Formulation optimization and in vitro characterization of orally disintegrating films using a factorial design and mathematical modeling for drug release

Yeongbin Lee, Prakash Thapa, Seong Hoon Jeong, Mi Hee Woo, Du Hyung Choi

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

Even though experimental designs are becoming popular especially for conventional dosage forms, limited studies have been performed to optimize formulations of orally disintegrating films (ODFs). This study aimed to evaluate sildenafil citrate-loaded ODFs for a controlled release with hydroxypropyl methylcellulose as a film-forming polymer. A factorial design was utilized for optimization with three control factors: ethanol ratio, plasticizer ratio, and the type of plasticizer. Tensile strength, disintegration time, water contact angle, and thickness were chosen as responses. For optimization, water contact angle, disintegration time, and thickness were minimized, while the tensile strength was maximized. Based on the conditions, optimal formulations were achieved for each type of plasticizer. Evaluation of desirability indicated that the response values were close to the target. When these optimal formulations were validated, the optimal solutions and target values were similar with small biases. The formulations were characterized using scanning electron microscopy, differential scanning calorimetry, Fourier transform infrared spectroscopy, surface pH, in vitro dissolution, and drug release simulation with a mathematical modeling. After the drug was homogenously dispersed throughout the film, the crystalline form of the drug provided strong hydrogen bonds between the drug and the film components. Moreover, it showed a controlled drug release profiles that were well matched with simulated results. This study suggests that the optimized films may present a better alternative to conventional tablets for the treatment of male erectile dysfunction.

Original languageEnglish
Pages (from-to)166-177
Number of pages12
JournalChemical and Pharmaceutical Bulletin
Volume65
Issue number2
DOIs
StatePublished - 2017

Keywords

  • Controlled release
  • Factorial design
  • Hydroxypropyl methylcellulose
  • Mathematical modeling
  • Optimization
  • Orally disintegrating film

Fingerprint

Dive into the research topics of 'Formulation optimization and in vitro characterization of orally disintegrating films using a factorial design and mathematical modeling for drug release'. Together they form a unique fingerprint.

Cite this