Sterilization stability of vesicular phospholipid gels loaded with cytarabine for brain implant

International Journal of Pharmaceutics
Na QiYu Zhang

Abstract

The aim of this study was to investigate the sterilization stability of cytarabine (Ara-C) loaded vesicular phospholipid gels (VPGs). VPGs were prepared by high pressure homogenization method intended for the treatment of glioblastoma multiforme (GBM) in brain as injectable implant. The particle size of VPGs after redispersion was 119.6 ± 66.24 nm, and entrapment efficiency (EE) was 32.6 ± 2.1%. Drug release in vitro from VPGs sustained for 80 h with 48.1% initial release within 1h, and rheological studies demonstrated a gel-like behavior. Comparatively, after autoclaved sterilization, increased particle size and EE were obtained as 165.6 ± 71.89 nm and 62.6 ± 2.3%, respectively. Additionally, characteristics of drug release were significantly altered with obviously prolonged release time to 450 h and remarkable reduced initial release to 24.7%. Also, the viscoelasticity was reinforced with clearly decreased fluidity. This result could be explained by the fusion of small vesicles witnessed in TEM observation, which resulted in percentages change of vesicle groups with different size. However, reduced Ara-C and increased lysophosphatidylcholine (LPC) were observed. Among the stabilizers, addition of sodium sulfite showed best ef...Continue Reading

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Citations

Jun 25, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Ammar ArsiwalaVandana Patravale
Nov 5, 2016·Journal of Controlled Release : Official Journal of the Controlled Release Society·C BastiancichF Danhier
Dec 6, 2019·Frontiers in Bioengineering and Biotechnology·Andrei BelousovVadim Kumeiko
Feb 7, 2021·International Journal of Pharmaceutics·Kouka Luc DelmaGéraldine Piel

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