Modulating intestinal mucus barrier for nanoparticles penetration by surfactants.

Improving peroral delivery efficiency is always a persistent goal for both small-molecule and macromolecular drug development. However, intestinal mucus barrier which greatly impedes drug-loaded nanoparticles penetration is commonly overlooked. Therefore, in this study, taking fluorescent labeled PLGA (poly (lactic-co-glycolic acid)) nanoparticles as a tool, the influence of anionic and nonionic surfactants on mucus penetration ability of nanoparticles and their mucus barrier regulating ability were studied.

Effect of Glyceryl Monocaprylate-Modified Chitosan on the Intranasal Absorption of Insulin in Rats.

Nasal administration of insulin showed the attractive potential to improve the compliance of diabetic patients and alleviate mild cognitive impairment of Alzheimer's patients. However, the nasal absorption of insulin was not ideal, limiting its therapeutic effect in clinic. This study was to explore the potential of glyceryl monocaprylate-modified chitosan (CS-GMC) on the intranasal absorption of insulin via in vivo pharmacodynamic experiment in conscious rats.

Enhanced oral insulin delivery via surface hydrophilic modification of chitosan copolymer based self-assembly polyelectrolyte nanocomplex.

It is desirable to design nanoparticles for oral insulin delivery that can cross mucus layer and epithelial membrane in the intestine in the meantime. Thus, using chitosan (CS) as the nanocarrier, the objective of this study is to elucidate the contribution of surface hydrophilic and hydrophobic modification on the oral absorption of insulin and the essential for these two strategies combination. First of all, the polyelectronic nanocomplexes (PEC) based on synthesized CS-g-polyethylene glycol monomethyl ether (mPEG) copolymers with different mPEG graft ratios were prepared by self-assembly method and their physicochemical properties were characterized, and surface hydrophilicity and interaction with mucus were estimated.

Chitosan based polymer-lipid hybrid nanoparticles for oral delivery of enoxaparin.

In the present study, chitosan based polymer-lipid hybrid nanoparticles (PLNs) were prepared by a self-assembly method and their use as the carrier for oral absorption enhancement of enoxaparin was evaluated. The enoxaparin-loaded nanoparticles were composed of chitosan as the polymer and glyceryl monooleate as the lipid with a lipid/polymer mass ratio ranging from 0 to 0.3, and F127 was added as a stabilizer.

Strategies and industrial perspectives to improve oral absorption of biological macromolecules.

Introduction: Therapeutic proteins have become a highly attractive drug of choice due to minimal toxicity, high activity and exquisite specificity. Oral delivery of protein drugs is a very interesting area for research, and, naturally, numerous technologies are required to improve the oral bioavailability of therapeutic proteins.

Areas Covered: This review article systemically generalized the major physiological barriers facing oral macromolecule delivery as well as the current approaches and novel developments in the field, including permeation enhancers, enzyme inhibitors, particulate drug delivery system, ligand delivery system, mucoadhesive delivery system, mucus penetration delivery system and other strategies.