Clarithromycin-Loaded Mucoadhesive Microspheres for Gastro-Retentive Drug Delivery: Formulation and Characterization Using Tamarind Seed Polysaccharide
Keywords:
Clarithromycin, Tamarind seed polysaccharide, TSP, mucoadhesive microspheres, gastro-retentive drug delivery, controlled release, mucoadhesionAbstract
Clarithromycin, a macrolide antibiotic, is widely used in treating bacterial infections, including Helicobacter pylori. Conventional oral dosage forms often undergo rapid gastrointestinal transit, limiting gastric residence and controlled release. Gastro‑retentive mucoadhesive microspheres offer a promising approach to prolong gastric residence and sustain drug delivery. Tamarind seed polysaccharide (TSP), a natural polymer, was evaluated for developing Clarithromycin microspheres.
Preformulation studies included physical characterization, solubility, pKa, log P, powder‑flow properties, UV estimation, and drug–excipient compatibility. Microspheres were prepared by a single‑emulsion technique, with 29 batches designed using Design‑Expert software by varying drug concentration, TSP concentration, stirring speed, and Span‑80 levels. Responses studied were mucoadhesion, entrapment efficiency, cumulative drug release, and particle size. Optimized microspheres were filled into hard gelatin capsules equivalent to 250 mg Clarithromycin.
Clarithromycin showed a melting point of 218–220°C, pKa 8.35, log P 3.05, and poor solubility in water, but higher solubility in acidic media. FTIR confirmed compatibility with TSP. Microspheres exhibited good flow (angle of repose 26.5°, Hausner’s ratio 1.035, Carr’s index 3.44%). Capsules demonstrated uniform drug content (250.08 ± 1.13 mg), disintegration time of 12.57 min, and satisfactory pharmaceutical quality. In‑vitro dissolution revealed prolonged release: 63.85% at 8 h, 81.76% at 12 h, 95.36% at 18 h, and 97.21% at 20 h.
The study confirms the feasibility of TSP‑based mucoadhesive microspheres for gastro‑retentive controlled release of Clarithromycin, with excellent content uniformity and sustained drug release up to 20 h.
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