Objective of the present investigation was to enhance the bioavailability of felodipine by targeting the M cells of Peyer's patches using PLGA nanoparticles (NPs). Felodipine exhibits poor bioavailability due to limited aqueous solubility and extensive first pass metabolism. NPs were prepared using nanoprecipitation and optimized by 3(2) factorial design. Particle size (PS) and entrapment efficiency (% EE) were dependent on Drug/PLGA ratio (X1) and Pluronic F-68 (X2) concentration. % EE, PS and Zeta potential for optimized batch were 91.56±3.21%, 161.3±2.23 nm and -25.7±2.52 mV respectively. DSC, XRD and FTIR studies confirmed compatibility of PLGA and drug. TEM image confirmed the spherical shape. The in vitro and ex vivo studies using rat stomach and intestinal segment confirmed sustained release from NPs. Pharmacodynamic studies in rats showed control of blood pressure and ECG changes for extended duration. Hence, NPs can be a suitable alternative to the current available therapy in hypertension and angina by enhancing the bioavailability.
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http://dx.doi.org/10.1016/j.msec.2013.10.038 | DOI Listing |
Int J Pharm
January 2025
Department of Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China; Hubei Province Clinical Research Center for Precision Medicine for Critical Illness, Wuhan, 430022, China. Electronic address:
Cancer associated fibroblasts (CAFs) are one of the most important stromal cells in the tumor microenvironment, playing a pivotal role in the development, recurrence, metastasis, and immunosuppression of cancer and treatment resistance. Here, we developed a core-shell biomimetic nanosystem termed as FAP-C NPs. This system was comprised of 4 T1 extracellular vesicles fused with a FAP single-chain antibody fragment to form the biomimetic shell, and PLGA nanoparticles loaded with calcipotriol as the core.
View Article and Find Full Text PDFBackground: About half of the patients suffering from Alzheimer's disease (AD) display sleeping disorders. Disruptions in the central circadian clock (CC), located in the brain, accelerate AD pathogenesis, making the CC a promising target. In preclinical trials, this strategy have shown efficacy but clinical results are inconsistent.
View Article and Find Full Text PDFBMC Cancer
January 2025
Department of Cellular and Molecular Biology, Lahijan Branch, Islamic Azad University, Lahijan, Iran.
Background/aims: Gastric cancer (GC) is a significant global health issue with high incidence rates and poor prognoses, ranking among the top prevalent cancers worldwide. Due to undesirable side effects and drug resistance, there is a pressing need for the development of novel therapeutic strategies. Understanding the interconnectedness of the JAK2/STAT3/mTOR/PI3K pathway in tumorigenesis and the role of Astaxanthin (ASX), a red ketocarotenoid member of xanthophylls and potent antioxidant and anti-tumor activity, can be effective for cancer treatments.
View Article and Find Full Text PDFChemMedChem
January 2025
Institute of Himalayan Bioresource Technology CSIR, Dietetics & Nutrition Technology Division, Palampur, 176061, Palampur, INDIA.
Gemcitabine (GEM), a chemotherapeutic agent, is widely utilized in treating various neoplasm conditions, such as pancreatic, lung, breast, and ovarian cancers. However, its therapeutic effectiveness is often hindered by its hydrophilic nature, short half-life and susceptibility to enzymatic degradation. To address these limitations, in this research, five new prodrugs of GEM were synthesized by conjugating its N-4 amino group with five different acids [4-decenoic acid (4Dec), lipoic acid (Lipo), lauric acid (Laur), 5-benzyl N-(tert-butoxycarbonyl)- L-glutamate (Glu), and decanoic acid (Dec)].
View Article and Find Full Text PDFPharmaceutics
November 2024
Guangdong Provincial Key Laboratory of Advanced Drug Delivery, Guangdong Provincial Engineering Center of Topical Precise Drug Delivery System, Guangdong Pharmaceutical University, No. 280 University Town Outer Ring East Road, Guangzhou 510006, China.
Background: Internal ocular diseases, such as macular edema, uveitis, and diabetic macular edema require precise delivery of therapeutic agents to specific regions within the eye. However, the eye's complex anatomical structure and physiological barriers present significant challenges to drug penetration and distribution. Traditional eye drops suffer from low bioavailability primarily due to rapid clearance mechanisms.
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