Amphiphilic dynamic covalent polymer vectors of siRNA.

Dynamic covalent polymers (DCPs) recently emerged as smart siRNA delivery vectors, which dynamically self-assemble through siRNA templating and depolymerize in a controlled manner. Herein, we report the dynamic combinatorial screening of cationic and amphiphilic peptide-based monomers. We provide experimental evidence, by mass spectrometry analyses, of the siRNA-templated formation of DCPs, and show that amphiphilic DCPs display superior activity in terms of siRNA complexation and delivery in cells.

Purification and characterization of pure curcumin, desmethoxycurcumin, and bisdemethoxycurcumin from North-East India Lakadong turmeric (Curcuma longa).

Lakadong turmeric has been outlined for its high content of curcuminoids across the globe. Three significant molecular markers are widely present in turmeric viz, curcumin, desmethoxycurcumin, and bisdemethoxycurcumin, and they are present very high amount in Lakadong turmeric. Curcuminoids have been reported for structural and spectrum similarity of 3 to 4 nm (432, 434, and 436 nm, respectively).

Amoxapine-Loaded Solid Lipid Nanoparticles with Superior Preclinical Pharmacokinetics for Better Brain Delivery: LC-MS/MS and GC-MS Analysis.

The tricyclic antidepressant amoxapine (AMX) has been reported for a rapid onset of action compared to other cyclic antidepressants. It has very low solubility and bioavailability due to first-pass metabolism. Therefore, we planned to develop solid lipid nanoparticles (SLNs) of AMX using a single emulsification method to increase its solubility and bioavailability.

Preparation and characterization of amoxapine- and naringin-loaded solid lipid nanoparticles: drug-release and molecular-docking studies.

Amoxapine (AMX) has been reported to be metabolized by CYP3A4 and CYP2D6. Naringin (NG) has been reported to inhibit CYP enzymes. Therefore, the current work was designed to develop AMX solid lipid nanoparticles (AMX-SLNs) and NG-SLNs for better therapeutic performance.

Development and validation of HPLC method for simultaneous estimation of erlotinib and niclosamide from liposomes optimized by screening design.

The emerging drug resistance to the approved first-line drug therapy leads to clinical failure in cancer. Drug repurposing studies lead to the identification of many old drugs to be used for cancer treatment. Combining the repurposed drugs (niclosamide) with first-line therapy agents like erlotinib HCl showed improved efficacy by inhibiting erlotinib HCl acquired resistance.

Process development for the total synthesis of the novel drug metabolite Carboxy toremifene as a standard reference material along with characterization and purity assessment for the Antidoping quality Control Purposes.

Tamoxifen and toremifene are two selective estrogen receptor modulators (SERMs) commonly used to treat breast cancer in women. Toremifene is well-known as a triphenylethylene derivative. Carboxy toremifene is a common metabolite of toremifene and tamoxifen.

Simultaneous Method Development and Validation of Anastrozole Along with Piperine: Degradation Studies and Degradants Characterization Using LC-QTOF-ESI-MS Along with In-silico ADMET Predictions.

Background: Anastrozole (ATZ) is a selective non-steroidal inhibitor widely used for the treatment of breast cancer in post-menopausal women. ATZ exerts its biological activity by inhibiting the enzyme aromatase, which is responsible for converting androgens to estrogens. Piperine (PIP), a natural alkaloid and the main component of black pepper, is used as a bioenhancer and for combating a variety of health issues ranging from upset stomach to dental problems.

Synthesis, characterization, method development, and validation of nor-ethylmorphine hydrochloride reference material using established analytical techniques for dope control analysis.

Ethylmorphine is permitted internationally for therapeutic purposes where morphine is not indicated across the globe. Nor-ethylmorphine a major metabolite of ethylmorphine. To differentiate the intake of morphine from ethylmorphine, nor-ethylmorphine stable reference material is desirable.

Analytical developments of p-hydroxy prenylamine reference material for dope control research: Characterization and purity assessment.

Prenylamine was initially used for the treatment of angina pectoris and later on withdrawn from the market in 1988 due to cardiac arrhythmias concern. The major phase I metabolite of prenylamine is p-hydroxy prenylamine that has a chiral center in the structure. Even though p-hydroxy prenylamine was synthesized earlier, it lacked complete analytical developments for chiral high-performance liquid chromatography (HPLC) separation.