Scholarlink

<p>To develop and optimize atogepant-loaded mucoadhesive buccal films for enhanced bioavailability and improved therapeutic outcomes in migraine management, addressing limitations of oral formulations including poor bioavailability and gastrointestinal side effects.&#xa0;Mucoadhesive buccal films were prepared using solvent casting method with HPMC K15 and Gellan gum as polymers. A 3² factorial design was employed to optimize formulation variables, with HPMC K15 (5–6%) and Gellan gum (0.002–0.006% w/w) as independent variables. Films were characterized for physicochemical properties, mechanical strength, drug release kinetics, Ex vivo permeation, and stability. In vivo pharmacokinetic studies were conducted in Wistar rats comparing buccal film with oral suspension and marketed tablet.&#xa0;Nine formulations were prepared and characterized. F6 formulation (600&#xa0;mg HPMC K15, 0.040&#xa0;mg Gellan gum) was identified as optimal through desirability function optimization, demonstrating superior tensile strength (6.16 ± 0.28&#xa0;N/mm²), mucoadhesive strength (1.95 ± 0.09&#xa0;N), and controlled drug release (85.1% at 480&#xa0;min). In vivo studies revealed 53.1% enhanced bioavailability compared to marketed tablets (AUC₀₋₂₄: 3926.8 vs. 2564.2 ng·h/mL) with reduced clearance (2.33 vs. 3.53&#xa0;L/h/kg). Stability studies confirmed excellent shelf-life exceeding 24 months.&#xa0;The optimized buccal film offers significant clinical advantages including enhanced bioavailability, reduced dosing frequency, and improved patient compliance through bypassing first-pass metabolism. This innovative delivery system demonstrates strong potential for clinical translation, warranting human trials for migraine therapy optimization.</p> Graphical Abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Formulation and Development of Atogepant-loaded Mucoadhesive Buccal Films for Improved Bioavailability

  • 期刊论文

  • 发表日期：

    2026年2月16日

查看全文
  • Vaishnavi Vijay Shirsath,
  • Mahesh Hari Kolhe,
  • Payal Sopan Gawali,
  • Pratibha Sudhakar Bhalerao,
  • Rajashree Dadasaheb Ghogare,
  • Gaurao Subhash Damre

摘要

To develop and optimize atogepant-loaded mucoadhesive buccal films for enhanced bioavailability and improved therapeutic outcomes in migraine management, addressing limitations of oral formulations including poor bioavailability and gastrointestinal side effects. Mucoadhesive buccal films were prepared using solvent casting method with HPMC K15 and Gellan gum as polymers. A 3² factorial design was employed to optimize formulation variables, with HPMC K15 (5–6%) and Gellan gum (0.002–0.006% w/w) as independent variables. Films were characterized for physicochemical properties, mechanical strength, drug release kinetics, Ex vivo permeation, and stability. In vivo pharmacokinetic studies were conducted in Wistar rats comparing buccal film with oral suspension and marketed tablet. Nine formulations were prepared and characterized. F6 formulation (600 mg HPMC K15, 0.040 mg Gellan gum) was identified as optimal through desirability function optimization, demonstrating superior tensile strength (6.16 ± 0.28 N/mm²), mucoadhesive strength (1.95 ± 0.09 N), and controlled drug release (85.1% at 480 min). In vivo studies revealed 53.1% enhanced bioavailability compared to marketed tablets (AUC₀₋₂₄: 3926.8 vs. 2564.2 ng·h/mL) with reduced clearance (2.33 vs. 3.53 L/h/kg). Stability studies confirmed excellent shelf-life exceeding 24 months. The optimized buccal film offers significant clinical advantages including enhanced bioavailability, reduced dosing frequency, and improved patient compliance through bypassing first-pass metabolism. This innovative delivery system demonstrates strong potential for clinical translation, warranting human trials for migraine therapy optimization.

Graphical Abstract