The invention relates to the technical field of pharmaceutical preparations, and particularly provides colon-targeted pH-responsive nano-
liposome and application thereof in improving oral
bioavailability of
saponin. Aiming at the problems of
gastric acid damage,
small intestine metabolism inactivation and low colon
absorption efficiency during oral delivery of
saponin, a three-layer core-shell structure design is adopted, wherein an inner core is composed of a
saponin-
phospholipid crystal compound; the middle layer is a
chitosan-PEG bimolecular layer, and pH response release is realized in a colon environment with pH of 7.4; and the outer layer is modified with a
folic acid-PE conjugate to enhance colon
cell targeted recognition. The uniform nanoparticles with the particle size of 80 + / -5 nm are prepared by combining a gradient pH
drug loading method with a microfluidic focusing technology. According to the preparation, the saponin
bioavailability (AUC0-12 reaches 43.31 h.
Microgram / mL) is remarkably improved, and the colon targeting property (the
cell uptake rate is 52.9%) is enhanced. The innovativeness is that the gastrointestinal segmented protection and accurate colon release are synergistically realized through a multi-layer
functional design, and the solubilization-
permeation paradox of the traditional delivery technology is broken through.