Mucin-Grafted Polyethylene Glycol Microparticles Enable Oral Insulin Delivery for Improving Diabetic Treatment

Abstract

In this study, different ratios of mucin-grafted polyethylene-glycol-based microparticles were prepared and evaluated both in vitro and in vivo as carriers for the oral delivery of insulin. Characterization measurements showed that the insulin-loaded microparticles display irregular porosity and shape. The encapsulation efficiency and loading capacity of insulin were >82% and 18%, respectively. The release of insulin varied between 68% and 92% depending on the microparticle formulation. In particular, orally administered insulin-loaded microparticles resulted in a significant fall of blood glucose levels, as compared to insulin solution. Subcutaneous administration showed a faster, albeit not sustained, glucose fall within a short time as compared to the polymeric microparticle-based formulations. These results indicate the possible oral delivery of insulin using this combination of polymers.

Pre-Formulation Studies: Physicochemical Characteristics and In Vitro Release Kinetics of Insulin from Selected Hydrogels

“…The enhancer cell was immersed in the dissolution vessels. The amount of insulin diffusing through the membrane was determined by spectrophotometry using a CECIL apparatus (CE 3021, Cambridge, United Kingdom) at a wavelength λ = 271 nm [ 31 ]. The linear dependence of absorbance as a function of the concentration of standard solutions was described by the equation y = 0.453x + 0.0072.…”

Helical‐Like Assembly of Nateglinide as Coating for Oral Delivery of Insulin and Their Synergistic Prevention of Diabetes Mellitus

“…[ 8 , 9 , 10 ] The convenience of oral Ins may encourage earlier initiation of Ins therapy, improve patient compliance, and ultimately lead to better glucose control and long‐term outcomes. [ 11 ] Nevertheless, being similar to many protein components, oral Ins still faces significant challenges such as poor gastrointestinal stability, [ 12 , 13 , 14 ] rapid metabolism, [ 15 , 16 , 17 ] quick systemic elimination, and both easy aggregation and difficult absorption face great challenges. [ 18 , 19 , 20 ] Which leads to low therapeutic efficiency.…”

10th Anniversary of Applied Sciences-Invited Papers in Chemistry Section

“…In addition, the coated strawberry achieved the best microbiological preservation when compared with controls. A very interesting use of a combination of polymers for oral drug delivery was presented by Mumuni et al [10]. They evaluated the use of different ratios of mucin-grafted polyethylene glycol-based micro-particles, both in vitro and in vivo, as carriers for the oral delivery of insulin.…”