Nano-carriers for drug routeing - towards a new era.

The objective of this article is to propose a re-visiting of the paradigms of nano-carriers based drug routeing from an industrial viewpoint. The accumulation of drugs in specific body compartments after intravenous administration and the improvement of the oral bioavailability of peptides were taken as examples to propose an update of the translational framework preceding industrialisation. In addition to the recent advances on the biopharmacy of nano-carriers, the evolution of adjacent disciplines such as the biology of diseases, the chemistry of polymers, lipids and conjugates, the physico-chemistry of colloids and the assembling of materials at the nanoscale (referred to as microfluidics) are taken into account to consider new avenues in the applications of drug nano-carriers.

Comparison of high pressure homogenization and stirred bead milling for the production of nano-crystalline suspensions.

Currently, the two technologies primarily used for the manufacturing of nano-crystalline suspensions using top down process (i.e. wet milling) are high pressure homogenization (HPH) and stirred bead milling (SBM).

Building the design, translation and development principles of polymeric nanomedicines using the case of clinically advanced poly(lactide(glycolide))-poly(ethylene glycol) nanotechnology as a model: An industrial viewpoint.

The design of the first polymeric nanoparticles could be traced back to the 1970s, and has thereafter received considerable attention, as evidenced by the significant increase of the number of articles and patents in this area. This review article is an attempt to take advantage of the existing literature on the clinically tested and commercialized biodegradable PLA(G)A-PEG nanotechnology as a model to propose quality building and outline translation and development principles for polymeric nano-medicines. We built such an approach from various building blocks including material design, nano-assembly - i.

Oral delivery of diabetes peptides - Comparing standard formulations incorporating functional excipients and nanotechnologies in the translational context.

While some orally delivered diabetes peptides are moving to late development with standard formulations incorporating functional excipients, the demonstration of the value of nanotechnology in clinic is still at an early stage. The goal of this review is to compare these two drug delivery approaches from a physico-chemical and a biopharmaceutical standpoint in an attempt to define how nanotechnology-based products can be differentiated from standard oral dosage forms for oral bioavailability of diabetes peptides. Points to consider in a translational approach are outlined to seize the opportunities offered by a better understanding of both the intestinal barrier and of nano-carriers designed for oral delivery.

Squalenoyl nanomedicine of gemcitabine is more potent after oral administration in leukemia-bearing rats: study of mechanisms.

In an earlier report, we demonstrated the superior anticancer efficacy of orally administered squalenoyl gemcitabine (SQdFdC) nanomedicine over its parent drug gemcitabine on rats bearing RNK-16 large granular lymphocytic (LGL) leukemia. In the present communication, we investigated the mechanisms behind this observation both at the cell and tissue level. The mechanisms were investigated by performing cytotoxicity, cell uptake, and biodistribution experiments.

Tumoricidal effects of etoposide incorporated into solid lipid nanoparticles after intraperitoneal administration in Dalton's lymphoma bearing mice.

The tumoricidal effects of etoposide incorporated into lipid nanoparticles after single-dose administration were investigated in Dalton's lymphoma ascites bearing mice. Etoposide and its nanoparticle formulations were administered intraperitoneally, and the cell cycle perturbation, cytogenetic damage, cell death (apoptosis), tumor regression, and animal survival were investigated as parameters of response with time. The tumor burden of mice treated with etoposide and its nanoparticle formulations decreased significantly (P < .

Enhanced delivery of etoposide to Dalton's lymphoma in mice through polysorbate 20 micelles.

The study evaluates the possibility of enhancing uptake of etoposide (topoisomerase II inhibitor) by tumor when delivered through polysorbate 20 micelles. The micelle formation was ascertained by determining the critical micellar concentration (CMC) with a du Nouy ring tensiometer and by size measurement using dynamic light scattering. Addition of 5% ethanol decreased the CMC of Polysorbate 20 (from 5.

Rapid and sensitive HPLC method for the estimation of doxorubicin in dog blood--the silver nitrate artifact.

A rapid and sensitive high performance liquid chromatographic (HPLC) assay utilizing fluorimetric detection (excitation at 480 nm, emission at 560 nm) for the determination of doxorubicin in dog blood was developed and validated. Treatment of blood samples containing doxorubicin with AgNO3 (as protein precipitant) resulted in appearance of an additional peak in the chromatogram of doxorubicin at 11.5 min along with the parent peak (tR = 5.

Etoposide-incorporated tripalmitin nanoparticles with different surface charge: formulation, characterization, radiolabeling, and biodistribution studies.

Etoposide-incorporated tripalmitin nanoparticles with negative (ETN) and positive charge (ETP) were prepared by melt emulsification and high-pressure homogenization techniques. Spray drying of nanoparticles led to free flowing powder with excellent redispersibility. The nanoparticles were characterized by size analysis, zeta potential measurements, and scanning electron microscopy.

Influence of polymerization technique and experimental variables on the particle properties and release kinetics of methotrexate from poly(butylcyanoacrylate) nanoparticles.

Poly(butylcyanoacrylate) nanoparticles were prepared by dispersion polymerization (DP) and emulsion polymerization (EP) of n-butyl cyanoacrylate monomer. The particles were characterized by infrared spectroscopy, differential scanning calorimetry, X-ray diffractometry and transmission electron microscopy. Particle properties such as size and zeta potential were determined for nanoparticles prepared by DP and EP techniques and compared.