Drug-Loaded Lipid-Core Micelles in Mucoadhesive Films as a Novel Dosage Form for Buccal Administration of Poorly Water-Soluble and Biological Drugs

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.

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or continue reading here: Chou, W.-H.; Galaz, A.; Jara, M.O.; Gamboa, A.; Morales, J.O. Drug-Loaded Lipid-Core Micelles in Mucoadhesive Films as a Novel Dosage Form for Buccal Administration of Poorly Water-Soluble and Biological Drugs. Pharmaceutics 2020, 12, 1168.

Keywords: lipid-core micelles; rhodamine 123; poorly water-soluble drugs; human insulin; biological drugs; mechanical properties; mucoadhesive films; buccal administration; in vitro release; ex vivo permeation, Gelucire 44/14®; Tween 20®, Span 80®, . Ethanol, hydrochloric acid, glycerol 85%, Hydroxypropyl methylcellulose (HPMC) K100 and ethylcelloluse NF (EC) Standard 10;Triethyl citrate (TEC) Vivaspin® 6