The Pharmacokinetic Profile of Freeze-dried Cyclosporine A-Eudragit S100 Nanoparticle Formulation in Dogs

Abstract

The pharmacokinetic profile of freeze-dried cyclosporine A-Eudragit S100 nanoparticles (CyA-S100-NP)was studied with a random two-way crossover study in dogs. The drug blood concentration was determined by internal standard HPLC method after oral administration of CyA-S100-NP and Neoral. Pharmacokinetics parameters were calculated by 3P97 program. The concentration-time data were fitted as a two-compartment open model. The AUC of CyA-S100-NP was higher than that of Neoral(P<0.05), while the CL significantly decreased(P<0.05). The relative bioavailability of CyA-S100-NP were 135.9% compared with Neoral. The bioavailability of CyA was significantly improved. CyA-S100-NP was a potential drug for developing a new CyA nanoparticles solid formulation.

Loading of doxorubicin on poly(methyl methacrylate-co-methacrylic acid) nanoparticles and release study

“…This material is the poly(methyl methacrylate (MMA)-co-methacrylic acid (MAA)) copolymer or P(MMA-co-MAA), in a MMA:MAA molar ratio of 0.64:0.36, which is similar to Eudragit S100 (ES 100), a polymer widely used in the elaboration of drug-loaded pills due to its water solubility at pH >7 [24]. Although the preparation of ES 100 NP with mean diameters ranging from 50 to 700 nm, loaded with different drugs, have been documented [25][26][27][28][29][30][31], obtaining NP from a copolymer similar to ES 100 loaded with drugs and with diameters less than 50 nm has only been reported by our group [32,33].…”

Biocompatible and Biodegradable Ultrafine Nanoparticles of Poly(Methyl Methacrylate-co-Methacrylic Acid) Prepared via Semicontinuous Heterophase Polymerization: Kinetics and Product Characterization

“…The processes involved usually include the dissolution of a drug-copolymer mixture in a suitable solvent which is subsequently evaporated to finally obtain the drug-copolymer particles. These particles usually show mean diameters in the order of hundred nanometers [2][3][4][5][6][7][8][9][10][11]; the exception is the work of Dai et al [3] who obtained drug-loaded nanoparticles with 37 nm in mean diameter, as measured by quasi-elastic light scattering (QLS). It is noticeable that none of these processes include the polymerization step.…”

Development of an enteric nanoparticle of marine sulfated polysaccharide propylene glycol alginate sodium sulfate for oral administration: formulation design, pharmacokinetics and efficacy

“…The result showed that PSS was submerged and dissolved quickly in the medium because PSS is a highly water‐soluble drug. The cumulative release percentage of PSS was approximately 100% in the first 2 h. While enteric PSS‐NP exhibited significant pH sensitivity, there was a slow release in the simulated gastric medium with the cumulative release percentage of PSS below 10% in the first 2 h. Then, the release profile of enteric PSS‐NP in the pH 6.8 medium was significantly different from that in the acid medium and there was a burst release of PSS from enteric nanoparticles in the first 1 h. This burst effect may be caused by the drug absorbed on the surface of nanoparticles . In addition, the dissolution of the Eudragit L30D‐55 in pH 6.8 medium could also lead the burst release of PSS.…”