Development of cyclosporine A nanosuspension: cytotoxicity and permeability on Caco-2 cell lines

Pinar, Sıla Gülbağ; Pezik, Esra; Ağardan, Başaran Mutlu; Çelebi, Nevin

doi:10.1080/10837450.2021.2020817

Cited by 6 publications

(2 citation statements)

References 44 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The corresponding injectable formulation consists of a large amount of Cremophor EL (a polyethoxylated castor oil) and alcohol to achieve the desired solubility. This has resulted in safety issues, such as a potential risk of intolerability at the injection site as well as anaphylaxis reactions [ 49 , 50 , 51 , 52 , 53 ]. Thus, there is a strong desire to develop alternative formulations of CsA without the need for excipients, such as Cremophor EL.…”

Section: Resultsmentioning

confidence: 99%

A New Approach for Preparing Stable High-Concentration Peptide Nanoparticle Formulations

Hu,

Zang,

Tam

et al. 2023

Pharmaceuticals

View full text Add to dashboard Cite

The subcutaneous administration of therapeutic peptides would provide significant benefits to patients. However, subcutaneous injections are limited in dosing volume, potentially resulting in high peptide concentrations that can incur significant challenges with solubility limitations, high viscosity, and stability liabilities. Herein, we report on the discovery that low-shear resonant acoustic mixing can be used as a general method to prepare stable nanoparticles of a number of peptides of diverse molecular weights and structures in water without the need for extensive amounts of organic solvents or lipid excipients. This approach avoids the stability issues observed with typical high-shear, high-intensity milling methods. The resultant peptide nanosuspensions exhibit low viscosity even at high concentrations of >100 mg/mL while remaining chemically and physically stable. An example nanosuspension of cyclosporine nanoparticles was dosed in rats via a subcutaneous injection and exhibited sustained release behavior. This suggests that peptide nanosuspension formulations can be one approach to overcome the challenges with high-concentration peptide formulations.

show abstract

Section: Resultsmentioning

confidence: 99%

A New Approach for Preparing Stable High-Concentration Peptide Nanoparticle Formulations

Hu,

Zang,

Tam

et al. 2023

Pharmaceuticals

View full text Add to dashboard Cite

show abstract

“…The active substance is dispersed in this dispersion medium, and this coarse suspension is added to the milling chamber [ 35 ]. An average of one-third of the chamber is filled with dispersion medium and one-third with milling beads; the remaining one-third is left empty to provide the necessary space for milling [ 36 ]. Beads (zirconium, stainless steel, etc.)…”

Section: Preparation Methods For Nanosuspensionsmentioning

confidence: 99%

Formulation Strategies of Nanosuspensions for Various Administration Routes

et al. 2023

Self Cite

View full text Add to dashboard Cite

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.

show abstract

Amino Acid Composition, Antioxidant, α-Glucosidase and α-Amylase Inhibitory Activities of the Enzymic Polypeptide from Acer truncatum Seed Meal

Liang

et al. 2022

Int J Pept Res Ther

View full text Add to dashboard Cite

Development of cyclosporine A nanosuspension: cytotoxicity and permeability on Caco-2 cell lines

Cited by 6 publications

References 44 publications

A New Approach for Preparing Stable High-Concentration Peptide Nanoparticle Formulations

A New Approach for Preparing Stable High-Concentration Peptide Nanoparticle Formulations

Formulation Strategies of Nanosuspensions for Various Administration Routes

Amino Acid Composition, Antioxidant, α-Glucosidase and α-Amylase Inhibitory Activities of the Enzymic Polypeptide from Acer truncatum Seed Meal

Contact Info

Product

Resources

About