Pharmacokinetics and biodegradation performance of a hydroxypropyl chitosan derivative

Abstract

Hydroxypropyl chitosan (HP-chitosan) has been shown to have promising applications in a wide range of areas due to its biocompatibility, biodegradability and various biological activities, especially in the biomedical and pharmaceutical fields. However, it is not yet known about its pharmacokinetics and biodegradation performance, which are crucial for its clinical applications. In order to lay a foundation for its further applications and exploitations, here we carried out fluorescence intensity and GPC analyses to determine the pharmacokinetics mode of fluorescein isothiocyanate-labeled HP-chitosan (FITC-HP-chitosan) and its biodegradability. The results showed that after intraperitoneal administration at a dose of 10 mg per rat, FITC-HP-chitosan could be absorbed rapidly and distributed to liver, kidney and spleen through blood. It was indicated that FITC-HP-chitosan could be utilized effectively, and 88.47% of the FITC-HP-chitosan could be excreted by urine within 11 days with a molecular weight less than 10 kDa. Moreover, our data indicated that there was an obvious degradation process occurred in liver (< 10 kDa at 24 h). In summary, HP-chitosan has excellent bioavailability and biodegradability, suggesting the potential applications of hydroxypropyl-modified chitosan as materials in drug delivery, tissue engineering and biomedical area.

Investigation of the Effects of Molecular Parameters on the Hemostatic Properties of Chitosan

“…Compared with chitosan (CS-D3 & CS-M1), O -carboxymethyl chitosan (CS-S1) showed the appearance of new absorptions at 1593 and 1411 cm −1 , which were ascribed to the asymmetric and symmetric stretching vibrations of -COO, as shown in Figure 2d, indicating the carboxymethylation of chitosan. Similarly, in the spectrum of hydroxypropyl chitosan (CS-S2) given in Figure 2e, new absorption bands at 2973 and 1376 cm −1 were assigned to the stretching and bending of the -CH 3 , which were in agreement with the results in References [28,29], confirming the successful hydroxypropylation of chitosan. In the spectrum of chitosan acid salts, as shown in Figure 2f,g, compared with that of the original chitosan (CS-D3), the broad absorption band at about 3400 cm −1 became wider and weaker, which might be due to the formation of NH 3 + in the molecule.…”

In vitro evaluation of the biodegradability of chitosan–genipin hydrogels

“…76,77 Studies in rats show that >80% of administered chitosan is excreted in urine within approximately 11 day. 78,79 When glucosamine or N -acetylglucosamine are intravenously administrated in humans, both amino-monosaccharides are readily eliminated from the blood, with over 50% excreted in the urine. 80 As chitosan monosaccharide units are smaller than the degradation particles of chitosan–genipin hydrogels, this suggests that the hydrogels are not completely degraded by lysozyme, with some crosslinks remaining intact.…”

Chitosan and Chitooligosaccharide: The Promising Non-Plant-Derived Prebiotics with Multiple Biological Activities

“…Hepatic enzymes play a dominant role in the process of degrading and metabolizing chitosan and COS. The final degradation products of chitosan and COS were primarily excreted from the body through the kidney in urine at low MWs [ 45 ]. The pharmacokinetic process of chitosan and COS is illustrated in Figure 2 .…”