Orphan Formulations in Pediatric Schistosomiasis Treatment: Development and Characterization of Praziquantel Nanoparticle-Loaded Powders for Reconstitution.

Praziquantel is a broad spectrum antihelmintic agent and represents the drug of choice for the treatment of schistosomiasis. However, its low aqueous solubility and strong bitter taste highly affect the bioavailability and compliance in pediatric patients. Thus, the purpose of this study was to develop a dry nanosuspension, by a combination of high-pressure homogenization and spray drying, intended for redispersion in a pleasant taste vehicle for extemporaneous use. Three formulations, varying stabilizers to drug ratio, were developed and characterized in terms of particle size distribution, crystallinity, morphology, in vitro dissolution, and sedimentation-redispersibility behavior. A significant reduction in particle size was achieved after the high-pressure homogenization process, and the nanoparticles were further microencapsulated by spray drying technique. The redispersed dried powders exhibited a conserved particle size distribution (in the nanometric range) and certain crystallinity extent, with satisfactory redispersion ability. Besides, the enhancement of the dissolution performance obtained after comminution was conserved, even after drying and redispersion of the extemporaneous powdered formulation. In conclusion, the developed nanoparticle-loaded powders comprise an interesting tool for the administration of praziquantel to preschool-age children.

Near-infrared spectroscopic applications in pharmaceutical particle technology.

Near-infrared spectroscopy (NIRS) is nowadays an established analytical technique in the pharmaceutical industry. The aim of this review is to present the progress of NIRS in providing useful information for pharmaceutical particle technology. NIR methods are now developed to characterize a wide variety of materials (active pharmaceutical ingredients, excipients, co-processed powders, and physical mixtures) and pharmaceutical dosage forms (conventional, modified drug release technologies, and phytomedicines). This review also provides a number of spectra to illustrate the fundamental understanding of NIRS which has been gained. The sampling that must occur prior to the acquisition of near-infrared spectra is also discussed, as well as developments in monitoring mixing, tableting, and coating. This review will be valuable for product formulation and process engineering specialists.

Praziquantel systems with improved dissolution rate obtained by high pressure homogenization.

Praziquantel (PZQ), an antihelmintic agent commonly administered to humans and cattle, has low aqueous solubility, which compromises its bioavailability and efficacy. The purpose of this study was to develop a new formulation, in order to improve PZQ dissolution rate. PZQ dispersions have been developed by high-pressure homogenization (HPH) using different stabilizers, selected upon PZQ saturation solubility. After the screening, two promising formulations were developed, combining poloxamer 188 with polyvinylpyrrolidone or maltodextrin. Characterization studies including particle size distribution, crystallinity, morphology, drug content, and in vitro dissolution profiles, were performed over selected formulations. The scanning electronic micrographs revealed that the morphology of suspended particles corresponded to elongated shapes, with an average particle size close to the micron range. X-ray powder diffractometry and differential scanning calorimetry results confirmed the drug crystallinity, before and after the HPH process. Besides, differential scanning calorimetry revealed the absence of interactions between PZQ and excipients. The dissolution rate of PZQ dispersions was significantly enhanced compared with raw PZQ, either in phosphate buffer or hydrochloric acid, mainly due to particle size reduction, thus improved saturation solubility.

Challenges and opportunities in polymer technology applied to veterinary medicine.

An important frontier in the administration of therapeutic drugs to veterinary species is the use of different polymers as drug delivery platforms. The usefulness of polymers as platforms for the administration of pharmaceutical and agricultural agents has been clearly recognized in the recent decades. The chemical versatility of polymers and the wide range of developed controlled-release strategies enhance the possibilities for the formulation of active molecules. In particular, the veterinary area offers opportunities for the development of novel controlled-release drug delivery technologies adapted to livestock or companion animal health needs. In some cases, it also allows to improve profitability in meat production or to meet the safety criteria related to drug residues. A number of factors affect the selection of polymers and subsequent properties of the controlled-release drug delivery system. However, their selection also dictates the release kinetics of the drug from the delivery system. Such choices are therefore crucial as they affect the success and potential of the delivery system for achieving the therapeutic goals of the veterinarian. It is the intention of this review to give an overview of the most relevant polymers, which are used or have been tested as drug delivery release rate modifiers in the veterinary field. The article highlights some recent developments focusing on their advantages and applications and analyzes the future direction of the scientific and technological advancements in this area.