a. School of Pharmacy；b. School of Pharmaceutical Engineering，1. Shenyang Pharmaceutical University，Shenyang 110016，China; 2. School of Pharmacy，Fudan University，Shanghai 200032，China
OBJECTIVE To prepare borneol modified azidothymidine palmitate liposomes,and evaluate the effect of borneol on blood-brain barrier penetration of azidothymidine palmitate(AZTP) in mice after i.v.administration.METHODS Soybean phosphatidylcholine(SPC)-cholesterol(CH)-borneol(B)(80:10:10,mol/mol/mol)(10%B-AZTPL) and SPC/CH/B(80:20:0) liposomes(AZTP-CL) containing AZTP were prepared by ethanol injection method followed by ultrasonic-dispersion.Then,15.85 mg·kg-1 AZT solution and 30.0 mg·kg-1 AZTP(at equimolar doses of AZT) in two liposomes were given to KM mice via the tail vein,respectively.The distributions of AZT in plasma and various organs were determined by reversed phase HPLC.AZT guantity contained in different tissues was calculated.RESULTS The mean diameter of two liposomes were both less than 120 nm and encapsulation efficiency more than 96%,Zeta potential about-28.2 mV.Compared with AZT control solution,brain absolute uptake of AZT was increased from 1.43 times of AZTP-CL to 1.96 times(P<0.05) of 10%B-AZTPL.The brain direct transport value of the 10% borneol modified preparation was 3.73 times(P<0.01) as that of common liposomes.The lung and renal uptakes of AZT in 10% borneol modified preparation were also significantly increased by 1.69 times and decreased by 0.7 times(P<0.05) compared with AZT solution,respectively.CONCLUSION 10%(mol/mol) borneol promoted the transient opening of blood-brain barrier and transportation of AZTP into brain,significantly increased AZTP permeability into brain tissues.10% borneol modified AZTP liposomes is expected to become a convenient and easy method for HIV encephalopathy therapy.
WU Hong-ing;WNG Sho-ning;Shi Li;DENG Yi-hui.
Effects of Borneol on the Distribution of Azidothymidine Palmitate Liposomes in Mice [J]. Chinese Pharmaceutical Journal, 2009, 44(08): 590-593
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