Formulation Strategies of Nanosuspensions for Various Administration Routes

Abstract

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.

Environmentally Benign Design of Renewable Oleoresin-Bioenergized Imidacloprid Nanohydrocolloids for Improved Activity, Lower Toxicity, and Agroecological Sustainability

“…Oleoresins are gluey and insoluble in water and can be applied as NSs for easy spray applications, reduced viscosity, increased solubility in water, and delay in crystallization. A NS is a colloidal dispersion that increases the surface area and absorption, boosting the bioavailability. , A combination of imidacloprid and oleoresin increased the bioactivity of the NS (91.56%) as compared with the commercial SC formulation (72.22%) ( Table ). The preparation parameters and composition were significantly impacted by properties like the PDI (0.02 d. nm), zeta potential (−0.32), and particle size (20 nm) of the final NS measured by a Zetasizer apparatus (dynamic light scattering technique) (Nano-ZS90, Malvern, UK) (Figure ).…”

Comparison of the pharmacokinetic characteristics and bioequivalence between two nanosuspension formulations of megestrol acetate in healthy Korean male subjects

“…Additionally, solidification enables the conversion of various formulations, such as powders, tablets or capsules [ 26 ]. Third, nanosuspensions enhance the stability and solubility, thereby reducing variability in bioavailability due to dietary influences [ 26 30 ]. Thus, the use of nanosuspensions with increased solubility and reduced dietary impact in this study is advantageous for real clinical applications.…”

Recent Advances in Nanotechnology for the Treatment of Dry Eye Disease

“…Nanosuspensions [78] Colloidal dispersions where drug particles are reduced to the nanometer scale and dispersed in a liquid medium.…”

“…Various methods, including high-pressure homogenization, media-milling, and precipitation techniques, can be employed to create nanosuspensions. The stabilizers used in the formulation of ophthalmic nanosuspensions often consist of natural, synthetic, or hybrid polymers [ 78 ]. However, the application of nanosuspensions for treating DED is constrained by physical instability issues, such as sedimentation, and potential toxicity arising from the use of surfactants [ 72 ].…”

“…Nanosuspension technology offers a secure and efficient method of delivering hydrophobic drugs to the ocular surface. However, like nanoemulsions, enhancing the physical stability of these nanocarriers is crucial for their practicality [ 66 , 78 ]. For instance, in the study conducted by Wu et al, the chitosan-modified mycophenolate mofetil nanosuspension showed decreased drug clearance compared to the non-chitosan-modified nanosuspensions [ 80 ].…”