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Physicochemical properties and pharmacokinetics of hydroxypropyl-β-cyclodextrin liposomes containing l-asparaginase / 第二军医大学学报
Academic Journal of Second Military Medical University ; (12): 700-703, 2019.
Article in Chinese | WPRIM | ID: wpr-837887
ABSTRACT
Objective To investigate the physicochemical properties and pharmacokinetics of L-asparaginase loaded hydroxypropyl-β-cyclodextrin liposome (AHL) in rats. Methods AHL was prepared by reverse evaporation method, and the entrapment rate, particle size, zeta potential and morphology of AHL were observed. Twelve SD rats were randomly divided into two groups. One group was injected with AHL, and the other group was injected with L-asparaginase (L-ASN). The blood samples were taken from infraorbital venous plexus, and the activity of L-ASN in the samples were determined and the activity-time curve was plotted. Main pharmacokinetic parameters were calculated by software DAS2.1.1. Results The average entrapment efficiency of AHL was (53.53±0.58)%, with an average particle size of (388.99±2.02) nm and an average zeta potential of (-8.56±0.75) mV. The pharmacokinetic parameters for AHL and L-ASN were 0-48 h area under curve (198.79±9.15) U/(mL • h), (57.78±2.90) U/(mL • h); 0-48 h mean resident time (4.61±0.09) h, (2.09±0.05) h; peak concentration (32.32±1.33) U/mL, (26.82±1.38) U/mL; and time to peak (1.08±0.20) h, (0.10±0.04) h, respectively. The relative bioavailability of AHL was 344.05%. Conclusion AHL can improve the pharmacokinetics and enhance the bioavailability of L-ASN.

Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Academic Journal of Second Military Medical University Year: 2019 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Academic Journal of Second Military Medical University Year: 2019 Type: Article