Chitosan Based Mucoadhesive Microspheres for Oral Insulin Delivery: Formulation, In Vitro Characterization, and Release Kinetics (Research Article)

Author(s): Shilpa Thakkalapally*, Deepika Shamakuri

Abstract: Oral insulin delivery remains a significant challenge due to enzymatic degradation and poor gastrointestinal absorption. This study presents the development and evaluation of chitosan-based mucoadhesive microsphere formulations for oral insulin delivery, with a focus on optimizing a lead formulation and comparing it to a chitosan only control. Microspheres were prepared using various methods, including emulsification crosslinking, electrospray, and membrane emulsification, with chemical modifications such as thiolation and quaternization to enhance performance. The formulations were characterized for particle size, zeta potential, encapsulation efficiency (EE), mucoadhesion, and in vitro release kinetics. The optimized formulation (F2), consisting of carboxymethyl β-cyclodextrin grafted carboxymethyl chitosan hydrogel-based microparticles, demonstrated a particle size of 28.3 ± 2.1 µm, EE of 82.1 ± 2.8%, mucoadhesion force of 0.48 ± 0.03 N/cm², and sustained release of 78% over 12 hours in simulated intestinal fluid (SIF). Compared to the chitosan only formulation (F0), F2 exhibited superior EE, mucoadhesion, and release kinetics. These findings highlight the potential of chitosan-based microspheres for improving oral insulin bioavailability, warranting further in vivo studies.

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