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

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 extractloaded 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 analysisdifferential 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.

Enhanced In Situ Availability of Aphanizomenon Flos-Aquae Constituents Entrapped in Buccal Films for the Treatment of Oxidative Stress-Related Oral Diseases: Biomechanical Characterization and In Vitro/Ex Vivo Evaluation

“…To mask the bad taste of algae and make the films palatable, Saccharin was preferred as a sweetening agent, due to its stability in acid environments and Tangerine essential oil, was used as a flavoring agent. The quantitative composition of films has been selected on the basis of our previous experiences [56].…”

Gellan Gum-Based Hydrogel for the Transdermal Delivery of Nebivolol: Optimization and Evaluation

“…The nebivolol release data were fitted into established mathematical release kinetics models and analyzed to predict the drug release pattern of formulated gels. The correlation coefficient (r 2 ) as well release mechanisms were determined using following equations [29,30]; Zero-order model Q = Q 0 + kt First-order model Q = Q 0 × e kt Higuchi model Q = k × t 0.5 Korsmeyer–Peppas model Q = k × t n Weibull model Q = 1 − exp[−( t ) b / a ] where Q represents the quantity of drug released in time t , Q 0 represents the value of Q at zero time, k represents the rate constant, n represents the diffusional exponent, a represents the time constant, and b represents the shape parameter. The correlation coefficient ( r 2 ) and the order of release pattern were calculated in each case.…”

Antibacterial PEGylated Solid Lipid Microparticles for Cosmeceutical Purpose: Formulation, Characterization, and Efficacy Evaluation

“…The permeation of RSV throughout the epidermis of porcine ear skin was evaluated, using Franz-type diffusion cell (Permeagear, flat flange joint, 9 mm orifice diameter, 16 mL acceptor volume, SES GmbH-Analysesysteme, Bechenheim, Germany), used as a two-compartment open model [22]. The ears' epidermis was obtained by dipping it for approximately 1 min in a warm (60 • C) saline solution; therefore, the epidermis was heat-detached from the underlying tissues [23], obtaining 2.16 ± 0.20 mm thickness epithelia, which was measured using a digital micrometer (Vogel, Germany).…”