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KMID : 0043320060290090795
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Archives of Pharmacal Research
2006 Volume.29 No. 9 p.795 ~ p.799
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Research on Thymopentin Loaded Oral N-Trimethyl Chitosan Nanoparticles
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Yuan Xiao-jia
Zhang Zhi-rong
Song Qing-guo
He Qin
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Abstract
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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 4oC or -20oC 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 givenTp5-TMC-NP (ig) was 2.59 time that of the group given Tp5 (ig).
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KEYWORD
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Thymopentin (Tp5), Oral drug delivery system, Nanoparticle, N-Trimethyl chitosan (TMC)
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