Development and In Vitro Evaluation of Oteseconazole-Loaded Mucoadhesive Microspheres for Controlled Oral Drug Release

Abstract

Mucoadhesive microspheres are investigated as multiparticulate carriers intended to prolong contact with mucosal surfaces and modulate drug release. Oteseconazole is an azole antifungal; however, the clinical rationale and intended site of action for an oral mucoadhesive formulation must be established separately from in vitro formulation performance. To prepare and characterize oteseconazole-loaded microspheres using an emulsion-based crosslinking approach and to compare six formulations (F1–F6) with different Carbopol 940 levels and crosslinking conditions. According to the supplied study record, microspheres contained oteseconazole, Carbopol 940, chitosan, sodium alginate, hydroxypropyl methylcellulose (HPMC), and xanthan gum. The reported evaluations included particle size, percentage yield, entrapment efficiency, swelling index, drug content, wash-off retention, in vitro release, and antifungal activity against Candida albicans. The original experimental record should be consulted to confirm procedural details, replicates, and statistical methods before submission. Reported particle size increased from 182 µm (F1) to 270 µm (F6), and percentage yield increased from 71.5% to 87.1%. Entrapment efficiency increased from 67.2% to 91.6%, swelling index from 88% to 122%, and reported mucoadhesion from 68% to 95%. Drug content ranged from 94.2% to 99.0%. At 12 h, cumulative release ranged from 98% for F1 to 78% for F6. The reported inhibition zone against C. albicans increased from 18.2 ± 0.6 mm to 26.3 ± 0.7 mm. F6 had the highest reported entrapment efficiency, swelling index, mucoadhesion, wash-off time, and inhibition-zone diameter, while showing the lowest 12-h drug release. These data suggest a formulation trend toward slower release with higher polymer content. They do not establish improved oral bioavailability, clinical efficacy, or targeted antifungal therapy; such claims require additional validated experiments.