Abstract
In this work, dasatinib (DAS) nanoemulsion and nanocrystal are produced by high-gravity technology that approaches to practical mass production. The drug nanoformulations were systematically characterized and evaluated. At a low high-gravity level (β) = 47, nanoemulsion droplets were 16.15 ± 0.42 nm with a PDI of 0.122 ± 0.021. The nanoemulsion’s size and active pharmaceutical ingredient (API) content remained stable at long-term (4 months) freeze–thaw and dilution experiments. At a high β = 188, the as-prepared nanocrystal was lamellar with a short diameter of about 200 nm and a long diameter of about 750 nm. In vitro performances demonstrated the nanoemulsion displayed higher cytotoxicity on MDA-MB-231 tumor cells, Caco-2 cell permeability and drug release than that of the nanocrystal, indicating that nanoemulsion should be an ideal alternative for dasatinib oral administration.
Highlights
Pharmaceutics 2022, 14, 197. https://Oral administration is the preferred route for drug delivery due to its painless convenience and cost effectiveness [1–3]
According to Taylor’s equation, which emphasizes the pivotal role of amphiphilic surfactants in reducing interfacial tension and enhancing emulsion stability, RH 40 was chosen after being compared with other common surfactants with the aid of the pseudo-ternary phase diagram and FDA’s excipient dosage data. 1,2-propanediol was selected as co-surfactant, the ratio of surfactant to co-surfactant (Km) was 2:1 and the amount of surfactant and co-surfactant were minimized as much as possible
A DASbynanoemulsion and nanocrystal for oral drug delivery mass were sucsuccessfully prepared high-gravity technology, which approaches to practical production
Summary
Pharmaceutics 2022, 14, 197. https://Oral administration is the preferred route for drug delivery due to its painless convenience and cost effectiveness [1–3]. The pharmaceutical industry has shown an increasing desire to formulate poorly water-soluble drugs as nanosized formulations with the goal of improving dissolution rate, enhancing bioavailability, eliminating food effects, and improving efficacy and safety. Nanoemulsion and nanocrystal formulations have proved effective to improve the oral bioavailability of hydrophobic drugs with an increasing dissolution rate, eliminating food effects, and improving efficacy and safety [5–10]. Drug nanocrystals, such as sirolimus (Rapamune® ), aprepitant (Emend® ), fenofibrate (Tricor® ) and drug nanoemulsions, i.e., cyclosporine (Neoral® , Gengraf® ), saquinavir (Fortovase® ), ritonavir (Norvir® ), have been approved by the FDA for clinical application [11,12]
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