Increasing bioavailability of very poorly water-soluble compounds. A case study of an anti-tumor drug, soloxolon methyl

Ogienko, A. G.; Markov, Andrey; Sen’kova, Aleksandra V.; Logashenko, Evgeniya B.; Salomatina, Oksana V.; Myz, S. A.; Nefedov, Andrey A.; Losev, Evgeniy A.; Drebushchak, T. N.; Salakhutdinov, N. F.; Болдырев, В. В.; Власов, В. В.; Зенкова, М. А.; Болдырева, Е. В.

doi:10.1016/j.jddst.2018.10.025

Cited by 4 publications

(8 citation statements)

References 53 publications

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“…[322] Interestingly, in various solid formulations used in large porous particles prepared by freeze-drying, b-glycine is present as a component of the composites with drug molecules. [195][196][197]321] As in the nanoferroelectrics metioned in Section 4, β-glycine remains very stable in these formulations. A dedicated study if and how the physical properties of this polymorph can influence the action of a pharmaceutical formulation are required.…”

Section: Glycine and Its Ability To Form Solid Complexes With Other C...mentioning

confidence: 89%

“…Nonphotochemical laser-induced nucleation (NPLIN), [162,[175][176][177][178][179][180][181] and crystallization in electromagnetic fields [182][183][184] have been taken as demonstration of the validity of such a model for the crystallization occurring in supersaturated (and aged) aqueous glycine solutions. The techniques based on changing the rate of increasing supersaturation (antisolvent crystallization, [185][186][187] spray-drying, [188][189][190][191][192] freeze-drying, [193][194][195][196][197] cooling at variable rates [45,198,199] ) suppose using the Ostwald's rule of stages, [200,201] when a metastable form nucleates first and in this way also the batch product can be prepared as a metastable polymorph. At the same time, many studies showed, that the relative rates of the growth of the already formed nuclei, and / or their solvent assistant transformation into other polymorphs are at least equally important.…”

Section: Crystallization Procedures and Mechanismsmentioning

confidence: 99%

“…Apart of being active as a pharmaceutical compound itself, glycine is widely used as an excipient in various pharmaceutical applications ranging from pulmonary delivery [196,309,318] to the solubilization of drugs, [195,319] the targeted delivery of drugs in cancer therapy [197,320,321] and intranasal delivery of drugs to brain. [322] Interestingly, in various solid formulations used in large porous particles prepared by freeze-drying, b-glycine is present as a component of the composites with drug molecules.…”

Section: Glycine and Its Ability To Form Solid Complexes With Other C...mentioning

confidence: 99%

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Glycine: The Gift that Keeps on Giving

Boldyreva

2021

Israel Journal of Chemistry

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Glycine is a small molecule. It cannot change its conformation and is achiral. Despite the apparent simplicity, glycine shows endless diversity in its behavior over many phenomena. It was the first amino acid for which polymorphism was reported, first on crystallization and then on hydrostatic compression. The polymorphs differ in their physical properties and their biological activity. Glycine clusters persist in solution, leading to "solution memory". Phenomena at interfaces are critically important for crystal growth, dissolution, and for physical properties, which can be at times unexpected, like polarity in centrosymmetric αpolymorph. It is a great pleasure to remind of these remarkable phenomena in a special issue honoring professors Meir Lahav and Leslie Leiserowitz, who pioneered the study of the behavior of this unique molecule in many respects, and showed how complex and non-trivial phenomena can be at interfaces: between phases and between research fields.

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Section: Glycine and Its Ability To Form Solid Complexes With Other C...mentioning

confidence: 89%

Section: Crystallization Procedures and Mechanismsmentioning

confidence: 99%

Section: Glycine and Its Ability To Form Solid Complexes With Other C...mentioning

confidence: 99%

See 1 more Smart Citation

Glycine: The Gift that Keeps on Giving

Boldyreva

2021

Israel Journal of Chemistry

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“…This could be because the low solid content fails to form a continuous matrix or because at low initial solid contents, particles are very fragile and collapse during lyophilization under vacuum, which are consistent with previous reports. 26,27 3.3.4. Flow Property of DPI Formulations using an FT4 Powder Rheometer.…”

Section: Morphology and Crystallinity Of Nanoparticlesmentioning

confidence: 99%

Inhalable Nanocomposite Microparticles with Enhanced Dissolution and Superior Aerosol Performance

Zhu

Chen

et al. 2020

Mol. Pharmaceutics

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Previous studies have shown that combining colistin (Col), a cationic polypeptide antibiotic, with ivacaftor (Iva), a cystic fibrosis (CF) drug, could achieve synergistic antibacterial effects against Pseudomonas aeruginosa. The purpose of this study was to develop dry powder inhaler formulations for co-delivery of Col and Iva, aiming to treat CF and lung infection simultaneously. In order to improve solubility and dissolution for the water-insoluble Iva, Iva was encapsulated into bovine serum albumin (BSA) nanoparticles (Iva-BSA-NPs). Inhalable composite microparticles of Iva-BSA-NPs were produced by spray-freeze-drying using water-soluble Col as the matrix material and L-leucine as an aerosol enhancer. The optimal formulation showed an irregularly shaped morphology with fine particle fraction (FPF) values of 73.8 ± 5.2% for Col and 80.9 ± 4.1% for Iva. Correlations between "D tapped ρ × " and FPF were established for both Iva and Col. The amorphous solubility of Iva is 66 times higher than the crystalline solubility in the buffer. Iva-BSA-NPs were amorphous and remained in the amorphous state after spray-freeze-drying, as examined by powder X-ray diffraction. In vitro dissolution profiles of the selected DPI formulation indicated that Col and Iva were almost completely released within 3 h, which was substantially faster regarding Iva release than the jet-milled physical mixture of the two drugs. In summary, this study developed a novel inhalable nanocomposite microparticle using a synergistic water-soluble drug as the matrix material, which achieved reduced use of excipients for high-dose medications, improved dissolution rate for the waterinsoluble drug, and superior aerosol performance.

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“…Poorly soluble or insoluble drugs result in low absorption, which certainly affects drug bioavailability, especially in oral drug delivery [ 1 , 2 , 3 , 4 , 5 ]. Therefore, many formulation strategies have been developed to overcome the limitations of these drugs [ 6 , 7 , 8 , 9 , 10 ].…”

Section: Introductionmentioning

confidence: 99%

Molecular Interactions in Solid Dispersions of Poorly Water-Soluble Drugs

Tran

2020

Pharmaceutics

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Physicochemical characterization is a crucial step for the successful development of solid dispersions, including the determination of drug crystallinity and molecular interactions. Typically, the detection of molecular interactions will assist in the explanation of different drug performances (e.g., dissolution, solubility, stability) in solid dispersions. Various prominent reviews on solid dispersions have been reported recently. However, there is still no overview of recent techniques for evaluating the molecular interactions that occur within solid dispersions of poorly water-soluble drugs. In this review, we aim to overview common methods that have been used for solid dispersions to identify different bond formations and forces via the determination of interaction energy. In addition, a brief background on the important role of molecular interactions will also be described. The summary and discussion of methods used in the determination of molecular interactions will contribute to further developments in solid dispersions, especially for quick and potent drug delivery applications.

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Increasing bioavailability of very poorly water-soluble compounds. A case study of an anti-tumor drug, soloxolon methyl

Cited by 4 publications

References 53 publications

Glycine: The Gift that Keeps on Giving

Glycine: The Gift that Keeps on Giving

Inhalable Nanocomposite Microparticles with Enhanced Dissolution and Superior Aerosol Performance

Molecular Interactions in Solid Dispersions of Poorly Water-Soluble Drugs

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