title: Development and evaluation of a novel phytosome-loaded chitosan microsphere system for curcumin delivery.
abstract: In this study, we developed a novel drug delivery system, curcumin-phytosome-loaded chitosan microspheres (Cur-PS-CMs) by combining polymer- and lipid-based delivery systems. Curcumin exhibits poor water-solubility and is rapidly eliminated from the body. We aimed to use our novel delivery system to improve the bioavailability and prolong the retention time of curcumin in the body. The Cur-PS-CMs were produced by encapsulating curcumin-phytosomes (Cur-PSs) in chitosan microspheres using ionotropic gelation. The final microsphere was spherical, with a mean particle size of 23.21 ± 6.72 μm and drug loading efficiency of 2.67 ± 0.23%. Differential scanning calorimetry and Fourier transform infrared spectroscopy demonstrated that the integrity of the phytosomes was preserved within the polymeric matrix of the microspheres. The in vitro release rate of curcumin from the Cur-PS-CMs was slower than that from curcumin-loaded chitosan microspheres (Cur-CMs) in pH 1.0, 4.0, 6.8, and 7.4. Pharmacokinetic studies in rats dosed with Cur-PS-CMs showed a 1.67- and a 1.07-fold increase in absorption of curcumin compared with Cur-PSs and Cur-CMs, respectively. The half-life of curcumin orally administration of Cur-PS-CMs (3.16 h) was longer than those of Cur-PSs (1.73 h) and Cur-CMs (2.34h). These results indicated that the new Cur-PS-CMs system combined the advantages of chitosan microspheres and phytosomes, which had better effects of promoting oral absorption and prolonging retention time of curcumin than single Cur-PSs or Cur-CMs. Therefore, the PS-CMs may be used as a sustained delivery system for lipophilic compounds with poor water-solubility and low oral bioavailability.
authors.affiliation: College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China. zhjf@swu.edu.cn
authors.forename: Jifen
authors.initials: J
authors.lastname: Zhang
authors.forename: Qin
authors.initials: Q
authors.lastname: Tang
authors.forename: Xiaoyu
authors.initials: X
authors.lastname: Xu
authors.forename: Na
authors.initials: N
authors.lastname: Li
mesh_terms: D000818:Animals; D002152:Calorimetry, Differential Scanning; D048271:Chitosan / Q000737:chemistry*; D003474:Curcumin / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D008863:Microspheres; D010316:Particle Size; D010743:Phospholipids / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D010743:Phospholipids; D048271:Chitosan; D003474:Curcumin