Promises of a biocompatible nanocarrier in improved brain delivery of quercetin: Biochemical, pharmacokinetic and biodistribution evidences.

Breast cancer (BC) is one of the leading causes of death from cancer in women; second only to lung cancer. Tamoxifen (TAM) is a hydrophobic anticancer agent and a selective estrogen modulator (SERM), approved by the FDA for hormone therapy of BC. Despite having striking efficacy in BC therapy, concerns regarding the dose-dependent carcinogenicity of TAM still persist, restricting its therapeutic applications. Nanotechnology has emerged as one of the most important strategies to solve the issue of TAM toxicity, owing to the ability of nano-enabled-formulations to deliver smaller concentrations of TAM to cancer cells, over a longer period of time. Various TAM-containing-nanosystems have been successfully fabricated to selectively deliver TAM to specific molecular targets found on tumour membranes, reducing unwanted toxic effects. This review begins with an outline of breast cancer, the current treatment options and a history of how TAM has been used as a combatant of BC. A detailed discussion of various nanoformulation strategies used to deliver lower doses of TAM selectively to breast tumours will then follow. Finally, a commentary on future perspectives of TAM being employed as a targeting vector, to guide the delivery of other therapeutic and diagnostic agents selectively to breast tumours will be presented.

https://www.mdpi.com/1420-3049/25/5/1182/pdf

Novel Tamoxifen Nanoformulations for Improving Breast Cancer Treatment: Old Wine in New Bottles.

Dimethyl fumarate (DMF) is an approved drug for the management of relapsing multiple sclerosis. Despite efficacy, DMF is also reported to be a challenging drug owing to concerns like gastrointestinal tract flushing, multiple dosing, lower brain permeability, less patient compliance, and economic hurdles. The present study aims to develop DMF-tocopherol acetate nanolipidic carrier (NLCs) to enhance brain permeability and improve the gastric tolerance. The developed DMF-tocopherol acetate NLCs offered an average size of 69.70 nm, PDI of 0.317, and a zeta potential of −9.71 mV. Higher drug entrapment (90.12%) and drug loading (20.13%) assured controlled drug release behavior both in gastric and intestinal pH. Cellular uptake studies on Caco-2 and SH-SY5Y monolayers confirmed better intestinal absorption and neuronal uptake of the developed system, which was further corroborated by the pharmacokinetic and biodistribution studies. The oral bioavailability was enhanced by 4.09 times and brain availability was s...

Enhanced Brain Delivery of Dimethyl Fumarate Employing Tocopherol-Acetate-Based Nanolipidic Carriers: Evidence from Pharmacokinetic, Biodistribution, and Cellular Uptake Studies

In vivo pharmacokinetic studies and intracellular delivery of methotrexate by means of glycine-tethered PLGA-based polymeric micelles.

PLGA-soya lecithin based micelles for enhanced delivery of methotrexate: Cellular uptake, cytotoxic and pharmacokinetic evidences.

The present work aims to develop tamoxifen-loaded polymeric micelles and explore their potential in topical delivery of the drug to breast cancer cells. The PLGA–PEG copolymer was chemically synthesized and the critical micelle concentration (CMC) of the polymer was determined, drug loaded micelles were developed by a modified solvent dialysis method. The developed system was characterized for micromeritics, surface charge, drug entrapment and morphology. Furthermore, nanocarriers were evaluated for drug-release-kinetics, erythrocyte-compatibility, in vitro cytotoxicity against MCF-7 breast cancer cells and a dermal pharmacokinetic profile. The developed system was of a spherical shape with size of 76.4 ± 2.1 nm and a neutral surface charge (−4.89 mV). The system was able to offer 60.86 ± 3.21% drug entrapment. Along with drug release controlling behaviour, the cytotoxic potential of tamoxifen against MCF-7 cell lines was substantially enhanced. Dermatokinetic studies revealed better drug availability to both the epidermis and dermis than that of the plain drug. The PLGA–PEG-based micellar system offered a safer and effective option for better delivery of tamoxifen to breast cancer with immense promise of delivery across skin.

Enhanced efficacy and a better pharmacokinetic profile of tamoxifen employing polymeric micelles

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Enhanced efficacy and a better pharmacokinetic profile of tamoxifen employing polymeric micelles