OBJECTIVE To investigate the preparation of hydroxycamptothecin(HCPT)
nanoliposomes coated by chitosan hydrochloride(CS-HCl)and its
tissue distribution in mice.METHODS
HCPT nanoliposomes were prepared by the film dispersion method followed by
chitosan hydrochloride coating.The
liposomes were extruded to obtain the particle size below 100 nm.Liposomes contained HCPT and free HCPT were separated by a Sephadex-G50 chromatography.Ultraviolet spectrophotometry was used to determine the entrapment efficiency(EE %).The Zeta potential,average size and size distribution of the HCPT liposomes were also detected.HCPT injection,traditional HCPT liposomes,non-coated HCPT nanoliposomes and CS-HCl coated HCPT nanoliposomes were injected in tail vein at a dose of 5 mg·kg~(-1) of HCPT,respectively.The HPLC-FLD was utilized for the determination of HCPT concentration in mice tissue,including plasma,liver and spleen.RESULTS The average EE% of the CS-HCl coated HCPT nanoliposomes was(61.2±1.20)%.The average size was(91.9±8.78)nm with the Zeta potential of(55.1±1.04)mV(n=3).The area under the curve(AUC_(0～48))of plasma of CS-HCl coated HCPT nanoliposomes was 1.3-fold of that of the non-coated nanoliposomes while 4.7-fold of that of the traditional liposomes and 25.4-fold of that of the HCPT injection.The ratio of AUC_(plasma)/ AUC_(RES) of CS-HCl coated HCPT nanoliposomes was 1.4fold of that of the non-coated nanoliposomes while 8.7-fold of that of the traditional liposomes and 3.4-fold of that of the HCPT injection.CONCLUSION The results suggest that CS-HCl coated HCPT nanoliposomes have uniform sizes below nanometer degree and high positive Zeta potential.The AUC_(0～48) of plasma is increased significantly and a longer circulation time is obtained after being coated by CS-HCl.
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