The technology for improving stability of nanosuspensions in drug delivery

Guan, Wenhao; Ma, Yingying; Ding, Shuaijie; Liu, Yanchao; Song, Zimin; Liu, Xiang; Tang, Lingling; Wang, Yancai

doi:10.1007/s11051-022-05403-9

Cited by 18 publications

(14 citation statements)

References 161 publications

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“…In these methods, the nanoparticulate systems are separated from the release medium through dialysis membranes that are permeable to the free drug but impermeable to the nanoparticles. Dialysis methods have been widely used to investigate in vitro drug dissolution/release profiles of liposomes [ 29 , 30 ], emulsions [ 31 ], polymeric nanoparticles [ 32 , 33 ], as well as lipid nanocarriers [ 34 ].…”

Section: Resultsmentioning

confidence: 99%

Formulation, Optimization, and Evaluation of Moringa oleifera Leaf Polyphenol-Loaded Phytosome Delivery System against Breast Cancer Cell Lines

et al. 2022

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Moringa oleifera leaf polyphenols (Mopp) were encapsulated with phytosomes to enhance their efficacy on 4T1 cancer cell lines. The Mopp were extracted via microwave-assisted extraction. Moringa oleifera polyphenol-loaded phytosomes (MoP) were prepared with the nanoprecipitation method and characterized using the dynamic light scattering and dialysis membrane techniques. The in vitro cytotoxic and antiproliferative activity were investigated with the (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazole) MTT assay. Acute toxicity was assessed using Swiss albino mice. An MoP particle size of 296 ± 0.29 nm, −40.1 ± 1.19 mV zeta potential, and polydispersity index of 0.106 ± 0.002 were obtained. The total phenolic content was 50.81 ± 0.02 mg GAE/g, while encapsulation efficiency was 90.32 ± 0.11%. The drug release profiles demonstrated biphasic and prolonged subsequent sustained release. In vitro assays indicated MoP had a low cytotoxicity effect of 98.84 ± 0.53 μg/mL, doxorubicin was 68.35 ± 3.508, and Mopp was 212.9 ± 1.30 μg/mL. Moreover, MoP exhibited the highest antiproliferative effect on 4T1 cancer cells with an inhibitory concentration of 7.73 ± 2.87 μg/mL and selectivity index > 3. The results indicated a significant difference (p ≤ 0.001) in MoP when compared to Mopp and doxorubicin. The in vivo investigation showed the safety of MoP at a dose below 2000 mg/kg. The present findings suggest that MoP may serve as an effective and promising formulation for breast cancer drug delivery and therapy.

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Section: Resultsmentioning

confidence: 99%

Formulation, Optimization, and Evaluation of Moringa oleifera Leaf Polyphenol-Loaded Phytosome Delivery System against Breast Cancer Cell Lines

et al. 2022

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“…However, this does not change the saturation solubility of a drug, and low oral bioavailability still poses a problem [ 67 ]. Although it is known that the saturation solubility of an active substance is a compound-specific property depending on crystalline form, the lipophilicity of the drug, fed/fasted state, pKa, temperature, and properties of dissolution medium, at a nanometer range of saturation solubility, are also functions of particle size, according to the Ostwald–Freundlich and Kelvin equations [ 16 , 68 , 69 ]. NSs provide a tremendous increase in the surface-area-to-volume ratio and this leads to a higher solubility.…”

Section: Administration Routes Of Nanosuspensionsmentioning

confidence: 99%

Formulation Strategies of Nanosuspensions for Various Administration Routes

et al. 2023

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Nanosuspensions (NSs), which are nanosized colloidal particle systems, have recently become one of the most interesting substances in nanopharmaceuticals. NSs have high commercial potential because they provide the enhanced solubility and dissolution of low-water-soluble drugs by means of their small particle sizes and large surface areas. In addition, they can alter the pharmacokinetics of the drug and, thus, improve its efficacy and safety. These advantages can be used to enhance the bioavailability of poorly soluble drugs in oral, dermal, parenteral, pulmonary, ocular, or nasal routes for systemic or local effects. Although NSs often consist mainly of pure drugs in aqueous media, they can also contain stabilizers, organic solvents, surfactants, co-surfactants, cryoprotectants, osmogents, and other components. The selection of stabilizer types, such as surfactants or/and polymers, and their ratio are the most critical factors in NS formulations. NSs can be prepared both with top-down methods (wet milling, dry milling, high-pressure homogenization, and co-grinding) and with bottom-up methods (anti-solvent precipitation, liquid emulsion, and sono-precipitation) by research laboratories and pharmaceutical professionals. Nowadays, techniques combining these two technologies are also frequently encountered. NSs can be presented to patients in liquid dosage forms, or post-production processes (freeze drying, spray drying, or spray freezing) can also be applied to transform the liquid state into the solid state for the preparation of different dosage forms such as powders, pellets, tablets, capsules, films, or gels. Thus, in the development of NS formulations, the components/amounts, preparation methods, process parameters/levels, administration routes, and dosage forms must be defined. Moreover, those factors that are the most effective for the intended use should be determined and optimized. This review discusses the effect of the formulation and process parameters on the properties of NSs and highlights the recent advances, novel strategies, and practical considerations relevant to the application of NSs to various administration routes.

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“…Nanosuspensions have some drawbacks which include long-term physical and chemical instability resulting in short shelf life periods. − Also, nanosuspensions produced by liquid AS crystallization tend to have low API concentrations and, thus, may require large dose volumes to achieve an effective dose. Thus, separating nanoparticles from suspension into a dry powder form is often desired but is not without its challenges due to slow filtration rates and particle growth or agglomeration during separation.…”

Section: Introductionmentioning

confidence: 99%

“…Nanosuspensions have some drawbacks which include longterm physical and chemical instability 26 resulting in short shelf life periods. 26−29 Also, nanosuspensions produced by liquid AS crystallization tend to have low API concentrations and, thus, may require large dose volumes to achieve an effective dose.…”

Section: Introductionmentioning

confidence: 99%

Impact of Additives on Drug Particles during Liquid Antisolvent Crystallization and Subsequent Freeze-Drying

Ghosh,

Rasmuson,

Hudson

2023

Org. Process Res. Dev.

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The impact of single or combinations of additives on the generation of nanosuspensions of two poorly water-soluble active pharmaceutical ingredients (APIs), fenofibrate (FF) and dalcetrapib (DCP), and their isolation to the dry state via antisolvent (AS) crystallization followed by freeze-drying was explored in this work. Combinations of polymeric and surfactant additives such as poly(vinyl alcohol) or hydroxypropyl methyl cellulose and sodium docusate were required to stabilize nanoparticles (∼200−300 nm) of both APIs in suspension before isolation to dryness. For both FF and DCP, multiple additives generated the narrowest, moststable particle size distribution, with the smallest particles in suspension, compared with using a single additive. An industrially recognized freeze-drying process was used for the isolation of these nanoparticles to dryness. When processed by the liquid AS crystallization followed by freeze-drying in the presence of multiple additives, a purer monomorphic powder for FF resulted than when processed in the absence of any additive or in the presence of a single additive. It was noted that all nanoparticles freeze-dried in the presence of additives had a flat, flaky habit resulting in large surface areas. Agglomeration occurred during freeze-drying, resulting in micron-size particles. However, after freeze-drying, powders produced with single or multiple additives showed similar dissolution profiles, irrespective of aging time before drying, thus attenuating the advantage of multiple additives in terms of size observed before the freeze-drying process.

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The technology for improving stability of nanosuspensions in drug delivery

Cited by 18 publications

References 161 publications

Formulation, Optimization, and Evaluation of Moringa oleifera Leaf Polyphenol-Loaded Phytosome Delivery System against Breast Cancer Cell Lines

Formulation, Optimization, and Evaluation of Moringa oleifera Leaf Polyphenol-Loaded Phytosome Delivery System against Breast Cancer Cell Lines

Formulation Strategies of Nanosuspensions for Various Administration Routes

Impact of Additives on Drug Particles during Liquid Antisolvent Crystallization and Subsequent Freeze-Drying

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