Characterization, biorecognitive activity and stability of WGA grafted lipid nanostructures for the controlled delivery of Rifampicin

Targeted nanomedicines improve the delivery of drugs by increasing the drug concentration at target site, protecting the premature degradation and releasing the encapsulated drug in controlled manner. To make rifampicin (RFN) delivery more effective, we designed and characterized wheat germ agglutinin (WGA) conjugated, RFN loaded solid-lipid nanoparticles (WRSN). Nanoparticles were prepared by solvent emulsification/evaporation and conjugated with fluorescein isothiocyanate-labeled WGA. Important characteristics, such as particle size, zeta potential, encapsulation efficiency, conjugation efficiency and in vitro drug release behavior, were investigated. WGA conjugation to the nanoparticles was confirmed by Fourier Transform Infrared (FTIR) analysis. Conjugation efficiency was determined by fluorescent spectroscopy and Bradford assay. RFN was released from nanoparticles via the diffusion-controlled, non-fickian and supercase II mechanism. A haemaglutination test confirmed that WGA retained its bio-recognition activity and sugar-binding specificity after it was coupled with the nanoparticles. In vitro experiments demonstrated that WRSN interacted more than non-conjugated nanoparticles with porcine mucin. WRSN were stable in the presence of electrolytes up to 1M concentration. Therefore, WGA-conjugated solid lipid nanoparticles could be a promising tool for the controlled delivery of RFN or other anti-tubercular drugs

Optimization of solid lipid nanoparticles prepared by a single emulsification-solvent evaporation method

This data article contains the data related to the research article "Characterization, biorecognitive activity and stability of WGA grafted lipid nanostructures for the controlled delivery of rifampicin" (Pooja et al. 2015) [1]. In the present study, SLN were prepared by a single emulsification-solvent evaporation method and the various steps of SLN preparation are shown in a flow chart. The preparation of SLN was optimized for various formulation variables including type and quantity of lipid, surfactant, amount of co-surfactant and volume of organic phase. Similarly, effect of variables related to homogezation, sonication and stirring processes, on the size and surface potential of SLN was determined and optimized

Nanomedicines for targeted delivery of etoposide to non-small cell lung cancer using transferrin functionalized nanoparticles

Lung cancer is the most common cause of cancer death. Clinical applications of anticancer drugs are limited due to non-specificity and systemic toxicity. Transferrin (Tf) receptors have been recognized to be up-regulated in several malignant carcinomas including non-small cell lung cancer. Herein, we investigate the anticancer activity of Tf conjugated and etoposide (ETPS) loaded solid lipid nanoparticles (Tf-ESN) against Tf-receptors expressing A549 human non-small cell lung cancer cells. Pharmacokinetic and tissue-distribution profiles of nanoparticles were studied in Balb/c mice. Targeted nanoparticles showed significantly higher anticancer activity of etoposide manifested by anti-proliferation assay, morphological changes and induced apoptosis in A549 cells. In biodistribution studies, Tf-ESN had higher plasma concentration, longer blood circulation and decrease in clearance of encapsulated ETPS than Etosid®, a marketed formulation of etoposide. In conclusion, the promising results of this study suggest that targeting of nanomedicines to Tf-receptors, those that are over expressed in non-small cell lung cancer could increase the therapeutic efficacy of lung cancer therapy

Serotonin-Stearic Acid Bioconjugate-Coated Completely Biodegradable Mn3O4 Nanocuboids for Hepatocellular Carcinoma Targeting

In this study, a serotonin-stearic acid (ST-SA)-based bioconjugate was synthesized for the surface modification of manganese oxide-based nanocuboids (MNCs) for delivering of anticancer drug (i.e., doxorubicin hydrochloride (DOX)) to human liver cancer cells. MNCs were synthesized by chemical precipitation method, and their surface was modified with ST-SA bioconjugate for targeting of MNCs to cancer cells. The ST-SA@MNCs along with DOX showed good colloidal stability, high drug encapsulation (98.3%), and drug loading efficiencies (22.9%) as well as pH-responsive biodegradation. Coating with ST-SA conjugate provided a shield to MNCs which sustained their degradation in an acidic environment. The release of DOX was higher (81.4%) in acidic media than under the physiological conditions (20.5%) up to 192 h. The in vitro anti-proliferation assay showed that ST-SA@MNCs exhibit higher cell growth inhibition compared to that of pure DOX after 48 h of treatment. The cellular uptake and apoptosis studies revealed the enhanced uptake of ST-SA@MNCs in contrast to the MNCs due to overexpressed ST receptor on hepatocellular carcinoma cells and triggered the generation of reactive oxygen species in the cells. Therefore, these results indicated that the DOX-loaded, ST-SA stabilized MNCs improved the therapeutic index of DOX and would be a promising therapeutic candidate for tumor therapy

Modulating the site-specific oral delivery of sorafenib using sugar-grafted nanoparticles for hepatocellular carcinoma treatment

Globally, one in six deaths is reported due to cancer suggesting the critical need for development of advanced treatment regimens. In this study, solid lipid nanoparticles (SLN) were prepared and appended with polyethylene glycol (PEGylated) galactose and a multikinase inhibitor sorafenib (SRFB) was used as chemotherapeutic drug, for treating hepatocellular carcinoma (HCC). The nanoparticles were evaluated for in-vitro and in-vivo performances to showcase the targeting efficiency and therapeutic benefits of the sorafenib loaded ligand conjugated nanoparticles (GAL-SSLN). When compared with SRFB or Sorafenib loaded SLN, GAL-SSLN showed superior cytotoxicity and apoptosis in HepG2 (human hepatocellular carcinoma cells). In addition, in-vivo pharmacokinetics and real time biodistribution studies in BALB/c mice showed that the surface conjugation of nanoparticles with galactose resulted in better pharmacokinetic performance and targeted delivery of the nanoparticles to liver. Results indicated that GAL-SSLN showed promising attributes in terms of targeting sorafenib to liver and therapeutic efficacy