Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

Abstract

A pharmaceutical vehicle based on lyophilized liposomes is proposed for the buccal administration of drugs aimed at systemic delivery through the sublingual mucosa. Liposomes made of egg phosphatidylcholine and cholesterol (7/3 molar ratio) were prepared and lyophilized in the presence of different additive mixtures with mucoadhesive and taste-masking properties. Palatability was assayed on healthy volunteers. The lyophilization cycle was optimized, and the lyophilized product was compressed to obtain round and capsule-shaped tables that were evaluated in healthy volunteers. Tablets were also assayed regarding weight and thickness uniformities, swelling index and liposome release. The results proved that lyophilized liposomes in unidirectional round tablets have palatability, small size, comfortability and buccal retention adequate for sublingual administration. In contact with water fluids, the tablets swelled, and rehydrated liposomes were released at a slower rate than permeation efficiency determined using a biomimetic membrane. Permeability efficiency values of 0.72 ± 0.34 µg/cm2/min and 4.18 ± 0.95 µg/cm2/min were obtained for the liposomes with and without additives, respectively. Altogether, the results point to the vehicle proposed as a liposomal formulation suitable for systemic drug delivery through the sublingual mucosa.

Formulation and characterization of lamotrigine nasal insert targeted brain for enhanced epilepsy treatment

“…This result is in agreement with previously reported by De Jesús Valle and Zarzuelo Castañeda et al. who found that the drug release could be explained by the difference in molecular packing and deformability associated with the edge activator used (De Jesús Valle et al., 2022 ). The presence of Tween 80 at high concentration could improve the drug’s solubility by raising nano-spanlastic bilayer fluidity, resulting in an improvement of membrane permeability and hence, forward improving the release rate (Al-Mahallawi et al., 2014 ).…”

The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets

“…The acceptor compartment was filled with 20 mL of phosphate-buffered saline (PBS) at pH 7.4 and 37 ± 0.5 • C with 250 rpm stirring (Figure S4, Supplementary Materials). These buffer solutions represent the physiological conditions under which the drug is released and permeates the membrane (n = 3) [17,19,55]. At each hour interval, 1 mL of samples were collected from the acceptor compartment and replaced with fresh PBS.…”

“…Compared to oral administration, sublingual administration can increase drug absorption by 3-10 times, with only hypodermic shots exceeding it [15]. However, several variables may restrict drug absorption via the sublingual mucosa, including a small area for absorption, tongue movement causing shearing forces, short residence duration due to rapid turnover of saliva, involuntary swallowing of fluids greater than 200 µL, and/or involuntary swallowing of the dosage forms [10,13,17,18].…”

“…A significant factor is the length of time the formulation lasts at the absorption site (sublingual). Extending the duration of the drug's residence time with mucoadhesive compounds that can create molecular connections with mucosal constituents, thus immobilizing dosage forms to create a longer time for drug absorption, can overcome these difficulties [12,13,[17][18][19]. Owing to its low penetration resistance and negative charge, mucin significantly promotes macromolecular drug penetration into the oral mucosa via mucoadhesion [10,20].…”