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A comprehensive mechanistic investigation of factors affecting intestinal absorption and…
Abstract
Aim
Proteolysis targeting chimeras (PROTACs) exhibit a unique and promising pharmacology. However, this comes with molecular properties exceeding the ‘drug-like’ rule of five chemical space, which often limits gastrointestinal absorption. This in vivo study aimed to investigate the…
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Electrospun Nanofiber-Scaffold-Loaded Levocetirizine Dihydrochloride Cerosomes for Combined…
Abstract
Objectives: In this study, we aimed to incorporate levocetirizine dihydrochloride (LVC) into electrospun nanovesicle-in-nanofiber (NF) scaffolds for combined management of atopic dermatitis and methicillin-resistant Staphylococcus Aureus skin infection, to sustain LVC release for…
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Development of mucoadhesive films with high polaprezinc content for oral mucositis: A study on…
Abstract
Polaprezinc (PLZ) has drawn attention to its potential to prevent oral mucositis caused by chemotherapy and radiotherapy. PLZ-containing lozenges have been developed in previous reports; however, for patients with mucositis, taking them may be challenging because of pain. Therefore, this…
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Preparation and Evaluation of Paliperidone Thermal Muco-Adhesive in Situ Gel as a Nasal to Brain…
Abstract
Background: Paliperidone PAL is a second-generation (atypical) antipsychotic medication widely used in the treatment of schizophrenia disorders. It is practically insoluble in water (class II) and has a first-pass metabolism, with oral bioavailability of about 28%.
Objective: To…
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Formulation and evaluation of HPMC and pullulan-based rapidly dissolving films containing…
Abstract
Cilnidipine is used to treat hypertension. However, it has poor solubility and undergoes extensive first-pass metabolism, which leads to poor bioavailability. This work aimed to prepare rapidly dissolving films (RDFs) containing nanosuspension of CLD with HPMC and pullulan as film-formers.…
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Design, Characterization, and Evaluation of Solid-Self-Nano-Emulsifying Drug Delivery of Benidipine…
Abstract
The main purpose of this study was to design and develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) for the oral administration of benidipine (BD) and telmisartan (TEL) using the adsorption method with eucalyptus oil, Transcutol P, and Kolliphor EL via the Box–Behnken…
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Comparative study of Hot-Melt Extrusion, spray drying, and KinetiSol® processing to formulate a…
Abstract
Fenbendazole (FBZ), a benzimidazole-carbamate anthelmintic, shows promising chemotherapeutic properties. However, it is a poorly water-soluble molecule, leading to low and variable oral bioavailability. This study investigated hot-melt extrusion (HME), spray drying, and KinetiSol…
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Design of lipid-based formulations for oral delivery of a BASP1 peptide targeting MYC-dependent…
Abstract
Hypothesis
Oral delivery of the proliferation-inhibiting brain acid-soluble protein 1 effector domain peptide (Myr-NT) towards MYC-dependent gastrointestinal tumors can be achieved by forming hydrophobic ion pairs (HIPs) and incorporating them into lipid-based formulations.…
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Formulation and In Vitro Evaluation of Matrix Tablets Containing Ketoprofen–Beta Cyclodextrin…
Abstract
Background: Rheumatoid arthritis is a chronic autoimmune disease that leads to severe disability and requires improved therapeutic strategies to optimize anti-inflammatory treatment. This study aimed to address this challenge by developing and characterizing an extended-release polymer…
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Highly Increasing Solubility of Clofazimine, an Extremely Water-insoluble Basic Drug, in Lipid-based…
Abstract
Clofazimine (CFZ) is a highly effective antibiotic against leprosy and drug-resistant tuberculosis and is on the WHO List of Essential Drugs. However, no CFZ product with optimal bioavailability is available worldwide. The manufacturer withdrew its only marketed product, presumably due to…
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