Lipase-catalyzed construction of glucose-modified brain targeting liposomes with paclitaxel and research on its optimized preparation process
10.7501/j.issn.0253-2670.2016.11.010
- Author:
Hua NIE
1
Author Information
1. Medical College of Jiaying University
- Publication Type:Journal Article
- Keywords:
Biocatalysis;
Brain targeting;
Cholesterol derivatives;
Film dispersion method;
Glucose transporter;
Lipase-catalyzed;
Liposomes;
Nonaqueous media;
Paclitaxel
- From:
Chinese Traditional and Herbal Drugs
2016;47(11):1867-1874
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To synthesize brain targeting lipid material [(5-cholesten-3β-yl) (D-glucopyranose-6) sebacate, CHS-SE-GLU] by lipase as catalyst in nonaqueous phase and optimize the preparation technology and formulation of CHS-SE-GLU-modified liposomes. Methods: CHS-SE-GLU was synthesized from CHS-SE prepared in previous work and D-glucose using lipase Novozym 435 in acetone. The structure characterization of the products is obtained by MS and NMR. The CHS-SE-GLU-modified paclitaxel-loaded brain targeting liposomes (GLU-PTX-LP) were prepared by thin film dispersion method. Single factor evaluation was applied to optimizing its preparation technology and formulation. Results: CHS-SE-GLU was confirmed by MS and NMR as target products. The optimal formulation and technology of GLU-PTX-LP were as follows: HSPC as membrane material, the ratio of HSPC to PTX was 0.1, the ratio of CHS to HSPC was 0.5, the dosage of DSPG-Na was 2.5%, hydration time was 0.5 h, and hydration temperature was 50 ℃. Three batches of samples were prepared by optimum preparation process and the average encapsulation efficiency was (93.62±1.34)%, (93.75±1.77)%, (92.04±1.50)%; The average particle size was (89.56±1.35), (92.05±3.42), (104.91±3.71) nm; And the average Zeta potential was (-25.21±0.27), (-26.43±0.44), (-25.17±0.65) mV, respectively. Conclusion: Lipase-catalyzed method for the preparation of brain targeting lipid material is simple and environment friendly with high yield. The entrapment efficiency, particle size, and stability of brain targeting drug-loading liposomes modified by CHS-SE-GLU all meet the requirement, which shows good application prospect.
