Further Development of Near-Infrared Mediated Quantum Dots and Paclitaxel Co-loaded Nanostructured Lipid Carrier System for Cancer Theragnostic.

Of colloidal systems, ceteris paribus, nanostructured lipid carriers are second to none in offering a single-unit platform for multifunctional benefits. Quantum dots are known to possess unique properties that make them ideal for imaging purpose and that they may be used for cancer detection. For several decades, paclitaxel has been the most effective drug against a wide range of solid tumours. Theragnostic nanomedicine provides a platform to monitor, evaluate, and individualize treatment in real time. Evaluation of cancer treatment outcome at an early stage therapy is key to increase survival prospects of a patient. Previously, a novel co-loaded nanostructured lipid carriers' theragnostic system for parenteral administration was developed. The aim of this study was to further investigate the co-loaded nanostructured lipid carriers in order to provide interpretation necessary for preclinical elucidation of the formulation, in part. The co-loaded nanostructured lipid carriers were prepared by oil/water emulsification-solvent evaporation technique. In this study, stability and co-loaded nanostructured lipid carriers' internalization by MCF 7 and HepG2 cells were investigated. The co-loaded nanostructured lipid carriers was stable at 4°C for 1 month. The formulation was successfully internalized by MCF-7 and HepG2 cells. Nevertheless, the co-loaded nanostructured lipid carrier was more apt for MCF-7 cells. This finding affirms the formulation to be the most appropriate for breast cancer treatment. In addition, if taken correctly by a patient for a month, the formulation would give true reflection of the contents' amounts, the factor paramount to appropriate changes in treatment protocol. It can therefore safely be concluded that the co-loaded nanostructured lipid carrier formulation may be potentially an effective theragnostic translational system.

Biomacromolecule/lipid hybrid nanoparticles for controlled delivery of sorafenib in targeting hepatocellular carcinoma therapy.

AIM: Hybrids composed of various materials are highly versatile for drug delivery in tumor therapy including hepatocellular carcinoma. Herein, a sorafenib (SF)-loaded biomacromolecule hyaluronic acid (HA)/lipid hybrid nanoparticles (HA/SF-cLNS) were developed for targeting drug delivery. MATERIALS & METHODS: In vitro assays determined HA/SF-cLNS release behavior, enzymatic degradation, uptake and cytotoxicity. H22-bearing liver cancer xenograft murine models were used to evaluate the biodistribution and therapeutic efficacy in vivo. RESULTS: HA/SF-cLNS could be disassembled and drug was released in response to hyaluronidase. In vivo imaging results demonstrated HA/cLNS could enhance drug accumulation at tumor site. Meanwhile, HA/SF-cLNS exhibited improved antitumor efficacy in vitro and in vivo. CONCLUSION: HA/SF-cLNS demonstrated the potential to enhance antitumor efficacy of SF.

Pulmonary delivery of an ultra-fine oxytocin dry powder formulation: potential for treatment of postpartum haemorrhage in developing countries.

Oxytocin is recommended by the World Health Organisation as the most effective uterotonic for the prevention and treatment of postpartum haemorrhage. The requirement for parenteral administration by trained healthcare providers and the need for the drug solution to be maintained under cold-chain storage limit the use of oxytocin in the developing world. In this study, a spray-dried ultrafine formulation of oxytocin was developed with an optimal particle size diameter (1-5 µm) to facilitate aerosolised delivery via the lungs. A powder formulation of oxytocin, using mannitol, glycine and leucine as carriers, was prepared with a volume-based median particle diameter of 1.9 µm. Oxytocin content in the formulation was assayed using high-performance liquid chromatography-mass spectroscopy and was found to be unchanged after spray-drying. Ex vivo contractility studies utilising human and ovine uterine tissue indicated no difference in the bioactivity of oxytocin before and after spray-drying. Uterine electromyographic (EMG) activity in postpartum ewes following pulmonary (in vivo) administration of oxytocin closely mimicked that observed immediately postpartum (0-12 h following normal vaginal delivery of the lamb). In comparison to the intramuscular injection, pulmonary administration of an oxytocin dry powder formulation to postpartum ewes resulted in generally similar EMG responses, however a more rapid onset of uterine EMG activity was observed following pulmonary administration (129 ± 18 s) than intramuscular injection (275 ± 22 s). This is the first study to demonstrate the potential for oxytocin to elicit uterine activity after systemic absorption as an aerosolised powder from the lungs. Aerosolised oxytocin has the potential to provide a stable and easy to administer delivery system for effective prevention and treatment of postpartum haemorrhage in resource-poor settings in the developing world.