Abstract
The aim of the study was to develop a novel buccal dosage form to transport rhodamine 123 and human insulin as models for poorly water-soluble and biological drugs, using lipid-core micelles (LCMs)-loaded mucoadhesive films. LCMs were synthesized by a low-energy hot emulsification process, yielding spherically shaped, small-sized, monodispersed and negatively charged carriers with high entrapment efficiency. In vitro release studies demonstrated a higher release of insulin rather than rhodamine from LCMs in simulated physiological conditions, due to an initial burst release effect; however, both release profiles are mainly explained by a diffusion mechanism. Furthermore, LCMs-loaded mucoadhesive films were manufactured and preserved with similar mechanical properties and optimal mucoadhesive behavior compared to nonloaded films. Ex vivo permeation experiments using excised porcine buccal epithelium reveal that both rhodamine and insulin-loaded LCM films elicited a significantly enhanced permeation effect compared to LCMs in suspension and free drugs in solution as controls. Hence, LCMs-loaded mucoadhesive films are suitable as buccal dosage form for the transport and delivery of rhodamine 123 and insulin, as models for poorly water-soluble and biological drugs, respectively.
Highlights
Among enteral routes for drug administration, the oral is the most used, comfortable and tolerated by patients
scanning-transmission electron microscope (STEM) micrographs confirmed that rhodamine 123 (Rho)-loaded lipid-core micelles (LCMs) show a bigger particle size rather than Ins-loaded particles (Figure S2A,B, respectively)
In terms of internalization rate, the small-sized nanoparticles are transported through the buccal epithelium by two different mechanisms: the intracellular or transcellular route, where the system can pass across the cells; and the intercellular or paracellular pathway, where the particle may pass through the spaces between the epithelial cells
Summary
Among enteral routes for drug administration, the oral is the most used, comfortable and tolerated by patients. Several disadvantages are reported, including fluctuation of pH values between gastric and intestinal segments, presence of lytic enzymes, epithelial barriers surrounding the intestinal absorptive lumen, gastric emptying time and intestinal motility, presence of food, presystemic first pass metabolism and elimination, and the administration of irritating or unstable to gastric conditions drugs [1]. These issues make it difficult for the administration of poorly water-soluble, as well as biological drugs, and lead to nonpredictable pharmacokinetic and pharmacodynamic profiles [2]. Considering the mentioned advantages, there are several candidates using films to deliver drugs that are currently facing various stages of clinical trials, with promising results that may lead to marketed products in the near future [15]
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