A Novel, Potential Microflora-Activated Carrier for a Colon-Specific Drug Delivery System and Its Characteristics

Abstract

A novel polyelectrolyte complex (PEC) formed by sodium cellulose sulfate (NaCS) and chitosan was prepared as a potential material for a colon-specific drug delivery system. The characteristics of NaCS-chitosan film were measured by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), in vitro degradation, and in vitro drug release experiments. SEM data indicated that the NaCS-chitosan film had relatively homogeneous and smooth morphology at the initial state and deformed after being immersed in simulated colonic fluid (SCF). FTIR data indicated that the NH 3 + of the chitosan had reacted with the SO 4of the NaCS. In vitro degradation behavior revealed that NaCS-chitosan could be degraded by colon microflora and be hydrolyzed in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). It is found in the experiment of in vitro drug release that the capsules formed by the NaCS-chitosan complex could release about 80% of the drug loaded in the SCF during 4 h. All these results indicated that the NaCS-chitosan complex shows excellent behavior for colon specificity and could be a potential material for a colon-specific drug delivery system.

Microparticle formation of sodium cellulose sulfate using supercritical fluid assisted atomization introduced by hydrodynamic cavitation mixer

“…Due to its favorable biological properties, including nontoxicity, biocompatibility, biodegradation, hydrophilicity, and good film-forming performance [4,[21][22][23][24][25], NaCS has been received much attention and widely used in many fields, especially in pharmaceutical and biomedical engineering. In particular, NaCS was frequently used as a polyanion encapsulation matrix to immobilize enzymes, microorganisms and animal/plant cells or as a swellable hydrophilic matrix applied in the drug delivery system which forms a gel layer when exposed to aqueous media.…”

Novel double-walled microspheres based on chitosan, sodium cellulose sulfate and sodium tripolyphosphate: Preparation, characterization and in vitro release study

“…4, under the weak acidic condition of pH 6.4, chitosan/NaCS/TPP microcapsules showed a regular drug release behavior with a trend of slowly increasing, and the BSA was released sustainably and almost completely during 10 h. However, the control microcapsules had a burst drug release (more than 63.1±0.7%) effect during the first hour and the drug released irregularly during the 10 h study, which was not suitable for use as a sustained drug carrier according to the Ritger-Peppas model [13] (less than 60.0%). Since PEC formed with chitosan and NaCS was a hydrophilic and swellable system, and can be degraded by the enzyme in SCF [3,5], the drug release would be a combination of diffusion and macromolecular relaxation processes followed by the erosion procedures of the system [14]. The chitosan/NaCS/TPP microcapsules prepared here could be used as a protein carrier in a further appropriate formulation for controllable release of drug in colon.…”

“…Sodium cellulose sulfate (NaCS) as a novel hydrophilic cellulose derivative is a polyanionic polymer, which has favorable biological properties as a drug carrier material, such as hydrosolubility, nontoxicity, biodegradability and good film-forming ability [2]. We have found that the polyelectrolyte complex (PEC) composed of chitosan and NaCS has the potential behaviors in the controlled release of drugs, and was used for preparing the colon-specific drug delivery capsules [3], the multilayer microcapsules [4], and the complex films [5]. However, chitosan/NaCS microcapsules tend to collapse, since NaCS with high molecular weight only binds on the surface of chitosan droplets [6].…”

Chitosan-based polyelectrolyte complexes as pharmaceutical excipients

“…This complex was used as an excipient to prepare a controlled release gastroretentive system of "tablets-in-capsule" based on the combination of different mini-tablets (Gómez-Burgaz et al, 2008). Capsules of chitosan-sodium cellulose sulfate showed a potential use for delivery of 5-aminosalicylic acid specifically to the colon (Wang et al, 2009). The swelling of the system and the drug release rate were dependent on chitosan molecular weight and environment pH.…”