Minimizing a drug’s size is an effective means to increase its dissolution and hence the bioavailability, which can be achieved by specialized dispersion techniques. This article reviews the most commonly used dispersion techniques for pharmaceutical processing that can practically enhance the dissolution and bioavailability of poorly water-soluble drugs. Major interests focus on solid dispersion, lipid-based dispersion (nanoencapsulation), and liquisolid dispersion (drug solubilized in a non-volatile solvent and dispersed in suitable solid excipients for tableting or capsulizing), covering the formulation development, preparative technique and potential applications for oral drug delivery. Otherwise, some other techniques that can increase the dispersibility of a drug such as co-precipitation, concomitant crystallization and inclusion complexation are also discussed. Various dispersion techniques provide a productive platform for addressing the formulation challenge of poorly water-soluble drugs. Solid dispersion and liquisolid dispersion are most likely to be successful in developing oral dosage forms. Lipid-based dispersion represents a promising approach to surmounting the bioavailability of low-permeable drugs, though the technique needs to traverse the obstacle from liquid to solid transformation. Novel dispersion techniques are highly encouraged to develop for formulation of poorly water-soluble drugs.

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“…Recent studies have shown that hydrophilic polymers, such as hydroxypropyl methylcellulose, polyvinylpyrrolidone, hydroxypropyl cellulose, and polyethylene glycol, are commonly used in the formation of SDs [18][19][20][21][22][23][24][25][26][27][28][29][30]. Moreover, ternary SDs of these polymers have also been utilized to further improve drug bioavailability [31][32][33][34][35][36][37][38][39][40][41].…”

Section: Introductionmentioning

confidence: 99%

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

Tran

2020

Polymers

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In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

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Improvement in the water solubility of drugs with a solid dispersion system by spray drying and hot-melt extrusion with using the amphiphilic polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer and d-mannitol

Cited by 45 publications

References 44 publications

Spray-Dried Succinylated Soy Protein Microparticles for Oral Ibuprofen Delivery

Spray-Dried Succinylated Soy Protein Microparticles for Oral Ibuprofen Delivery

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

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

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