Abstract:
:Present work describes a novel composition for encapsulating TRPsiRNA (TRPV1-targeting siRNA) within lipid-matrix (4:1::glyceryl behnate:stearic acid) of SLNs, using suitably modified cold high-pressure homogenisation technique. Optimisation of the method and composition conducted using calf-thymus DNA (ctDNA), to avoid cost of TRPsiRNA molecules, resulted in small size (d50 = 50-100 nm) and high entrapment (77.22-98.5%). Complete masking of extreme negative charge of both ctDNA (-34.50 mV) and TRPsiRNA (-23.98 mV) upon encapsulation in SLNs without employing cationic components is reported herein for the first time. Diffusion-controlled release (90.17% at 72 h) from a rigid matrix shifted to porous matrix (at 24 h) due to solubilisation of stearic acid at 37 °C. Efficient in vitro (HEK293 T cells) and in vivo transfection and expression established the proof-of-concept. PEG600 as supporting-surfactant and vitrifying agent promoted small size, effective transfection and rupture of endosomal membrane to affect endosomal escape. Physiological efficacy in terms of significant increase (p < .0001) in paw-withdrawal-latency, following topical and intradermal application of TRPsiRNA-loaded SLNs, in rats, exposed to thermal hyperalgesia (145 and 182%, respectively) and capsaicin-induced pain (155 and 182%, respectively) indicate effective silencing of skin TRPV1. Significant decrease in intensity and duration (one-fifth) of capsaicin-induced nocifensive behaviour was also observed. Naked TRPsiRNA, however, did not show any effect.
journal_name
J Drug Targetjournal_title
Journal of drug targetingauthors
Sharma G,Chopra K,Puri S,Bishnoi M,Rishi P,Kaur IPdoi
10.1080/1061186X.2017.1350857subject
Has Abstractpub_date
2018-02-01 00:00:00pages
135-149issue
2eissn
1061-186Xissn
1029-2330journal_volume
26pub_type
杂志文章abstract::An oral vaccine formulation comprised of starch microparticles with conjugated antigens is being developed. In this report we have examined the uptake of such microparticles by the intestinal mucosa and examined whether the conjugated antigen can influence the uptake. Two model antigens were used: recombinant cholera ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186042000223662
更新日期:2004-06-01 00:00:00
abstract:BACKGROUND:The polycationic nanopeptide RKKRRQRRR is a fragment of HIV-Tat protein known to be a transfection enhancer. Such factors control the transfection efficiency of plasmid DNA complexed with tat peptide. However, their actions are poorly understood. METHODS AND RESULTS:Several cell lines and primary cells were...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/106118604200041403
更新日期:2004-01-01 00:00:00
abstract::Paclitaxel is not effective for treatment of brain cancers because it cannot cross the blood-brain barrier (BBB) due to efflux by P-glycoprotein (P-gp). In this work, glutathione-coated poly-(lactide-co-glycolide) (PLGA) nanoparticles (NPs) of paclitaxel were developed for brain targeting for treatment of brain cancer...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2011.589435
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abstract::Recent studies have shown that drugs that are normally unable to cross the blood-brain barrier (BBB) following intravenous injection can be transported across this barrier by binding to poly(butyl cyanoacrylate) nanoparticles and coating with polysorbate 80. However, the mechanism of this transport so far was not know...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860290031877
更新日期:2002-06-01 00:00:00
abstract::Rabies virus glycoprotein (RVG), a 505 amino acid type-1 glycoprotein, is responsible for the neurotrophic nature of the rabies virus infection. Despite varying reports in the literature as to which receptor is ultimately responsible for interaction of RVG with the nervous system, there is a strong argument for major ...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/1061186X.2016.1223676
更新日期:2017-06-01 00:00:00
abstract::In this review, we emphasize the efforts on the development of radiolabeled nanoparticles (NPs) for cancer treatment, i.e. theranostic tools based on nanotechnology and nuclear medicine. Currently, radionuclide therapy remains to be an important treatment option. The ionizing radiation from radionuclides (not provided...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.3109/1061186X.2014.988216
更新日期:2015-04-01 00:00:00
abstract::A biophysical model was developed, using Ascaris suum as a model gastrointestinal nematode, to provide quantitative perspectives into the microenvironmental pH within the water-filled, porous, negatively charged cuticle matrix of gastrointestinal nematodes. The central features of the model include (a) the constant ra...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869409015888
更新日期:1994-01-01 00:00:00
abstract::I125 radiolabelled HSA (HSA-I125) was utilised as a probe to quantify protein adsorption onto polystyrene (PS) and Poloxamine 908 coated PS (PS-908) particles. Upon ageing of the HSA-I125 a dramatic increase in the amount of protein adsorbed onto the two particle systems was observed. This phenomenon was not due to la...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869708995849
更新日期:1997-01-01 00:00:00
abstract::The transport of 125I-radiolabelled latex nanoparticles across the nasal mucosa of rats was studied using a range of particle sizes and surface coatings. Translocation of the particles into the blood stream was examined by means of monitoring the radiolabel associated with the particles. Particles were detected in the...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611860108997935
更新日期:2001-01-01 00:00:00
abstract:BACKGROUND:High expression of glucagon-like peptide-1 receptor (GLP-1R) in insulinoma supplies a potential drug target for tumor imaging. Exendin-4 can specifically bind to GLP-1R as an agonist and its analogs are extensively used in receptor imaging studies. PURPOSE:A new GLP-1R imaging agent, [(18)F]AlF-NOTA-MAL-Cys...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2015.1020808
更新日期:2015-01-01 00:00:00
abstract::We have developed a new method to evaluate the transfer of macromolecular drugs to intrapulmonary lymph nodes in rats after intrapulmonary administration. By using this method, we observed that the transfer of fluorescein isothiocyanate dextrans (FDs) to the intrapulmonary lymph nodes was markedly higher than that to ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869509015955
更新日期:1995-01-01 00:00:00
abstract::Drug systems targeting tumor cells using basic fibroblast growth factor (bFGF) have been widely reported. In this study, the peptide KRTGQYKLC (bFGFp), containing cysteine at the carboxyl termination of the bFGF-derived peptide, was applied as a novel ligand targeting tumor cells. bFGFp was conjugated with bovine seru...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860600849498
更新日期:2006-09-01 00:00:00
abstract::An aqueous dispersion of self-organized phospholipid tubules has been utilized as the template for silica-deposited nanotubules (approximately 0.5 microm thick and >10 microm long) by a sol-gel method. The formation of the hybrid tubules was mechanistically investigated by controlled sol-gel reaction. The incorporatio...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860802295581
更新日期:2008-11-01 00:00:00
abstract::Graphene, the mother of all carbon materials, has unlocked a new era of biomedical nanomaterials due to its exceptional biocompatibility, physicochemical and mechanical properties. It is a single atom thick, nanosized, two-dimensional structure and provides high surface area with adjustable surface chemistry to form h...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2018.1437920
更新日期:2018-12-01 00:00:00
abstract::Polynucleotides are anionic macromolecules which are expected to transfer into the targeted cells through specific uptake mechanisms. So, we developed polynucleotides coating complexes of plasmid DNA (pDNA) and polyethylenimine (PEI) for a secure and efficient gene delivery system and evaluated their usefulness. Polya...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2014.950665
更新日期:2015-01-01 00:00:00
abstract::The purpose of this research is to develop ligand-targeted plasmid based gene delivery systems for gene transfer to tumor endothelium. Cell adhesion assays were used to test the peptide inhibition of human endothelial cell adsorption to vitronectin-treated tissue culture plates. A series of RGD containing peptides wer...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860410001724468
更新日期:2004-05-01 00:00:00
abstract::HEK cells were transfected with the GFP gene using various vectors: naked DNA, lipofectamine, and both PLGA and P(FASA) plasmid-loaded nanospheres. All methods were assessed alone and with the use of chloroquine, a lysosomal enzyme inhibitor. Transfection efficiencies were determined and compared at various times post...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186021000038373
更新日期:2002-09-01 00:00:00
abstract::The purpose of the study was to develop the liposomal formulations of TFu for oral and intravenous (i.v.) administration, clarify the biodistribution characteristics and in vivo pharmacokinetic behaviors of TFu-loaded liposomes. Four TFu-loaded liposomes of different sizes were prepared and characterized. The pharmaco...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860801927598
更新日期:2008-06-01 00:00:00
abstract::Archaeal ether glycerolipid vesicles (archaeosomes) efficiently deliver exogenous antigen for induction of humoral and cell-mediated immunity. Because induction of CD8 cytotoxic T cells is critical for protective vaccination against tumors, we compared the ability of various archaeosome lipid compositions to evoke a s...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860410001670044
更新日期:2003-01-01 00:00:00
abstract:BACKGROUND:Multifunctional gold nanospheres (MGNs)-loaded with docetaxel (MGN@DTX) were prepared and evaluated for therapeutic efficacy in nude mice bearing human prostate cancer xenografts. METHODS:MGNs were prepared from PEGylated hollow gold nanospheres (HGNs) coated with folic acid and DTPTT chelate. Then, the eff...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2015.1018910
更新日期:2015-01-01 00:00:00
abstract::As a percutaneous sustained-release preparation, insulin micropiles (MPs) were prepared with biodegradable polymers poly(lactic acid) (PLA), poly(ϵ-caprolactone) (PCL) and poly(lactic-co-glycolic acid) (PLGA) as the base. The obtained PLA, PCL, and PLGA MPs of which the insulin:polymer ratio was 1:2 were administered ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2010.492521
更新日期:2011-04-01 00:00:00
abstract::The aim of the present study was to develop a polymeric delivery system for water-insoluble drug oridonin. Amphiphilic block copolymers, poly(epsilon-caprolactone)-poly(ethylene glycol)-poly (epsilon-caprolactone) (PCL-PEO-PCL), were synthesized by ring-opening polymerization of caprolactone initiated by the hydroxyl ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860802200938
更新日期:2008-07-01 00:00:00
abstract::This study was aimed to generate a new agent, norcantharidin (NCTD) encapsulated liposomes modified with a novel murine anti-human CD19 monoclonal antibody 2E8 (2E8–NCTD–liposomes), to specifically target the B-lineage leukemia stem cells (B-LSCs) and their progeny in vitro. Our results have shown that the positive pe...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611861003649720
更新日期:2010-11-01 00:00:00
abstract::A promising strategy to carry genetic material to brain cells either in vitro or in vivo is using the LDL receptor (LDLr) on blood-brain barrier. LDLr naturally help to low density lipoproteins (LDL(S)) transporting across the BBB by endocytosis. Here we present the idea of using the LDLr-mediated pathway for transpor...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860601148908
更新日期:2007-04-01 00:00:00
abstract::Cell-penetrating peptides (CPPs) are efficient vehicles to transport bioactive molecules into the cells. Despite numerous studies the exact mechanism by which CPPs facilitate delivery of cargo to its intracellular target is still debated. The current work presents methods that can be used for tracking CPP/pDNA complex...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2015.1095194
更新日期:2016-01-01 00:00:00
abstract::The effects of concentration, amperage and duration on the antidiuretic response induced by iontophoretic delivery of desmopressin acetate (DDAVP) were examined using a diabetes insipidus model in rats. A higher current density brought about a larger and longer antidiuretic response. Prolonged iontophoretic duration c...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869509015918
更新日期:1995-01-01 00:00:00
abstract::Chloramphenicol-loaded (CHL) poly-d,l-lactic-co-glycolic acid (PLGA) nanoparticles (NPs) were prepared by emulsification solvent evaporation technique either by using polyvinyl alcohol (PVA) as emulsion stabilizer or polysorbate-80 (PS-80) as surfactant and characterised by transmission electron microscopy, zeta-poten...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860801899300
更新日期:2008-05-01 00:00:00
abstract::Toxoplasmic encephalitis (TE) is the most common clinical manifestation of reactivated infection with Toxoplasma gondii in immunocompromised patients that is lethal if untreated. The combination of pyrimethamine plus sulfadiazine or clindamycin is the standard therapy for the treatment of TE, but these combinations ar...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611861003733995
更新日期:2011-02-01 00:00:00
abstract::A novel concept in drug delivery discussed here, takes advantage of certain properties of the drug "containers" cyclodextrins and liposomes to combine them into a single system thus circumventing problems associated with both systems. The concept, entailing entrapment of water-soluble cyclodextrin-drug inclusion compl...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.3109/10611869408996821
更新日期:1994-01-01 00:00:00
abstract::The biodistribution of orally and intravenously administered archaeosomes in mice was compared to that of archaeosomes containing either coenzyme Q10 (archaeosome-CoQ10), polyethylene glycol (archaeosome-PEG), or PEG plus CoQ10 (archaeosome-PEG-CoQ10). The archaeosome formulations were prepared by a reverse-phase evap...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869909085521
更新日期:2000-01-01 00:00:00