European Journal of Pharmaceutical Sciences This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

Altering distribution profile of palbociclib by its prodrugs
Eur J Pharm Sci. 2023 Nov 13:106637. doi: 10.1016/j.ejps.2023.106637. Online ahead of print.ABSTRACTPalbociclib, a cyclin-dependent kinase (CDK) 4/6 inhibitor, is currently used clinically for treating hormone receptor-positive and human epidermal growth factor receptor 2 negative breast cancer. Additionally, it has the potential to be utilized in the treatment of various tumors, including malignant glioblastoma. Previous research has indicated that palbociclib is a substrate for two efflux transporters, P-glycoprotein (P-gp; MDR1) and breast cancer-resistant protein (BCRP), which restrict the brain exposure of palbociclib...
Source: European Journal of Pharmaceutical Sciences - November 15, 2023 Category: Drugs & Pharmacology Authors: Juulia J ärvinen Ahmed B Montaser Santosh Kumar Adla Jukka Lepp änen Marko Lehtonen Kati-Sisko Vellonen Tuomo Laitinen Aaro Jalkanen William F Elmquist Juri Timonen Kristiina M Huttunen Jarkko Rautio Source Type: research

Nanostructured lipid carriers loaded into in situ gels for breast cancer local treatment
In conclusion, these results contribute to improving our understanding of nanocarrier design with increased cytotoxicity and prolonged retention for the intraductal route. Tributyrin incorporation increased the cytotoxicity of paclitaxel and 5-fluorouracil in monolayer and spheroids, while NLC incorporation in thermosensitive gels prolonged tissue retention of both hydrophilic and hydrophobic compounds.PMID:37967657 | DOI:10.1016/j.ejps.2023.106638 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - November 15, 2023 Category: Drugs & Pharmacology Authors: Julia S Passos Alexsandra C Apolinario Kelly Ishida Tereza S Martins Luciana B Lopes Source Type: research

Analysis of Stabilization Mechanisms in β-Lactoglobulin-based Amorphous Solid Dispersions by Experimental and Computational Approaches
Eur J Pharm Sci. 2023 Nov 13:106639. doi: 10.1016/j.ejps.2023.106639. Online ahead of print.ABSTRACTOur previous work shows that β-lactoglobulin-stabilized amorphous solid dispersion (ASD) loaded with 70% indomethacin remains stable for more than 12 months. The stability is probably due to hydrogen bond networks spread throughout the ASD, facilitated by the indomethacin which has both hydrogen donors and acceptors. To investigate the stabilization mechanisms further, here we tested five other drug molecules, including two without any hydrogen bond donors. A combination of experimental techniques (differential scanning cal...
Source: European Journal of Pharmaceutical Sciences - November 15, 2023 Category: Drugs & Pharmacology Authors: Xuezhi Zhuo Vito Foder à Per Larsson Zarah Schaal Christel A S Bergstr öm Korbinian L öbmann Aleksei Kabedev Source Type: research

Topical delivery of seriniquinone for treatment of skin cancer and fungal infections is enabled by a liquid crystalline lamellar phase
Eur J Pharm Sci. 2023 Nov 10:106635. doi: 10.1016/j.ejps.2023.106635. Online ahead of print.ABSTRACTSeriniquinone (SQ) was initially described by our group as an antimelanoma drug candidate and now also as an antifungal drug candidate. Despite its promising in vitro effects, SQ translation has been hindered by poor water-solubility. In this paper, we described the challenging nanoformulation process of SQ, which culminated in the selection of a phosphatidylcholine-based lamellar phase (PLP1). Liposomes and nanostructured lipid carriers were also evaluated but failed to encapsulate the compound. SQ-loaded PLP1 (PLP1-SQ) was...
Source: European Journal of Pharmaceutical Sciences - November 12, 2023 Category: Drugs & Pharmacology Authors: Rodrigo Dos A Miguel Amanda S Hirata Giovanna C Salata Alexsandra C Apolin ário Vinicius M Barroso Kelly Ishida James J La Clair William Fenical Tereza S Martins Leticia V Costa-Lotufo Luciana B Lopes Source Type: research

Digestion is a critical element for absorption of cinnarizine from supersaturated lipid-based type I formulations
Eur J Pharm Sci. 2023 Nov 9:106634. doi: 10.1016/j.ejps.2023.106634. Online ahead of print.ABSTRACTEnabling formulations, such as lipid-based formulations (LBFs), are means to deliver challenging-to-formulate, poorly soluble drugs. LBFs may be composed of lipids, surfactants and/or cosolvents and can be classified depending on the proportions of the components and the hydrophilicity of the surfactant according to the Lipid Formulations Classification System, ranging from type I (very lipophilic) to type IV (hydrophilic). In cases where drug solubility in LBFs does not suffice, e.g. for preclinical toxicity studies, supersa...
Source: European Journal of Pharmaceutical Sciences - November 11, 2023 Category: Drugs & Pharmacology Authors: Felix Paulus Annette Bauer-Brandl Jef Stappaerts Ren é Holm Source Type: research

Preparation of Polycaprolactone and Polymethacrylate Nanofibers for Controlled Ocular Delivery of Ketorolac tromethamine: Pharmacokinetic study in Rabbit's Eye
Eur J Pharm Sci. 2023 Nov 9:106631. doi: 10.1016/j.ejps.2023.106631. Online ahead of print.ABSTRACTOphthalmitis is an inflammation of the eye triggered by various conditions including diseases, allergy, trauma, or surgery. Management of this condition usually includes administration of topical anti-inflammatory eye drops such as nonsteroidal anti-inflammatory drugs. To overcome the challenges of conventional eye drops such as frequent administration and low intraocular bioavailability, nanofibrous inserts of Ketorolac tromethamine (KET) were developed in this study. Polycaprolactone and polymethacrylate containing KET were...
Source: European Journal of Pharmaceutical Sciences - November 11, 2023 Category: Drugs & Pharmacology Authors: Shiva Taghe Shahla Mirzaeei Masood Bagheri Source Type: research

A robust analytical method for simultaneous quantification of 13 low-molecular-weight N-Nitrosamines in various pharmaceuticals based on solid phase extraction and liquid chromatography coupled to high-resolution mass spectrometry
Eur J Pharm Sci. 2023 Nov 9:106633. doi: 10.1016/j.ejps.2023.106633. Online ahead of print.ABSTRACTRecently, the potentially highly carcinogenic N-nitrosamines (NAs) have become the focus of pharmaceutical regulatory authorities, the pharmaceutical industry and researchers because trace amounts have been detected in some drug products (DPs), resulting in drug supply shortages. In the absence of sufficient analytical methods for the determination of multiple regulated low-molecular-weight NAs in various DPs, a robust, selective, sensitive and accurate method based on sample preparation by solid-phase extraction, followed by...
Source: European Journal of Pharmaceutical Sciences - November 11, 2023 Category: Drugs & Pharmacology Authors: Timeja Planin šek Parfant Taja Skube Robert Ro škar Source Type: research

The overview of development of novel bacterial topoisomerase inhibitors effective against multidrug-resistant bacteria in an academic environment: from early hits to in vivo active antibacterials
This article reviews our efforts in developing highly potent NBTIs over the past decade. Following the discovery of an initial hit with potent enzyme inhibitory and broad-spectrum antibacterial activity, an extensive hit-to-lead campaign was conducted with the goal of optimizing physicochemical properties, reducing hERG inhibition, and maintaining antibacterial activity against both Gram-positive and Gram-negative bacteria, with a focus on methicillin-resistant Staphylococcus aureus (MRSA). This optimization strategy resulted in an amide-containing, focused NBTI library with compounds exhibiting potent antibacterial activi...
Source: European Journal of Pharmaceutical Sciences - November 10, 2023 Category: Drugs & Pharmacology Authors: Ma ša Zorman Martina Hrast Maja Kokot Nikola Minovski Marko Anderluh Source Type: research

A Comprehensive Review of Advanced Nasal Delivery: Specially Insulin and Calcitonin
Eur J Pharm Sci. 2023 Nov 8:106630. doi: 10.1016/j.ejps.2023.106630. Online ahead of print.ABSTRACTPeptide drugs through nasal mucous membrane, such as insulin and calcitonin have been widely used in the medical field. There are always two sides to a coin. One side, intranasal drug delivery can imitate the secretion pattern in human body, having advantages of physiological structure and convenient use. Another side, the low permeability of nasal mucosa, protease environment and clearance effect of nasal cilia hinder the intranasal absorption of peptide drugs. Researchers have taken multiple means to achieve faster therapeu...
Source: European Journal of Pharmaceutical Sciences - November 10, 2023 Category: Drugs & Pharmacology Authors: Dan Luo Xiaoqing Ni Hao Yang Lu Feng Zhaoqun Chen Lan Bai Source Type: research

Novel nanomicelle butenafine formulation for ocular drug delivery against fungal keratitis: In Vitro and In Vivo study
Eur J Pharm Sci. 2023 Nov 2;192:106629. doi: 10.1016/j.ejps.2023.106629. Online ahead of print.ABSTRACTFungal keratitis (FK) is a serious infectious corneal disease that leads to blindness. Butenafine (BTF) is an allylamine drug with high antifungal activity, but its poor water solubility and low bioavailability limit its clinical application in ophthalmology. To increase its aqueous solubility and corneal permeability, butenafine was encapsulated in d-ɑ-tocopheryl polyethylene glycol succinate (TPGS) polymeric nanomicelles to improve the bioavailability of the drug for the treatment of FK. Butenafine was successfully fab...
Source: European Journal of Pharmaceutical Sciences - November 2, 2023 Category: Drugs & Pharmacology Authors: Ping Lu Zhen Liang Zhen Zhang Jingjing Yang Fei Song Tianyang Zhou Jingguo Li Junjie Zhang Source Type: research