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

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 mu g/cm(2)/min and 4.18 +/- 0.95 mu g/cm(2)/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.

Automated summary

A pharmaceutical vehicle based on lyophilized liposomes was developed for the buccal administration of drugs aimed at systemic delivery through the sublingual mucosa. The optimized formulation of lyophilized liposomes in unidirectional round tablets showed palatability, small size, comfortability, and buccal retention suitable for sublingual administration. The liposome release rate was slower compared to the permeation efficiency determined using a biomimetic membrane. The proposed liposomal formulation is suitable for systemic drug delivery through the sublingual mucosa.