Formulation and in-Vitro-in-Vivo Evaluation of Alginate-Chitosan Microspheres of Glipizide by Ionic Gelation Method

Abstract

Objective: This work is aimed to formulate and evaluate alginate-chitosan microspheres of glipizide for the effective use in the treatment of diabetes.Methods: Sustained release (SR) microspheres were prepared by gentle mixing of polymers in water with the drug by agitation. The polymers used were sodium alginate and chitosan, which was extruded into 5% calcium chloride solution to produce microspheres by ionic gelation method.Results: Single unit dosage form of glipizide causes gastric irritation. When converted into the multiple unit dosage forms, it will release the drug evenly throughout the stomach causing suppression of irritation. The aim of the study was to formulate and evaluate alginate-chitosan microspheres, for SR of the chosen drug. The particle size of microspheres was in the range of 200-500 µ, maximum mucoadhesive property observed was 88.2±0.50% for formulation GCS7, maximum swelling index was 27.0% for GCS7, and the maximum entrapment was 89.1±0.28% for GCS6 formulation. It showed better in-vitro release between 80% and 90% for GCS1 and GCS2 formulation and in formulation GCS3, 50-60% reduction in plasma glucose level than conventional dosage forms when tested in-vivo. The work also aims to study various parameters affecting the behavior of microspheres in oral dosage form. Conclusion:Drugs with short half life that are absorbed from the gastrointestinal tract (GIT) are eliminated rapidly from the blood flow. To avoid this, the oral SR was developed as this formulation released the drug slowly into the GIT and maintained a stable drug concentration in the serum for a longer duration of time.

Preparation and Characterization of Porous Hydroxyapatite and Alginate Composite Scaffolds for Bone Tissue Engineering

“…Alginate is highly hydrophilic that can form stable hydrogels in the presence of certain divalent cations, such as Ca2+, Mg2+, Fe2+, Ba2+, or Sr2+. Ca2+ is one of the most commonly used divalent cations to ionically crosslink with alginate [26,27].…”

Study on the Effect of Alginate, Type of Cross Linkers, and Mucoadhesive Polymers on Drug Release From Lovastatin-Loaded Mucoadhesive Cross-Linked Microbeads

“…The surface morphology of microbeads was explored using SEM (USA model). A known quantity of dried alginate beads were placed or spread on a brass stub using double-sided adhesive tape and made electrically conductive by coating with a thin layer of gold, and SEM images were seen at various accelerating voltage [15,16]. These test samples were then randomly scanned, and photomicrographs were taken care.…”

“…Carboxymethyl cellulose in conjunction with sodium alginate in equal proportions with different curing agents naming aluminum chloride (LF8), barium chloride (LF17), and calcium chloride (LF18) at same concentration, i.e., 5% w/v to modulate drug loading, shape, surface, and drug release kinetics profile in sustained manner [23,24]. After 2 h of dissolution studies, drug release in 0.1N HCL buffer medium was found to be at rate of 16 In initial span of 2 h. The intensity of swelling of beads is to a minimum extent in the presence of acidic medium, which is due to alginate was protonated into insoluble form of alginic acid and the creation of intermolecular and intra molecular hydrogen bonding between the two used polymers, the less swelling should reduce the matrix permeability and limit the drug diffusion at acidic atmosphere and the force of H 2bond is more noteworthy than the repulsive forces, the microbeads are kept in a contracted state in acidic medium, and the alginate microspheres shrink due to tightening of the gel meshwork and the drug is discharged slowly. The rate of swelling is significantly increased than acidic medium (0.1N HCL).…”

<p>The Oral Administration of Lidocaine HCl Biodegradable Microspheres: Formulation and Optimization</p>

“…One recent study reported the oral administration of LID HCL prior to anesthesia for laparoscopy. 18 Other research studies have described the oral delivery of microspheres, consisting of Alginate (ALG) and Chitosan (CS) as mucoadhesive polymers. These microspheres were successfully combined with various drugs, such as glipizide, 19 insulin, 20 ranitidine, 21 metformin, 22 diclofenac, 23 and various other drugs, 24 and showed improved solubility and bioavailability.…”