Design and evaluation of an innovative floating and bioadhesive multiparticulate drug delivery system based on hollow structure

• Published in: International journal of pharmaceutics 2016-04, Vol.503 (1-2), p.41-55
• Main Authors: Zhang, Chungang, Tang, Jingya, Liu, Dechun, Li, Xuetao, Cheng, Lan, Tang, Xing
• Format: Article
• Language: English
• Subjects: Acrylic Resins - chemistry; Adhesiveness; Animals; Bioadhesive particulate; Cellulose - analogs & derivatives; Cellulose - chemistry; Chemistry, Pharmaceutical; Delayed-Action Preparations - chemistry; Delayed-Action Preparations - pharmacokinetics; Drug Delivery Systems; Drug Liberation; Hollow spherical shell; In Vitro Techniques; Male; Novel coating materials; Ofloxacin - administration & dosage; Ofloxacin - blood; Ofloxacin - chemistry; Ofloxacin - pharmacokinetics; Pharmacokinetic; Polymethacrylic Acids - chemistry; Rabbits; Rats, Sprague-Dawley; Stearic Acids - chemistry; Stomach - chemistry; Stomach - metabolism; X-ray image
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2016.02.045

[Display omitted] In this study a gastric-retentive delivery system was prepared by a novel method which is reported here for the first time. An innovative floating and bioadhesive drug delivery system with a hollow structure was designed and prepared. The floating and bioadhesive drug delivery system was composed of a hollow spherical shell, a waterproof layer (Stearic acid), a drug layer (Ofloxacin), a release retarding film (the novel blended coating materials) and a bioadhesive layer (Carbomer 934P) prepared by using a liquid multi-layering process. A novel blended coating material was designed and investigated to solve the problem of the initial burst release of the formulation and the release mechanism of the novel material was analyzed in this study. The optimized formulation provided the sustained release characteristic and was able to float for 24h. The SEM cross-section images showed that the particulates were hollow with a spherical shell. X-ray images and pharmacokinetic studies (Frel=124.1±28.9%) in vivo showed that the gastric-retentive delivery system can be retained in the stomach for more than 6h. The floating and bioadhesive particulate drug delivery system based on a hollow structure with a dual function presented here is a viable alternative to other for gastroretentive drug delivery system.