Engineering pH-Dependent Orally Disintegrating Tablets for Modified Indomethacin Release: A Polymer-Based Approach

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Drug Delivery Systems

Background:

• pH-sensitive polymers are crucial for targeted drug release in pharmaceutical formulations.
• Orally disintegrating tablets (ODTs) offer improved patient compliance, but achieving controlled release within them presents challenges.
• Indomethacin (IND), an anti-inflammatory drug, requires careful formulation to minimize gastrointestinal side effects.

Purpose of the Study:

• To develop delayed-release orally disintegrating tablets (ODTs) for indomethacin (IND) using pH-dependent polymers.
• To investigate the impact of polymer particle size on the mechanical and pharmaceutical properties of IND-containing pellets and ODTs.
• To optimize pellet formulation for balanced integrity and controlled drug release characteristics.

Main Methods:

• Indomethacin (IND) was incorporated into pellets using Eudragit L100, a pH-dependent polymer, via extrusion spheronization with varying particle sizes (45, 60, 93 µm).
• Pellets were characterized for mechanical properties (Young's modulus, tensile strength) and pharmaceutical properties (aspect ratio, yield).
• Pellets were embedded into ODT matrices, and their disintegration time and drug release profiles in acidic (pH 1.2) and alkaline (pH 6.8) media were evaluated.

Main Results:

• Pellet particle size did not significantly affect Young's modulus (YM), indicating consistent elastic properties across sizes.
• Pellet tensile strength correlated positively with YM, ensuring structural integrity under compression.
• Pellets made from 63 µm Eudragit L100 demonstrated optimal mechanical and pharmaceutical properties, yielding ODTs with rapid disintegration (14 ± 0.6 s) and modified IND release.
• The formulation achieved delayed release in acidic conditions (pH 1.2) and immediate release in neutral/alkaline conditions (pH 6.8), confirming pH-dependent drug release.

Conclusions:

• Optimized pellet integrity is essential for achieving pH-dependent drug release in ODTs.
• The 63 µm Eudragit L100 pellets provide a promising formulation strategy for controlled indomethacin release in ODTs.
• This approach enhances drug delivery, potentially improving patient compliance and reducing side effects for irritant drugs, especially in elderly populations.