Composite alkali polysaccharide supramolecular nanovesicles improve biocharacteristics and anti-lung cancer activity of natural phenolic drugs via oral administration.

Abstract

Natural phenolic drugs have good safety and various biological activities. However, poor bioavailability and inadequate bioactivity severely limit their application. A novel composite alkali polysaccharide nanovesicle was formed with supramolecule- and nano- technologies to efficiently deliver natural phenolic antitumor drugs. Alkali polysaccharide nanovesicles (ASDLM) containing supramolecular diferuloylmethane (DLM) had the additional effects of alkali polysaccharide nanovesicles and supramolecules of drug and high-molecular-weight polymers. DLM was isolated from the external environment when double loaded by cyclodextrin and nanovesicles; The nanosize, negative/positive charges and supramolecular structure were beneficial attributes that helped to increase the bioavailability and antitumor activity; supramolecular DLM-loaded nanovesicles made of natural biodegradable excipients showed good safety. Compared to free DLM, ASDLM exhibited superior physicochemical characteristics, favorable changes in the in vitro/in vivo kinetic performance, a possible in vitro-in vivo correlation, enhanced in situ gastrointestinal absorption, increased bioavailability, and an elevated anti-lung cancer efficiency. Composite alkali polysaccharide nanovesicles conjugated with supramolecular-/nano- technology may provide a valuable platform for the oral delivery of botanical drugs to meet clinical requirements.