Formulation, process, and storage strategies for lyophilizates of lipophilic nanoparticulate systems established based on the two models paliperidone palmitate and solid lipid nanoparticles

Trenkenschuh, Eduard; Savšek, Ula; Frieß, Wolfgang

doi:10.1016/j.ijpharm.2021.120929

Cited by 5 publications

(7 citation statements)

References 43 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Lyoprotectants were added to NRG-NSps solution at a concentration of 0.5% ( w / v ), and then lyophilized for 24 h after freezing at −80 °C (ALPHR 2–4 LD plus, CHRIST, Germany) [ 44 ]. The white powder was dispersed in 1 mL deionized water, and the particle size and PDI values were recorded.…”

Section: Methodsmentioning

confidence: 99%

Preparation of Naringenin Nanosuspension and Its Antitussive and Expectorant Effects

et al. 2022

View full text Add to dashboard Cite

Naringenin (NRG) is a natural flavonoid compound abundantly present in citrus fruits and has the potential to treat respiratory disorders. However, the clinical therapeutic effect of NRG is limited by its low bioavailability due to poor solubility. To enhance the solubility, naringenin nanosuspensions (NRG-NSps) were prepared by applying tocopherol polyethylene glycol succinate (TPGS) as the nanocarrier via the media-milling method. The particle size, morphology, and drug-loading content of NRG-NSps were examined, and the stability was evaluated by detecting particle size changes in different physiological media. NRG-NSps exhibited a flaky appearance with a mean diameter of 216.9 nm, and the drug-loading content was 66.7%. NRG-NSps exhibited good storage stability and media stability. NRG-NSps presented a sustainable release profile, and the cumulative drug-release rate approached approximately 95% within 7 d. NRG-NSps improved the antitussive effect significantly compared with the original NRG, the cough frequency was decreased from 22 to 15 times, and the cough incubation period was prolonged from 85.3 to 121.6 s. Besides, NRG-NSps also enhanced expectorant effects significantly, and phenol red secretion was increased from 1.02 to 1.45 μg/mL. These results indicate that NRG-NSps could enhance the bioavailability of NRG significantly and possess a potential clinical application.

show abstract

Section: Methodsmentioning

confidence: 99%

Preparation of Naringenin Nanosuspension and Its Antitussive and Expectorant Effects

et al. 2022

View full text Add to dashboard Cite

show abstract

“…The stressful conditions of the freeze-drying process affected the physicochemical characteristics of all of the PEG formulations compared to CO-cSLNs. Previous studies also reported a rise in particle size after freeze-drying, providing further evidence of the effects of lyophilization on nanoparticles [26,30,[33][34][35][36].…”

Section: Lyophilization Of the Peg-cslnsmentioning

confidence: 52%

“…Furthermore, the formulation containing Brij S100 produced the smallest particle size (166.2 ± 23.1 nm), accompanied by the highest employed quantity of PEG (350 mg; Table 1). The incorporation of polymers, such as PEG, onto the nanoparticle surface can enhance colloidal stability and prolong circulation time through steric stabilization [22,26]. These effects are influenced by the molecular weight and structure characteristics of PEG and are directly correlated with the length and surface density of the PEG employed [22].…”

Section: Factorial Studymentioning

confidence: 99%

“…Thus, for the entire product to be well lyophilized, the process should be performed at a minimum of 10−20 degrees lower than the aforementioned temperature [30]. Therefore, the freezing temperature used in the lyophilization cycle was −55 • C to ensure vitrification of the trehalose matrix and the appropriate lyophilization of all formulations [26].…”

Section: Freeze-drying Of Peg-cslns 231 Glass Transition Temperature ...mentioning

confidence: 99%

See 1 more Smart Citation

Comparative Analysis of the Physicochemical and Biological Characteristics of Freeze-Dried PEGylated Cationic Solid Lipid Nanoparticles

Narváez-Narváez,

Duarte-Ruiz,

Jiménez-Lozano

et al. 2023

Pharmaceuticals

View full text Add to dashboard Cite

Cationic solid-lipid nanoparticles (cSLNs) have become a promising tool for gene and RNA therapies. PEGylation (PEG) is crucial in enhancing particle stability and protection. We evaluated the impact of PEG on the physicochemical and biological characteristics of cholesteryl-oleate cSLNs (CO-cSLNs). Several parameters were analyzed, including the particle size, polydispersity index, zeta potential, shape, stability, cytotoxicity, and loading efficiency. Five different formulations with specific PEGs were developed and compared in both suspended and freeze-dried states. Small, homogeneous, and cationic suspended nanoparticles were obtained, with the Gelucire 50/13 (PEG-32 hydrogenated palm glycerides; Gelucire) and DSPE-mPEG2000 (1,2-distearoyl-phosphatidylethanolamine-methyl-polyethyleneglycol conjungate-2000; DSPE) formulations exhibiting the smallest particle size (~170 nm). Monodisperse populations of freeze-dried nanoparticles were also achieved, with particle sizes ranging from 200 to 300 nm and Z potential values of 30–35 mV. Notably, Gelucire again produced the smallest particle size (211.1 ± 22.4), while the DSPE and Myrj S100 (polyoxyethylene (100) stearate; PEG-100 Stearate) formulations had similar particle sizes to CO-cSLNs (~235 nm). The obtained PEGylated nanoparticles showed suitable properties: they were nontoxic, had acceptable morphology, were capable of forming SLNplexes, and were stable in both suspended and lyophilized states. These PEG-cSLNs are a potential resource for in vivo assays and have the advantage of employing cost-effective PEGs. Optimizing the lyophilization process and standardizing parameters are also recommended to maintain nanoparticle integrity.

show abstract

“…Many NPs are lyophilized for storage and transportation to increase their stability. However, this strategy does not alter the stability of NPs once administered [ 96 ]. NPs rely on a delicate balance between stability and degradation to effectively release the drug they convey, and this balance must be taken into consideration while designing the NPs.…”

Section: Biological Barriersmentioning

confidence: 99%

Engineering nano-drug biointerface to overcome biological barriers toward precision drug delivery

Waheed

Zhang

et al. 2022

J Nanobiotechnol

View full text Add to dashboard Cite

The rapid advancement of nanomedicine and nanoparticle (NP) materials presents novel solutions potentially capable of revolutionizing health care by improving efficacy, bioavailability, drug targeting, and safety. NPs are intriguing when considering medical applications because of their essential and unique qualities, including a significantly higher surface to mass ratio, quantum properties, and the potential to adsorb and transport drugs and other compounds. However, NPs must overcome or navigate several biological barriers of the human body to successfully deliver drugs at precise locations. Engineering the drug carrier biointerface can help overcome the main biological barriers and optimize the drug delivery in a more personalized manner. This review discusses the significant heterogeneous biological delivery barriers and how biointerface engineering can promote drug carriers to prevail over hurdles and navigate in a more personalized manner, thus ushering in the era of Precision Medicine. We also summarize the nanomedicines' current advantages and disadvantages in drug administration, from natural/synthetic sources to clinical applications. Additionally, we explore the innovative NP designs used in both non-personalized and customized applications as well as how they can attain a precise therapeutic strategy.

show abstract

Formulation, process, and storage strategies for lyophilizates of lipophilic nanoparticulate systems established based on the two models paliperidone palmitate and solid lipid nanoparticles

Cited by 5 publications

References 43 publications

Preparation of Naringenin Nanosuspension and Its Antitussive and Expectorant Effects

Preparation of Naringenin Nanosuspension and Its Antitussive and Expectorant Effects

Comparative Analysis of the Physicochemical and Biological Characteristics of Freeze-Dried PEGylated Cationic Solid Lipid Nanoparticles

Engineering nano-drug biointerface to overcome biological barriers toward precision drug delivery

Contact Info

Product

Resources

About