Nanotechnology Based Approach for Hepatocellular Carcinoma Targeting.

Hepatocellular carcinoma (HCC) is the primary liver cancer that has shown a high incidence and mortality rate worldwide among several types of cancers. A large variety of chemotherapeutic agents employed for the treatment have a limited success rate owing to their limited site-specific drug targeting ability. Thus, there is a demand to develop novel approaches for the treatment of HCC. With advancements in nanotechnology-based drug delivery approaches, the challenges of conventional chemotherapy have been continuously decreasing. Nanomedicines constituted of lipidic and polymeric composites provide a better platform for delivering and opening new pathways for HCC treatment. A score of nanocarriers such as surface-engineered liposomes, nanoparticles, nanotubes, micelles, quantum dots, etc., has been investigated in the treatment of HCC. These nanocarriers are considered to be highly effective clinically for delivering chemotherapeutic drugs with high site-specificity ability and therapeutic efficiency. The present review highlights the current focus on the application of nanocarrier systems using various ligand-based receptor-specific targeting strategies for the treatment and management of HCC. Moreover, the article has also included information on the current clinically approved drug therapy for hepatocellular carcinoma treatment and updates of regulatory requirements for approval of such nanomedicines.

Evaluation of the Antidiabetic Potential of an Isolated Hydroalcoholic Fraction from the Fruit of Withania coagulans.

The hydro-alcoholic extract of Withania coagulans fruits was investigated for preliminary phytochemical screening and characterized by high-performance thin-layer chromatography. Column chromatography of the hydro-alcoholic extract of W. coagulans eluted with four different combinations of ethyl acetate and methanol yielded four fractions (WCF01, WCF02, WCF03, and WCF04). One of these fractions, WCF02, significantly (P < 0.05) inhibited in vitro α-amylase and α-glucosidase activity with IC50 values of 104.71 µg/mL and 70.79 µg/mL, respectively. WCF02 further reduced blood glucose levels in comparison to control in the starch tolerance test. The extract showed a relative dose-dependent effect. It was observed that none of the extracts could delay the peak blood glucose that was achieved after 60 min of carbohydrate challenge, but these blunted the glycemic peak.

Surface functionalized folate targeted oleuropein nano-liposomes for prostate tumor targeting: Invitro and invivo activity.

AIMS: This study aims to develop and evaluate oleuropein loaded surface functionalized folate-targeted - PEG liposomes for the effective management of prostate cancer in an animal model. MATERIALS AND METHODS: Film hydration-cum-extrusion technique was used to produce liposomes. Particle size, entrapment efficiency, drug loading, electron microscopy, and drug release study were performed for the characterization. Cell viability and various in vitro studies (phosphatidylserine internalization, TUNEL assay, measurement of mitochondrial membrane potential and caspase-3 assay) were performed to compare the anticancer and apoptotic effects of developed liposomes against the plain oleuropein. Comparative pharmacokinetic profiling and anticancer efficacy studies including a change in tumor volume, body weight, and survival analysis were performed in mice model. KEY FINDINGS: The developed liposomes (OL-FML) showed the particle size of 184.2 ±â€¯9.16 nm, the zeta potential of 1.41 ±â€¯0.24 mV, entrapment efficiency of 63.52 ±â€¯4.15% and drug loading of 21.31 ±â€¯2.37%. OL-FML showed higher in vitro anti-proliferative effect and apoptosis on 22Rv1 cells. In vivo pharmacokinetic study revealed a nearly 6 fold increase in the bioavailability of OL-FML (AUC0→∞ = 641.78 ±â€¯103.764 µg/mL·hr) as compared to OL solution (AUC0→∞ = 104.11 ±â€¯18.374 µg/mL·hr) in mice. Increased tumor suppression, weight loss resistance, and survival probability were observed in 22Rv1 induced tumor-bearing mice with OL-FML treatment as compared to OL. SIGNIFICANCE: The study provides conclusive evidence for the utilization of combining passive and active targeting strategy to enhance the anticancer effect of OL.