Ameliorated Stomach Specific Floating Microspheres for Emerging Health Pathologies Using Polymeric Konjac...

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Improving oral drug bioavailability often requires strategies to prolong drug residence time in the gastrointestinal tract.
• Domperidone (DoN) is a widely used antiemetic drug with limited oral bioavailability due to rapid absorption and metabolism.

Purpose of the Study:

• To develop and characterize stomach-specific floating microspheres (SSFM) for domperidone (DoN) delivery.
• To enhance the in vivo bioavailability of DoN by increasing its gastric residence time.
• To investigate the potential of polymeric konjac glucomannan (KGM) and Kollidon VA 64 (KVA64) in SSFM formulation.

Main Methods:

• SSFM were prepared using an emulsion cross-linking process with KGM, KVA64, and glutaraldehyde.
• Phase solubility studies were conducted to determine thermodynamic parameters and A_L classes.
• Characterization included particle size analysis, drug content determination, in vitro drug release studies, and morphological analysis (FT-IR, XRD, DSC).
• In vivo pharmacokinetic studies compared the gastric residence time and bioavailability of SSFM with intravenous administration.

Main Results:

• The optimized SSFM exhibited a particle size of 163.71 ± 2.26 µm and high drug content (96.66 ± 0.32%).
• In vitro studies showed sustained drug release over 12 hours (92.62 ± 2.43%).
• Morphological and spectroscopic analyses confirmed the spherical shape and structural integrity of the SSFM.
• In vivo studies demonstrated significantly prolonged mean residence time (17.36 ± 1.4 h) and half-life (10.47 ± 0.6 h) compared to i.v. treatment, indicating enhanced gastric retention and absorption.
• The SSFMs maintained good physical stability for three months at room temperature.

Conclusions:

• Polymeric konjac glucomannan and Kollidon VA 64 are suitable excipients for developing stomach-specific floating microspheres.
• The developed SSFM effectively prolong gastric residence time and enhance domperidone's in vivo bioavailability.
• This formulation strategy holds promise for improving the therapeutic efficacy of drugs with poor oral absorption.