Tacrolimus-Loaded Superabsorbent Hydrogels: Formulation, Evaluation, and Therapeutic Potential.

Area of Science:

• * Pharmaceutical Sciences
• * Polymer Chemistry
• * Drug Delivery Systems

Background:

• * Tacrolimus, a BCS class-II drug, suffers from poor water solubility and low bioavailability.
• * Sustained therapeutic concentrations of tacrolimus are crucial for preventing transplant rejection.
• * Chitosan-based superabsorbent hydrogels were investigated for enhanced tacrolimus delivery.

Purpose of the Study:

• * To develop pH-sensitive, tacrolimus-loaded hydrogels for sustained drug release.
• * To optimize hydrogel formulation for improved entrapment efficiency and bioavailability.
• * To evaluate the physicochemical properties and in vitro drug release kinetics.

Main Methods:

• * Free-radical polymerization technique used for hydrogel synthesis with chitosan, acrylamide, and potassium persulfate.
• * Formulation design and optimization conducted using Design Expert software.
• * Evaluation of swelling behavior, porosity, entrapment efficiency, and in vitro drug release.

Main Results:

• * Hydrogels exhibited good swelling capacity and porosity (77.7-232.16%), indicating a suitable network for drug delivery.
• * Sol-gel fraction ranged from 4.65-17.71% and 82.29-95.35%, respectively.
• * Sustained release of 59.9% tacrolimus over 8 hours was achieved, demonstrating effective controlled release.

Conclusions:

• * The developed chitosan hydrogels successfully entrapped tacrolimus and provided sustained release.
• * The formulation and preparation method are efficient for delivering poorly soluble drugs like tacrolimus.
• * This approach offers a promising strategy for improving tacrolimus bioavailability and therapeutic efficacy.