ABSTRACT
OBJECTIVE: The present study discusses paclitaxel (PTX)-loaded mannosylated-DSPE (Distearoyl-phosphatidyl-ethanolamine) solid lipid nanoparticles (M-SLNs) using mannose as a lectin receptor ligand conjugate for lung cancer targeting and to increase the anticancer activity of PTX against A549 lung's epithelial cancer cells. MATERIALS AND METHODS: The PTX-SLNs were prepared by solvent injection method and mannose was conjugated to the free amine group of stearylamine. The M-SLNs obtained were characterized for their particle size, polydispersity index, zeta potential and morphology by transmission electron microscope. RESULTS: The M-SLNs were spherical in shape with 254 ± 2.3 nm average size, positive zeta potential (3.27 mV), 79.4 ± 1.6 drug entrapment efficiency and showed the lower extent of drug release 40% over 48 h in vitro. Cytotoxicity study on A549 cell lines and biodistrubtion study of drug revealed that M-SLNs deliver a higher concentration of PTX as compared to PTX-SLNs in an alveolar cell site. DISCUSSION AND CONCLUSION: These results suggested that mannosylated M-SLNs are safe and potential vector for lung cancer targeting.
Subject(s)
Antineoplastic Agents, Phytogenic/administration & dosage , Drug Delivery Systems , Lung Neoplasms/drug therapy , Mannose/analogs & derivatives , Nanoparticles/chemistry , Paclitaxel/administration & dosage , Phosphatidylethanolamines/chemistry , Absorption, Physiological , Animals , Antineoplastic Agents, Phytogenic/pharmacokinetics , Antineoplastic Agents, Phytogenic/pharmacology , Antineoplastic Agents, Phytogenic/therapeutic use , Biological Availability , Cell Line, Tumor , Drug Compounding , Drug Delivery Systems/adverse effects , Drug Liberation , Drug Stability , Drug Storage , Humans , Lung Neoplasms/metabolism , Lung Neoplasms/pathology , Male , Mannose/chemistry , Nanoparticles/adverse effects , Nanoparticles/ultrastructure , Paclitaxel/pharmacokinetics , Paclitaxel/pharmacology , Paclitaxel/therapeutic use , Particle Size , Phosphatidylethanolamines/adverse effects , Pulmonary Alveoli/drug effects , Pulmonary Alveoli/metabolism , Pulmonary Alveoli/pathology , Rats , Surface Properties , Tissue Distribution , Triglycerides/adverse effects , Triglycerides/chemistry , Xenograft Model Antitumor AssaysABSTRACT
OBJECTIVE: The present study discusses folic acid-etoricoxib-bovine serum albumin nanoparticles (F-ETX-NPs) using folic acid as an over expressed folate receptor ligand for activated macrophages in targeting of rheumatoid arthritis. MATERIALS AND METHODS: For this purpose etoricoxib-loaded BSA nanoparticles (ETX-NPs) were prepared by desolvation method and activated folic acid conjugation with free amine group of BSA was confirmed by FTIR study and zeta potential measurements. RESULTS: The F-ETX-NPs showed spherical in shape with 215.8 ± 3.2 nm average size + 7.8 mV zeta potential, 72 ± 1.3% etoricoxib entrapment efficiency and showed 93.1 ± 2.2% cumulative etoricoxib release upto 72 h. The etoricoxib concentration from F-ETX-NPs was found to be 9.67 ± 0.34 µg/g in inflamed joint after 24 h administration revealed remarkably targeting potential to the activated macrophages cells and keep at a high level during the experiment. DISCUSSION AND CONCLUSION: These results suggest that F-ETX-NPs are potentially vector for activated macrophages cells targeting of rheumatoid arthritis.
Subject(s)
Arthritis, Rheumatoid/drug therapy , Drug Delivery Systems/methods , Folic Acid/administration & dosage , Nanoparticles/administration & dosage , Pyridines/administration & dosage , Serum Albumin, Bovine/administration & dosage , Sulfones/administration & dosage , Animals , Arthritis, Rheumatoid/pathology , Cattle , Etoricoxib , Folic Acid/chemistry , Male , Mice , Mice, Inbred BALB C , Nanoparticles/chemistry , Pyridines/chemistry , Serum Albumin, Bovine/chemistry , Sulfones/chemistryABSTRACT
OBJECTIVE: The present study was focused to prepare controlled release glycyrrhizin (GL) conjugated low molecular weight chitosan nanoparticles (CS-NPs) for liver targeting. The hydrophilic antiretroviral drug lamivudine was chosen as a model drug and encapsulated within glycyrrhizin conjugated low molecular weight chitosan nanoparticles (GL-CS-NPs) for liver specificity. METHODS: First, the low molecular weight chitosan (CS) was synthesized through depolymerization method. The low molecular weight chitosan nanoparticles were prepared by inotropic gelation method. Then glycyrrhizin was conjugated with previously prepared low molecular weight chitosan nanoparticles (CS-NPs) and conjugation was confirmed by Fourier transform infrared (FT-IR) spectroscopy. KEY FINDINGS: The prepared GL-CS-NPs were characterized using dynamic light scattering, transmission electron microscopy and FT-IR. The encapsulation efficiency and in-vitro drug release behaviour of drug-loaded GL-CS-NPs were studied using ultra violet spectroscopy and high performance liquid chromatographic methods. Release of lamivudine from the nanoparticles exhibited a biphasic pattern, initial burst release and consequently sustained release. In-vivo biodistribution study suggested the target ability of GL-CS-NPs is better and haematological study shows decline of the tissue damage in comparison with plain drug solution. CONCLUSION: The experimental results show that the glycyrrhizin conjugated LMWC nanoparticles may be used as a potential drug delivery system with hepatocyte-targeting characteristics.
