De Jaeghere F, Allémann E, Cerny R, Galli B, Steulet AF, Müller I, Schütz H, Doelker E and Gurny R pH-Dependent Dissolving Nano- and Microparticles for Improved Peroral Delivery of a Highly Lipophilic Compound in Dogs AAPS PharmSci 2001; 3 (1) article 8 (https://www.pharmsci.org/scientificjournals/pharmsci/journal/01_08.html).

Figures and Tables

Figure 1.Chemical structure of pH-sensitive Eudragit L100-55.

Table 1. Characteristics and Production Yield of pH-sensitive Nanoparticles and Microparticles Produced by Emulsification-Diffusion and Spray-Drying

* Polydispersity index (0-9 scale)

Figure 2.Size distribution of Eudragit L100-55 microparticles as assessed by laser light diffraction (drug loading 50%).

Figure 3.Scanning electron micrograph of Eudragit L100-55 microparticles (drug loading 50%).

Figure 4.X-ray diffraction pattern of (a) compound RR01, (b) Eudragit L100-55 nanoparticles (drug loading 50%), (c) Eudragit L100-55 microparticles (drug loading 50%), (d) physical mixture of compound RR01 and Eudragit L100-55 (50% of compound RR01), and (e) Eudragit L100-55.

Figure 5.Plasma concentration profiles of compound RR01 after oral administration of the reference formulation (- -), Eudragit L100-55 nanoparticles (- -), and microparticles (- -) (drug loading 5%) to fasted dogs; mean ± SD (n = 6).

Figure 6.Individual dose-normalized AUC0-48h values calculated from the plasma concentrations of compound RR01 obtained after oral administration of the reference formulation (- -), Eudragit L100-55 nanoparticles (- -), and microparticles (- -) (drug loading 5%) to fasted dogs; mean ± SD (n = 6).

Table 2. Pharmacokinetic Parameters of the Test Drug Administered Orally to Fasted Beagle Dogs as Control Suspension and Incorporated into Eudragit L100-55 Particles; Mean (CV, n = 6)