Abstract
Polymeric delivery systems based on microparticles have emerged as a promising approach for peroral insulin delivery. The amount of insulin was quantified by the improved Bradford method. It was shown that water-soluble chitosan/insulin/tripolyphosphate (TPP) mass ratio played an important role in microparticles formation. Stable, uniform, and spherical water-soluble chitosan microparticles (WSC-MPs) with high insulin association efficiency were formed at or close to optimized WSC/insulin/TPP mass ratio. WSC-MPs had higher association efficiency in the pH 4.0 and pH 9.7 of TPP solution. The results showed that association efficiency and loading capacity of insulin-loaded WSC-MPs prepared in 0.01 mol/L HCl of insulin were 48.28 ± 0.90% and 9.52 ± 1.34%. The average size of insulin-loaded WSC-MPs was 292 nm. The presented WSC microparticulate system has promising properties towards the development of an oral delivery system for insulin.
Highlights
In the present paper, insulin was chosen as the model protein
The zone of the opalescence corresponding to a suspension of water-soluble chitosan microparticles (WSC-MPs) was associated with a formulation containing a final water-soluble chitosan (WSC) aqueous solution concentration in the range 1.0-2.0 mg/mL and a final TPP concentration in the range 0.5–1.0 mg/mL, respectively
These conditions were selected for preparation of the WSC-MPs to reach final theoretical WSC/TPP ratios of 6 : 1–8 : 1 (w/w)
Summary
Insulin was chosen as the model protein. It is a well-known 51 amino acids protein, and the oral approach remains the most attractive due to convenience and high patient compliance [1]. The main reasons for the low oral bioavailability of biologicals are presystemic enzymatic degradation and poor penetration of the intestinal membrane [2, 3]. One approach to improve the gastrointestinal uptake of low molecular weight proteins is to bind them to colloidal systems like microparticles (MPs), protecting them from degradation in the gastrointestinal tract and promoting the transport into systemic circulation [5,6,7,8]
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