A novel scaffold long-acting selective estrogen receptor antagonist and degrader with superior preclinical profile against ER+ breast cancer.

Breast cancer is one of the most common malignant tumors in women worldwide, with the majority of cases showing expression of estrogen receptors (ERs). Although drugs targeting ER have significantly improved survival rates in ER-positive patients, drug resistance remains an unmet clinical need. Fulvestrant, which overcomes selective estrogen receptor modulator (SERM) and AI (aromatase inhibitor) resistance, is currently the only long-acting selective estrogen receptor degrader (SERD) approved for both first and second-line settings.

The preparation and characterisation of tasteless core-shell clarithromycin microcapsules.

This study aims to fabricate core-shell clarithromycin (CAM) microcapsules to cover up the bitter taste of CAM by spray drying with aqueous polymer dispersion. Water dispersion of Eudragit EPO and Surelease were innovatively used to encapsulate CAM into microcapsules via a one-step spray-drying method. The inlet air temperature, airflow rate, CAM-polymer ratio, and particle size of CAM were optimised based on drug content and T (the time taken for the drug to release equal to 6% /).

Characterization of nimodipine amorphous nanopowder prepared by quenching cooling combined with wet milling and spray drying.

Currently, reducing particle size or preparing drugs into amorphous forms are widely used methods to improve the solubility and dissolution rate of insoluble drugs. The purpose of this study was to prepare nimodipine amorphous nanopowder (NMD-NAP) using nimodipine (NMD) as a model drug to increase the solubility and dissolution rate of insoluble drugs by the combined effect of reducing the particle size and preparing the drug into an amorphous form. The NMD-NAP was successfully prepared by quenching cooling combined with wet milling and spray drying.

Utility of apparent diffusion coefficient histogram analysis in differentiating benign and malignant palate lesions.

Objectives: To explore the ability of conventional MRI and histogram analysis of apparent diffusion coefficient (ADC) for differentiating between malignant and benign palatal lesions.

Materials And Methods: A retrospective analysis was performed on MRI images of 86 patients with palatal lesions confirmed by histopathology between January 2015 and December 2018. Each lesion was evaluated based on the conventional MRI characteristics, including size, location, morphology, inner texture, enhancement, capsule, bone destruction, and nerve invasion.

A c-MET-Targeted Topical Fluorescent Probe cMBP-ICG Improves Oral Squamous Cell Carcinoma Detection in Humans.

Introduction: The postoperative survival of oral squamous cell carcinoma (SCC) relies on precise detection and complete resection of original tumors. The mucosal extension of the tumor is evaluated visually during surgery, but small and flat foci are difficult to detect. Real-time fluorescence imaging may improve detection of tumor margins.

Resources allocation optimization algorithm based on the comprehensive utility in edge computing applications.

In the mobile edge computing environment, aiming at the problems of few classifications of resource nodes and low resource utilization in the process of multi-user and multi-server resource allocation, a resource optimization algorithm based on comprehensive utility is proposed. First, the algorithm improves the Naive Bayes algorithm, obtains the conditional probabilities of job types based on the established Naive Bayes formula and calculates the posterior probabilities of different job types under specific conditions. Second, the classification method of resource service nodes is designed.

Dynamic computation offloading algorithm based on particle swarm optimization with a mutation operator in multi-access edge computing.

The current computation offloading algorithm for the mobile cloud ignores the selection of offloading opportunities and does not consider the uninstall frequency, resource waste, and energy efficiency reduction of the user's offloading success probability. Therefore, in this study, a dynamic computation offloading algorithm based on particle swarm optimization with a mutation operator in a multi-access edge computing environment is proposed (DCO-PSOMO). According to the CPU utilization and the memory utilization rate of the mobile terminal, this method can dynamically obtain the overload time by using a strong, locally weighted regression method.

Rod-shaped nintedanib nanocrystals improved oral bioavailability through multiple intestinal absorption pathways.

Nintedanib (BIBF) is a biopharmaceutical classification system II (BCS II) drug that has a good therapeutic effect for the treatment of nonsmall cell lung cancer; however, it shows poor oral bioavailability due to low dissolution and intestinal absorption. This study aims to fabricate rod-shaped nanocrystals to enhance oral bioavailability by improving the dissolution and absorption of BIBF in the intestine. By prescription screening, BIBF nanocrystals (BIBF-NCs) with a particle size of 325.

A Novel Eyes Topical Drug Delivery System: CsA-LNC for the Treatment of DED.

Purpose: The objective of the present work was to prepare safe and effective Ciclosporin A Lipid nanocapsule (CsA-LNC) eye-drops for the treatment of DED.

Methods: The phase-inversion method was used to prepared different sizes CsA-LNC. CsA biodistribution in ocular after topical administration in rabbits was analyzed by a validated UPLC-MS/MS method.

Nanostructured lipid carriers as oral delivery systems for improving oral bioavailability of nintedanib by promoting intestinal absorption.

The aim of this study was to fabricate nanostructured lipid carriers, NLCs, of nintedanib (BIBF) to improve its oral bioavailability. Two types of NLCs loaded with BIBF (BIBF-NLCs-1 and BIBF-NLCs-2) were prepared by the melt-emulsification technique. BIBF-NLCs-1 and BIBF-NLCs-2 showed nanoscale particle sizes of 142.