Pharmacology

Micro and nano polycaprolactone particles preparation by pulsed back-and-forward cross-flow batch membrane emulsification for parenteral administration
In the pharmaceutical field, manufacturing processes which are able to make products with tailored size at suitable shear stress conditions and high productivity are important requirements for their industrial application. Cross-flow and premix membrane emulsification are the membrane-based processes generally used for particles preparation at large scale, however some disadvantages still limit...


Corneal targeted nanoparticles for sustained natamycin delivery and their PK/PD indices: An approach to reduce dose and dosing frequency
Natamycin is the only approved medication for the treatment of mycotic keratitis. Current dosage regimen include one drop of natamycin suspension (5% w/v) instilled in the conjunctival sac at hourly or two hourly intervals for several days which has poor patient compliance. The purpose of the present study was to design a corneal targeted nanoformulation in order to reduce dose and dosing frequ...
Oil-enriched, ultra-small nanostructured lipid carriers (usNLC): A novel delivery system based on flip–flop structure
For the development of ultra-small NLC (usNLC) the determination of the required HLB (hydrophilic lipophilic balance) was found to be a suitable method, i.e., usNLC with a size below 50nm were obtained by this method. Loading with 5% (w/w) coenzyme Q10 (Q10) led to usNLC with a size of about 85nm. In comparison to classical NLC with a size of 230nm and a nanoemulsion with similar size, the Q10 ...


Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application
Nlc topical formulation as an alternative to oral and parenteral (IM) delivery of artemether (ART), a poorly water-soluble drug was designed. A Phospholipon 85G-modified Gelucire 43/01 based nlc formulation containing 75% Transcutol was chosen from DSC studies and loaded with gradient concentration of ART (100–750mg). ART-loaded nlcs were stable (−22 to −40mV), polydispersed (0.4–0.7) w...
Acetalated dextran encapsulated AR-12 as a host-directed therapy to control Salmonella infection
Ar-12 has been evaluated in clinical trials as an anti-cancer agent but also has demonstrated host-directed, broad-spectrum clearance of bacteria. We have previously shown that ar-12 has activity in vitro against Salmonella enterica serovar Typhimurium and Francisella species by inducing autophagy and other host immune pathways. ar-12 treatment of S. Typhimurium-infected mice resulted in a 10-f...


The crystallinity of cellulose controls the physical distribution of sorbed water and the capacity to present water for chemical degradation of a solid drug
The purpose of the research was to investigate the effect of moisture content of cellulose on the degradation of a drug in binary mixtures with cellulose. Physical mixtures of acetylsalicylic acid and two forms of cellulose, either microcrystalline cellulose or low crystalline cellulose, in the proportion 1:1 were stored at 50°C at a series of relative humidities (0–90%) for up to 175 days. ...
Theoretical investigations into the influence of the position of a breaking line on the tensile failure of flat, round, bevel-edged tablets using finite element methodology (FEM) and its practical relevance for industrial tablet strength testing
Flat, round tablets may have a breaking (“score”) line. Pharmacopoeial tablet breaking load tests are diametral in their design, and industrially used breaking load testers often have automatic tablet feeding systems, which position the tablets between the loading platens of the machine with the breaking lines in random orientation to the applied load. The aim of this work was to ascertain ...

Stabilization of amorphous paracetamol based systems using traditional and novel strategies
There is a special interest in having pharmaceutical active ingredients in the amorphous state due to their increased solubility and therefore, higher bioavailability. Nevertheless, not all of them present stable amorphous phases. In particular, paracetamol is an active ingredient widely known for its instability when prepared in the amorphous state. In the present work thermally stable amorpho...
Antisolvent precipitation of novel xylitol-additive crystals to engineer tablets with improved pharmaceutical performance
The purpose of this work was to develop stable xylitol particles with modified physical properties, improved compactibility and enhanced pharmaceutical performance without altering polymorphic form of xylitol. Xylitol was crystallized using antisolvent crystallization technique in the presence of various hydrophilic polymer additives, i.e., polyethylene glycol (PEG), polyvinylpyrrolidone (PVP) ...

Protein release from electrospun nonwovens: Improving the release characteristics through rational combination of polyester blend matrices with polidocanol
Nonwoven scaffolds consisting of poly-ε-caprolactone (PCL), poly(lactic-co-glycolic acid) (PLGA) and polidocanol (PD), and loaded with lysozyme crystals were prepared by electrospinning. The composition of the matrix was varied and the effect of PD content in binary mixtures, and of PD and PLGA content in ternary mixtures regarding processability, fiber morphology, water sorption, swelling and...
Effects of stabilizing agents on the development of myricetin nanosuspension and its characterization: An in vitro and in vivo evaluation
Although myricetin has various pharmacological applications, it shows low oral bioavailability (<10%) in rats due to its poor aqueous solubility. To overcome this issue, myricetin nanosuspensions were developed and the effects of stabilizers were investigated. Based on the particle size and zeta potential, stabilizers soya lecithin, TPGS, HP-β-CD, and/or a combination thereof were used....

Release characteristics of polyurethane tablets containing dicarboxylic acids as release modifiers – a case study with diprophylline
The influence of several dicarboxylic acids on the release characteristics of polyurethane tablets with a high drug load was investigated. Mixtures of diprophylline (Dyph) and thermoplastic polyurethane (TPUR) (ratio: 50/50, 65/35 and 75/25wt.%) were hot-melt extruded and injection molded with the addition of 1, 2.5, 5 and 10% wt.% dicarboxylic acid as release modifier. Incorporating malonic, s...
A Cross-Country Comparison of Rivaroxaban Spontaneous Adverse Event Reports and Concomitant Medicine Use with the Potential to Increase the Risk of Harm
Concerns with the safety profiles of the newer anticoagulants have been raised because of differences in treatment populations between pre-marketing studies (randomized controlled trials) and clinical practice. Little is known about the potential safety issues and the reporting in spontaneous adverse event databases associated with rivaroxaban. To analyse spontaneous adverse event reports assoc...
Evaluation of Drug–Polymer Solubility Curves Through Formal Statistical Analysis: Comparison of Preparation Techniques
In this study, the influence of the preparation technique (ball milling, spray drying, and film casting) of a supersaturated amorphous dispersion on the quality of solubility determinations of indomethacin in polyvinylpyrrolidone was investigated by means of statistical analysis. After annealing of the amorphous dispersions above the crystallization temperature for 2 h, the solubility curve was...
Characterization of an Oncolytic Herpes Simplex Virus Drug Candidate
The structural integrity and conformational stability of a genetically modified live, oncolytic herpes simplex virus (o-HSV) were investigated across a wide pH (5.5–8.0) and temperature (10°C–87.5°C) range. A combination of circular dichroism, intrinsic and extrinsic fluorescence, and static light scattering results was visualized using an empirical phase diagram approach to provide a glo...