Assembled modules technology for site-specific prolonged delivery of norfloxacin.
The aim of this research was to design and study norfloxacin (NFX) release in floating conditions from compressed hydrophilic matrices of hydroxypropylmethylcellulose (HPMC) or poly(ethylene oxide) (PEO). Module assembling technology for drug delivery system manufacturing was used. Two differently cylindrical base curved matrix/modules, identified as female and male, were assembled in void configuration by friction interlocking their concave bases obtaining a floating release system. Drug release and floatation behavior of this assembly was investigated. Due to the higher surface area exposed to the release medium, faster release was observed for individual modules compared to their assembled configuration, independently on the polymer used and concentration. The release curves analyzed using the Korsmeyer exponential equation and Peppas & Sahlin binomial equation showed that the drug release was controlled both by drug diffusion and polymer relaxation or erosion mechanisms. However, convective transport was predominant with PEO and at low content of polymers. NFX release from PEO polymeric matrix was more erosion dependent than HPMC. The assembled systems were able to float in vitro for up to 240min, indicating that this drug delivery system of norfloxacin could provide gastro-retentive site-specific release for increasing norfloxacin bioavailability.
Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Quality Control Laboratory, J/K 207, 88040-900 Florianópolis-SC, Brazil.
Paulo Renato
PR
Oliveira
Larissa Sakis
LS
Bernardi
Orazio Luca
OL
Strusi
Salvatore
S
Mercuri
Marcos A
MA
Segatto Silva
Paolo
P
Colombo
Fabio
F
Sonvico
D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D007785:Lactose / Q000031:analogs & derivatives / Q000737:chemistry; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D009643:Norfloxacin / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers; D012995:Solubility
D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D011108:Polymers; C509290:hydroxypropylmethylcellulose-lactose matrix; D011092:Polyethylene Glycols; D008747:Methylcellulose; D007785:Lactose; D009643:Norfloxacin