Archives of Pharmacal Research

The Pharmaceutical Society of Korea (대한약학회)
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Research on Thymopentin Loaded Oral N-Trimethyl Chitosan Nanoparticles

  • Yuan, Xiao-Jia (West China School of Pharmacy, Sichuan University) ;
  • Zhang, Zhi-Rong (West China School of Pharmacy, Sichuan University) ;
  • Song, Qing-Guo (West China School of Pharmacy, Sichuan University) ;
  • He, Qin (West China School of Pharmacy, Sichuan University)
  • Published : 2006.09.01
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Abstract

Peptides, although high efficacy and specificity in their physiological function, usually have low therapeutical activities due to their poor bioavailability when administrated orally. Nanoparticles have been regarded as a useful vector for targeted drug delivery system because they can protect drug from being degraded quickly and pass the gastrointestinal barriers. Here we described a novel oral N-trimethyl chitosan nanoparticles formulation containing thymopentin (Tp5-TMC-NP). N-trimethyl chitosan (TMC) was synthesized and then used to prepare Tp5-TMC-NP by ionotropic gelation. A three-factor, five-level CCD (Central Composite Design) design was used in the optimization procedure, with HPLC as the analyzing method. The resulting Tp5-TMC-NP had a regular spherical surface and a narrow particle size range with a mean diameter of 110.6 nm. The average entrapment efficiency was 78.8%. The lyophilized Tp5-TMC-NP formulation was stable in $4^{\circ}C\;or\;-20^{\circ}C$ after storage of 3 months without obvious changes in morphology, particle size, pH and entrapment ratio. The results of the flow cytometer determination showed that the ratio of $CD4^+/CD8^+$ of Wistar female rat given Tp5-TMC-NP (ig) was 2.59 time that of the group given Tp5 (ig).

Keywords

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