Study of morphological changes of poly(2-oxazoline) micelles induced by high loading of drugs
10.16781/j.0258-879x.2017.02.0155
- Author:
Min XU
1
Author Information
1. Department of Pharmaceutical Science, School of Pharmacy, Second Military Medical University
- Publication Type:Journal Article
- Keywords:
Paclitaxel;
Poly (2-oxazoline);
Spherical micelle;
Worm-like micelle
- From:
Academic Journal of Second Military Medical University
2017;38(2):155-160
- CountryChina
- Language:Chinese
-
Abstract:
Objective To prepare the paclitaxel-loaded poly(2-oxazolyl) nano-micelles and to investigate the morphological changes of nano-micelles after changing drug dosage, so as to establish a novel block copolymer micelles delivery system with high loading capacity. Methods The paclitaxel-loaded poly(2-oxazolyl) nano-micelles were prepared using filming-rehydration method. The physical and chemical properties of the prepared nano-micelles, including particle size, encapsulation efficiency and drug loading efficiency, were characterized. The in vitro release characteristics of the prepared nano-micelles were investigated by membrane dialysis method, and the cytotoxicity was determined by CCK-8 method. Results The morphology of micelles gradually extended from spherical to worm-like when the mass ratio of paclitaxel and poly(2-oxazoline) increased from 80: 100 to 110: 100. The particle size, encapsulation efficiency and drug loading efficiency of spherical micelles were (43. 17 + 0. 95) nm, (88. 81 + 2. 93) % and (40. 49 + 2. 03)%, respectively, while those of worm-like micelles were (107. 83 + 1. 51) nm, (77. 08 + 0. 97)% and (40. 34 + 0. 51) %, respectively. The 24 h cumulative release rates of spherical micelles and worm-like micelles in PBS were (76. 58 + 3. 07)% and (77. 66 + 1. 00)%, respectively; meanwhile, those in PBS with 2% bovine serum albumin were up to (100. 31 + 1. 80)% and (99. 73 + 2. 56)%, respectively. The IC50 values of sphere micelles and worm-like micelles on human lung adenocarcinoma cell line A549 were 0. 336 μg/mL and 0. 342 μg/mL, respectively. Conclusion Paclitaxel-loaded spherical micelles and worm-like micelles with high loading capacity have been successfully prepared. In vitro cytotoxicity results have found that both micelles have anti-tumor activities.
