Oral Insulin

Oral insulin is an exciting area of research and development in the field of diabetology. This brief review covers the various approaches used in the development of oral insulin, and highlights some of the recent data related to novel oral insulin preparation

Eudragit S100 entrapped insulin microspheres for oral delivery

The purpose of this research was to investigate whether Eudragit S100 microspheres have the potential to serve as an oral carrier for peptide drugs like insulin. Microspheres were prepared using water-in oil-in water emulsion solvent evaporation technique with polysorbate 20 as a dispersing agent in the internal aqueous phase and polyvinyl alcohol (PVA)/polyvinyl pyrrolidone as a stabilizer in the external aqueous phase. The use of smaller internal aqueous-phase volume (50 μL) and external aqueous-phase volume (25 mL) containing PVA in the manufacturing process resulted in maximum encapsulation efficiency (81.8%±0.9%). PVA-stabilized microspheres having maximum drug encapsulation released 2.5% insulin at pH 1.0 in 2 hours. In phosphate buffer (pH 7.4), microspheres showed an initial burst release of 22% in 1 hour with an additional 28% release in the next 5 hours. The smaller the volumes of internal and external aqueous phase, the lower the initial burst release. The release of drug from microspheres followed Higuchi kinetics. Scanning electron microscopy of PVA-stabilized microspheres demonstrated spherical particles with smooth surface, and laser diffractometry revealed a mena particle size of 32.51±20 μm. Oral administration of PVA stabilized microspheres in normal albino rabbits (equivalent to 6.6 IU insulin/kg of animal weight) demonstrated a 24% reduction in blood glucose level, with maximum plasma glucose reduction of 76±3.0% in 2 hours and effect continuing up to 6 hours. The area under the percentage glucose reduction-time curve was 93.75%. Thus, our results indicate that Eudragit S100 microspheres on oral administration can protect insulin from proteolytic degradation in the gastrointestinal tract and produce hypoglycemic effect

Chemistry and Pharmacology of GPBAR1 and FXR Selective Agonists, Dual Agonists, and Antagonists

In this review, we summarize the most recent acquisition on natural, semisynthetic, and synthetic steroidal and nonsteroidal ligands, able to interact with FXR and GPBAR1. In the recent years, bile acid receptors FXR and GPBAR1 have attracted the interest of scientific community and companies, as they proved promising targets for the treatment of several diseases, ranging from liver cholestatic disorders to metabolic syndrome, inflammatory states, nonalcoholic steatohepatitis (NASH), and diabetes

Peptides, Proteins and Antibodies

Peptide and protein therapeutics are increasingly able to address a growing range of clinical pathologies and their high specificity and potency combined with low toxicity of metabolic products and minimal potential for drug–drug interactions makes them attractive candidates for clinical development. The pharmaceutical industry is today more in need of delivery technologies that are able to stabilise and effectively deliver therapeutic peptides and proteins across physiological barriers and particularly via non-parenteral routes. Nanoparticulate delivery has the potential to stabilise peptide and protein therapeutics from physical and enzymatic degradation, reduce clearance via the kidneys, prolong plasma half-lives and even target these molecules to the tissue of interest. Nanoparticulate technologies have enabled the delivery of peptide therapeutics via the oral, nasal and pulmonary route and numerous preclinical nano-delivery systems such as polymeric nanoparticles, lipidic nanoparticles and drug–polymer conjugates have been investigated for the delivery of protein therapeutics. In this chapter, a description of these delivery systems and their applications will be discussedNon peer reviewe