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AAPS PharmSciTech

, 20:18 | Cite as

Mucoadhesive Polymeric Films to Enhance Barbaloin Penetration Into Buccal Mucosa: a Novel Approach to Chemoprevention

  • Giulia Di Prima
  • Alice Conigliaro
  • Viviana De CaroEmail author
Research Article
  • 93 Downloads

Abstract

Nowadays, chemoprevention by administering natural supplements is considered an attractive strategy to reverse, suppress, or prevent the evolution of premalignant oral lesions. In particular, Barbaloin exhibits anti-proliferative, anti-inflammatory, and anti-cancer properties, and it results useful in multi-therapy with classic chemotherapeutics. Therefore, in this work, mucoadhesive buccal films, as locoregional drug delivery system able to provide a targeted and efficient therapeutic delivery of Barbaloin, are proposed. Thus, Aloin extract-loaded Eudragit® RL100 or Eudragit® RS100-based buccal films were designed in order to obtain an easily self-administrable formulation capable of promoting Barbaloin penetration into buccal mucosa and assuring high patient compliance. Large amounts of extract (44%) were loaded into the polymer matrix and six formulations were prepared varying polymers and plasticizers ratios. For all formulations, physical form (thermogravimetric analysis-differential scanning calorimetry, TGA-DSC), swelling degree, mucoadhesiveness, drug release, and ability to promote drug penetration in mucosa have been investigated. After a sequential selection process, Eudragit RS 100-based film, with low PVP and high plasticizers amounts, emerged as the most promising. It results appropriately flexible, uniform in terms of weight, thickness and drug content, as well as characterized by suitable surface pH, good mucoadhesiveness, and low swelling degree. It displays a Higuchian drug release behavior up to 89% of Barbaloin released, thus demonstrating that diffusion through the matrix is the main release mechanism. Remarkable penetration enhancer properties of film were demonstrated by evidence of Barbaloin accumulation into buccal mucosa up to 10-fold higher than those obtained following administration of Aloin solution.

KEY WORDS

Barbaloin buccal film chemoprevention mucoadhesion ex vivo permeation 

Notes

Acknowledgments

Authors are thankful to Dr. Francesco Carfì Pavia and ATeN Center of Palermo for technical support for DSC analyses.

Funding

Associazione Italiana per la Ricerca sul Cancro (Italian Association for Cancer Research) MFAG 2017 Id.19982.

Compliance with Ethical Standards

Conflict of Interest

The authors declare that they have no conflict of interest.

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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  1. 1.Istituto di Biofisica, Consiglio Nazionale delle RicerchePalermoItaly
  2. 2.Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF)Università degli Studi di PalermoPalermoItaly
  3. 3.Dipartimento di Biopatologia e Biotecnologie Mediche (DIBIMED)Università degli Studi di PalermoPalermoItaly

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