High drug loading glaucocalyxin a nanosuspensions: preparation and in vitro evaluation
- Author:
Yan-Hong LI
1
Author Information
- Publication Type:Journal Article
- Keywords: Drug loading; Glaucocalyxin A; MTT assay; Nanosuspension
- From: Chinese Pharmaceutical Journal 2015;50(7):606-612
- CountryChina
- Language:Chinese
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Abstract:
OBJECTIVE: To prepare high drug loading glaucocalyxin A (GLA) nanosuspensions and study their properties in vitro. METHODS: Using solvent precipitation combined with high pressure homogenization method, the GLA nanosuspensions were successfully prepared with PLGA-PEG-PLGA block copolymer being a stabilizer. The particle size of the resultant nanosuspensions was determined by dynamic light scattering (DLS), their morphology was observed by transmission electron microscopy (TEM), the crystalline state of GLA in the nanosuspensions was examined by differential scanning calorimetry (DSC), and the in vitro release of GLA nanosuspensions was investigated using dialysis method. The in vitro anticancer cytotoxic activity of free GLA solution and GLA nanosuspensions against a gastric cancer cell line (BGC cells) and a hepatic cancer cell line (HepG-2 cells) were performed using MTT assay. RESULTS: GLA Nanosuspensions showed a mean particle size of (222.6±4.32) nm, a polydispersity index (PDI) of (0.237±0.016) and a Zeta potential of (-11.5±0.954) mV. The average entrapment efficiency was (69.11±3.02)% and the average drug loading was (40.67±2.45)%. The particles in the nanosuspensions were spherical with smooth surface and u-nilorm size distribution, and displayed sustained release in vitro. GLA nanosuspensions showed significant higher cytotoxicity than free GLA against BGC cells (IC
50 value 0.784 μg·ml-1 vs. 1.658 μg·mL-1) and HepG2 cells (IC50 value 12.4 μg·mL-1 vs. 6.44 μg·mL-1). CONCLUSION: High drug loading GLA nanosuspensions are successfully prepared and well characterized in vitro. The resultant nanoparticles can efficiently enhance the antitumor activity of GLA and thus can be used as a suitable dosage form in this respect.
