Baicalin lipid nanocapsules for treatment of glioma: characterization, mechanistic cytotoxicity, and pharmacokinetic evaluation.

OBJECTIVES: Baicalin is a promising anticancer nutraceutical compound, but its application is hindered by its low water solubility and bioavailability, which can be remedied by its encapsulation in nanoparticles. METHODS: Lipid nanocapsules (LNCs) were developed to enhance baicalin delivery via intravenous and intranasal routes, and potentiate its therapeutic activity in treatment of glioma. RESULTS: LNCs displayed a particle size of 17.76 nm and sustained release of 74.36% after 24 h. The IC50 of baicalin LNCs (13 ± 5 µg/ml) was 60 times lower than free baicalin (780 ± 107 µg/ml) on human glioblastoma multiform cell line U87, with adequate cellular uptake as delineated by confocal laser microscopy. Both baicalin and LNCs induced cell cycle arrest at S and G2/M phases, with significant up-regulation in P21 gene, and decline in Nrf-2, HO-1 and VEGF gene expression. LNCs increased baicalin's bioavailability, either after intravenous (AUC0-24 h 10.94 ± 0.28 vs 3.53 ± 0.09 µg/ml*h), or intranasal administration (AUC0-24 h 6.26 ± 0.11 vs 3.17 ± 0.04 µg/ml*h). They also bypassed the blood brain barrier and achieved significantly higher brain delivery compared to free baicalin (drug targeting efficiency 160.73% vs 52.9%). CONCLUSION: Baicalin LNCs is a promising treatment modality for glioma, when administered through intravenous or intranasal routes.

Conventional and hybrid nanoparticulate systems for the treatment of hepatocellular carcinoma: An updated review.

Hepatocellular carcinoma (HCC) is considered a serious malignancy which affects a large number of people worldwide. Despite the presence of some diagnostic techniques for HCC, the fact that its symptoms somehow overlap with other diseases causes it to be diagnosed at a late stage, hence negatively affecting the prognosis of the disease. The currently available treatment strategies have many shortcomings such as high cost, induction of serious side effects as well as multiple drug resistance, hence resulting in therapeutic failure. Accordingly, nanoformulations have been developed in order to overcome the clinical challenges, enhance the therapeutic efficacy, and elicit chemotherapy tailor-ability. Hybrid nanoparticulate carriers in particular, which are composed of two or more drug vehicles with different physicochemical characteristics combined together in one system, have been recently reported to advance nanotechnology-based therapies. Therefore, this review sheds the light on HCC, and the role of nanotechnology and hybrid nanoparticulate carriers as well as the latest developments in the use of conventional nanoparticles in combating this disease.