“…The drug concentration was examined under the conditions of 0.5% surfactant, antisolvent and solvent ratio of 1:7, stirring rate of 950 rpm, temperature of 25°C, and stirring time of 10 minutes. The effect of drug concentration of 20,25,30,35,40,50, and 60 mg/mL on the mean particle size of the resulting LE-NPs suspension was determined. The results ( Figure 3C) showed that as the drug concentration increased (from 20 to 50 mg/mL), the mean particle size decreased.…”
Section: Drug Concentrationmentioning
confidence: 99%
“…35,36 Compared with other micronization technologies, LAP has advantages of simplicity, easy operation, and lower cost, and can thus be used for industrial production. 35 This technology has been successfully applied in pharmaceutical industry to prepare resveratrol, 37 curcumin, 38 catechins, 39 rifampicin, 40 and amphotericin B. 32 However, application of LAP to prepare LE-NPs has not been reported previously.…”
Background: Lutein ester (LE) is an important carotenoid fatty acid ester. It is a form in which lutein is present in nature and is produced by free non-esterification and fatty acid esterification. LE is one of the safe sources of lutein. Increasing lutein intake can prevent and treat age-related macular degeneration. In addition, it can effectively inhibit gastric cancer, breast cancer, and esophageal cancer. However, the poor aqueous solubility of LE has impeded its clinical applications. Objective: The objective of this study was to prepare lutein ester nanoparticles (LE-NPs) by liquid antisolvent precipitation techniques to improve the bioavailability of LE in vivo and improve eye delivery efficiency. Materials and methods: The physical characterization of LE-NPs was performed, and their in vitro dissolution rate, in vitro antioxidant capacity, in vivo bioavailability, tissue distribution, and ocular pharmacokinetics were studied and evaluated. Results: The LE freeze-dried powder obtained under the optimal conditions possessed a particle size of ~164.1±4.3 nm. The physical characterization analysis indicated the amorphous form of LE-NPs. In addition, the solubility and dissolution rate of LE-NPs in artificial gastric juice were 12.75 and 9.65 times that of the raw LE, respectively. The bioavailability of LE-NPs increased by 1.41 times compared with that of the raw LE. The antioxidant capacity of LE-NPs was also superior to the raw LE. The concentration of lutein in the main organs of rats treated with the LE-NPs was higher than that in rats treated with the raw LE. The bioavailability of LE-NPs in rat eyeballs was found to be 2.34 times that of the original drug. Conclusion: LE-NPs have potential application as a new oral pharmaceutical formulation and could be a promising eye-targeted drug delivery system.
“…Another example of successful encapsulation but with lower drug loading and precipitation yield is that of a tuberculous drug, rifampicin [31]. Solid dispersions of rifampicin loaded in an ethyl cellulose matrix were obtained exhibiting a drug loading up to 38.5% and a drug precipitation yield up to 77.2%.…”
Supercritical fluid (SCF) technology has been applied to drug product development over the last thirty years and drug particle generation using SCFs appears to be an efficient way to carry out drug formulation which will form end-products meeting targeted specifications. This article presents an overview of drug particle design using SCFs from a rather different perspective than usual, more focused on chemical and process engineering aspects. The main types of existing processes are described in a concise way and a focus is put on how to choose the right operating conditions considering both thermodynamic and hydrodynamic aspects. It is shown that the operating conditions and parameters can be easily optimized so as to facilitate the further process scale-up. Furthermore, the new trends in particle generation using SCFs are introduced, related either to new types of drug medicines that are treated or new ways of process implementation methods.
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