Unknown

Dataset Information

0

Enhanced Oral Absorption of Icaritin by Using Mixed Polymeric Micelles Prepared with a Creative Acid-Base Shift Method.


ABSTRACT: The purpose of this study was to develop mixed polymeric micelles with high drug loading capacity to improve the oral bioavailability of icaritin with Soluplus® and Poloxamer 407 using a creative acid-base shift (ABS) method, which exhibits the advantages of exclusion of organic solvents, high drug loading and ease of scaling-up. The feasibility of the ABS method was successfully demonstrated by studies of icaritin-loaded polymeric micelles (IPMs). The prepared IPMs were characterized to have a spherical shape with a size of 72.74 ± 0.51 nm, and 13.18% drug loading content. In vitro release tests confirmed the faster release of icaritin from IPMs compared to an oil suspension. Furthermore, bioavailability of icaritin in IPMs in beagle dogs displayed a 14.9-fold increase when compared with the oil suspension. Transcellular transport studies of IPMs across Caco-2 cell monolayers confirmed that the IPMs were endocytosed in their intact forms through macropinocytosis, clathrin-, and caveolae-mediated pathways. In conclusion, the results suggested that the mixed micelles of Soluplus® and Poloxamer 407 could be a feasible drug delivery system to enhance oral bioavailability of icaritin, and the ABS method might be a promising technology for the preparation of polymeric micelles to encapsulate poorly water-soluble weakly acidic and alkaline drugs.

SUBMITTER: Tang C 

PROVIDER: S-EPMC8201319 | biostudies-literature |

REPOSITORIES: biostudies-literature

Similar Datasets

| S-EPMC5568702 | biostudies-other
| S-EPMC4829353 | biostudies-literature
| S-EPMC6956019 | biostudies-literature
| S-EPMC8803101 | biostudies-literature
| S-EPMC6523239 | biostudies-literature
| S-EPMC7558956 | biostudies-literature
2024-11-21 | PXD057444 | Pride
| S-EPMC4201986 | biostudies-literature
| S-EPMC3625707 | biostudies-literature
| S-EPMC9696676 | biostudies-literature