Formulation and evaluation the bioadhesive properties of drug delivery system based on PEGylated mucin matrices

摘要

Objective:To formulate and evaluate the application of PEGylated mucin in oral bioadhesive drug (OBD) delivery system. Methods:The bioadhesive strength of different formulation ratios of polyethylene glycol (PEG) and mucin was evaluated by tensiometry. Co polymer matrices containing mucin and PEG (PEGylated mucin) in the following ratios of 1:1 (A), 2:1 (B), 1:2 (C), 0:1 (D) and 1:0 (E) were prepared by co-precipitation. Microparticles were prepared from the matrices using a size reduction technique. Five different samples were prepared using direct mixtures in the appropriate solvenfs having mucin and PEG ratios of 1:1, 2:1 , 1:2, 0:1 , 1:0 and labeled as (A-E). The matrices were evaluated for their flow properties and the in vitro bioadhesion characteristics of the samples were examined. Results:The range of flow rates of the matrices was 1.35-2.23 g/sec. The angle of repose was in the range of 37.3-39.9 degree. The bulk and tapped densities were within the ranges of 0.41-0.49. The Hausner’s quotient (HQ) were 1.12, 1.24, 1.14, 1.25 and 1.2 for matrix batches A-E respectively, The bioadhesive strength of polymer matrices appeared to be directly related to amount of mucin. The order of bioadhesive strength is 2:1>1:1>1:0>1:2>0:1 of PEG:mucin in both simulated intestine fluid (SIF) and simulated gastrointestinal fluid (SGF). The physical properties of the micrometrics properties of the matrices were within the accepted values. Conclusions: OBD preparation containing PEGylated mucin can be prepared by direct compression and be used in drug delivery to the oral cavity.