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Enhanced oral delivery and anti-gastroesophageal reflux activity of curcumin by binary mixed micelles.

The aim of this study was to improve the solubility, oral bioavailability, and anti-gastroesophageal reflux activity of curcumin (CM) by preparing two CM-loaded, novel, binary mixed micelles (CM-M). The two CM-M were prepared by ethanol thin-film hydration method. One (CM-T) was prepared using D-alpha-tocopheryl polyethylene glycol 1000 succinate and Solutol®HS15, and the other (CM-F) was prepared using Pluronic®F127 and Solutol®HS15. The entrapment efficiency and drug loading of CM-T were 83.61 ± 0.54% and 2.20 ± 0.65%, respectively, which were lower than those of CM-F (88.66 ± 0.12% and 1.47

Effect of hemostatic material on sternal healing after cardiac surgery.

BACKGROUND: Postoperative sternal infection and dehiscence cause increased morbidity, mortality, and socioeconomic costs as well as patient discomfort and pain. Some predisposing factors have been uncovered but others remain uninvestigated. Among these are the influence of topical hemostatic agents such as bone wax (BW) and Ostene (Ceremed Inc, Los Angeles, CA) a new, water-soluble polymer wax (WSW). The object of this study was to investigate the impact of topical hemostatic agents on sternal healing in patients. METHODS: In total, 50 patients subjected to elective cardiac surgery and requir

Enhancement of cellular uptake and cytotoxicity of curcumin-loaded PLGA nanoparticles by conjugation with anti-P-glycoprotein in drug resistance cancer cells.

AIM: To compare the anti-cancer activity and cellular uptake of curcumin (Cur) delivered by targeted and non-targeted drug delivery systems in multidrug-resistant cervical cancer cells. METHODS: Cur was entrapped into poly (DL-lactide-co-glycolide) (PLGA) nanoparticles (Cur-NPs) in the presence of modified-pluronic F127 stabilizer using nano-precipitation technique. On the surface of Cur-NPs, the carboxy-terminal of modified pluronic F127 was conjugated to the amino-terminal of anti-P-glycoprotein (P-gp) (Cur-NPs-APgp). The physical properties of the Cur-NPs, including particle size, zeta pot

A novel reverse thermosensitive polymer to achieve temporary atraumatic vessel occlusion in infra-popliteal bypasses.

OBJECTIVE: The study aims to assess a novel thermosensitive polymer (LeGoo(®)) for distal vessel control during infra-popliteal (crural/pedal) bypass surgery in severe leg ischaemia. METHOD: Retrospective analysis of all distal bypasses from October 2009 to February 2012. Technical success, patency, limb salvage and amputation-free survival rates were analysed. RESULTS: Fifty-four infra-popliteal bypasses using the polymer were performed in 46 patients. The distal anastomosis was at the anterior tibial (n = 15, 28%), posterior tibial (n = 12, 22%), peroneal (n = 8, 15%), tibio-peroneal trunk

Influence of microencapsulation method and peptide loading on formulation of poly(lactide-co-glycolide) insulin nanoparticles.

Insulin stability during microencapsulation and subsequent release is essential for retaining its biological activity. Therefore we investigated a novel solid/oil/water anhydrous encapsulation method with a combination of stabilizers for maintaining the integrity of insulin during formulation and delivery. Two methods were used for preparation of nanoparticles, namely water/oil/water solvent evaporation and s/o/w anhydrous encapsulation to study the influence of the microencapsulation method on nanoparticle characteristics such as size and morphology, drug content, encapsulation efficiency, an

Гибридные нанопчасти на основе гиалюронной кислоты в качестве перспективных перевозчиков Интранасальной администрации диметилФумарата.

ПППОСА: Диметилфумарат (ДМФ) - пероральная терапия с релапсирующим множественным склерозом, быстро метаболизируется в монометилфумарат. Оральное управление DMF вызывает желудочно-кишечный дискомфорт, вызывая вынос лечения. Цель настоящего исследования заключается в разработке новаторской формулировки для управления носовым слоем ДМФ. Гибридные наночастицы (LPN) липидового полимера были разработаны для повышения устойчивости DMF, ограничения побочных эффектов желудочно-кишечного кишечника и увеличения биодоступности головного мозга за счет нацеливания нос на мозг.МЕТОДЫ: С помощью методов магни

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… These were produced by nanoprecipitation magnetic/mechanical stirring technique using phosphatidylcholine (CP), palmitoylethanolamide (PEA), cholesterol (Chol), poloxamers (P), and optionally hyaluronic acid (HA), with selected concentration. … Bioadhesive behavior of poloxamer/hyaluronic acid-based formulations analyzed by rheology method . Sci Talks . 2022 ; 4 : 100072 . doi: 10.1016/j.sctalk.2022.100072 63. Di Cagno M , Luppi B . …

The efficacy and safety of bufadienolides-loaded nanostructured lipid carriers.

Bufadienolides-loaded nanostructured lipid carriers (BU-NLC) were prepared for parenteral application using glyceryl monostearate as solid core, medium-chain triglyceride and oleic acid as liquid lipid material, and Lipoid E-80, sodium deoxycholate and pluronic F68 as stabilizers. In this study, the in vitro cytotoxicity, pharmacokinetics, biodistribution, antitumor efficacy and safety of BU-NLC were evaluated. Against human astrocytoma cell line (U87-MG) and human gastric carcinoma cell line (HGC-27) BU-NLC exhibited cytotoxicity that was similar to that of the free drug, and superior to that

Comparison of different methods for preparation of a stable riccardin D formulation via nano-technology.

Riccardin D is a new compound extracted from liverwort Marchantia polymorpha L. It has been proved to be useful in antifungal therapy and reversing the resistance of Candida albicans against fluconazole. However, the poor solubility leads to the poor bioavailability and limits its development. In this study, nanocrystals were prepared in the evaporative precipitation into aqueous solution (EPAS) and the microfluidisation process. The characterizations of nanocrystals were compared by transmission electron microscope, size distribution, and zeta potential. In the EPAS method, the drug was disso

Investigation of the micellar effect of pluronic P85 on P-glycoprotein inhibition: cell accumulation and equilibrium dialysis studies.

The objective of this study was: (1) to characterize the P-gp inhibitory effect of different concentrations of Pluronic P85 on anti-HIV-1 drug cellular accumulation, and (2) to investigate the relationship between cellular accumulation and free fraction of drug. Cellular accumulation studies in MDCKII-WT and MDCKII-MDR1 cell monolayers showed a biphasic dose response characterized by decline in accumulation at Pluronic concentrations greater than the CMC. This phenomenon was independent of the inhibition of P-gp efflux by Pluronic. Cell-free equilibrium dialysis was used to determine the effec

Resveratrol Nanoformulations for Cancer Management: A Comprehensive Review of Disease-Specific Strategies and Clinical Translational Barriers.

Cancer remains a leading cause of mortality worldwide, highlighting the need for therapeutic strategies that reduce systemic toxicity and drug resistance. Resveratrol (RES), a natural polyphenolic stilbenoid, possesses antioxidant, anti-inflammatory, pro-apoptotic, anti-metastatic, and chemosensitizing activities. However, its clinical translation is limited by poor aqueous solubility, chemical instability, rapid metabolic clearance, and consequently low systemic bioavailability. Nanotechnology-based drug delivery systems provide a promising strategy to address these limitations. This review s

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… A key advantage of specific micellar systems—notably those incorporating poloxamers or TPGS—lies in their intrinsic capacity to inhibit the P-gp efflux pump, thereby counteracting MDR prevalent in advanced CRC. 147 Polymeric micelles based on poloxamer block copolymers offer a multifunctional delivery … In an illustrative formulation, Radeva et al 149 developed poloxamer 407/poloxamer 403 mixed micelles (1:1 w/w) co-loaded with doxorubicin and resveratrol via film hydration, achieving a hydrodynamic diameter of approximately 26 nm with encapsulation efficiencies of 83.4% (doxorubicin, sequestered in …

The Evolving Pharmacotherapeutic Landscape for the Treatment of Sickle Cell Disease.

Sickle cell disease (SCD) is an extremely heterogeneous disease that has been associated with global morbidity and early mortality. More effective and inexpensive therapies are needed. During the last five years, the landscape of the pharmacotherapy of SCD has changed dramatically. Currently, 54 drugs have been used or under consideration to use for the treatment of SCD. These fall into 3 categories: the first category includes the four drugs (Hydroxyurea, L-Glutamine, Crizanlizumab tmca and Voxelotor) that have been approved by the United States Food and Drug Administration (FDA) based on suc

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… 188 for treatment of acute vaso-occlusive crisis of sickle cell disease: A randomized controlled trial JAMA 2001 286 17 2099 106 10.1001/jama.286.17.2099 11694150 13 Ballas SK Files B Luchtman-Jones L Benjamin L Swerdlow P Hilliard L Safety of purified poloxamer 188 in sickle cell disease: phase I … study of a non-ionic surfactant in the management of acute chest syndrome Hemoglobin 2004 28 2 85 102 10.1081/HEM-120035919 15182051 14 Mast Therapeutics Inc Phase III Randomized Study of Poloxamer 188 for Vaso-Occlusive Crisis of Sickle Cell Disease ( NCT00004408 ) ClinicalTrials.gov [Available from …

Gambogic Acid as a Candidate for Cancer Therapy: A Review.

Gambogic acid (GA), a kind of dry resin secreted by the Garcinia hanburyi tree, is a natural active ingredient with various biological activities, such as anti-cancer, anti-inflammatory, antioxidant, anti-bacterial effects, etc. An increasing amount of evidence indicates that GA has obvious anti-cancer effects via various molecular mechanisms, including the induction of apoptosis, autophagy, cell cycle arrest and the inhibition of invasion, metastasis, angiogenesis. In order to improve the efficacy in cancer treatment, nanometer drug delivery systems have been employed to load GA and form mice

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… Mixed micelles self-assembled from two or more dissimilar block copolymers provide a direct and convenient approach to increase micelle stability and drug-loading efficiency, superior to those of the individual components. 88 GA was encapsulated in the mixed micelles constituted of Poloxamer 407 and … Poloxamer 407/TPGS mixed micelles for delivery of gambogic acid to breast and multidrug-resistant cancer. Int J Nanomed . 2012;7:713–721. 90. Yu F, Jiang FG, Tang XH, Wang BC. …

Recent Advances in Doxorubicin Formulation to Enhance Pharmacokinetics and Tumor Targeting.

Doxorubicin (DOX), a widely used drug in cancer chemotherapy, induces cell death via multiple intracellular interactions, generating reactive oxygen species and DNA-adducted configurations that induce apoptosis, topoisomerase II inhibition, and histone eviction. Despite its wide therapeutic efficacy in solid tumors, DOX often induces drug resistance and cardiotoxicity. It shows limited intestinal absorption because of low paracellular permeability and P-glycoprotein (P-gp)-mediated efflux. We reviewed various parenteral DOX formulations, such as liposomes, polymeric micelles, polymeric nanopar

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… The engulfed Tf–DOX–PLGA nanoparticles release DOX and poloxamer into the cells. … Poloxamer has been reported to have multiple functions in P-gp overexpressed cells, such as inhibiting P-gp and depleting ATP in mitochondria, resulting in ROS generation and cytochrome c release, which lead to apoptosis [ 80 ]. …

Plant-Derived Natural Products in Cancer Research: Extraction, Mechanism of Action, and Drug Formulation.

Cancer is one of the main causes of death globally and considered as a major challenge for the public health system. The high toxicity and the lack of selectivity of conventional anticancer therapies make the search for alternative treatments a priority. In this review, we describe the main plant-derived natural products used as anticancer agents. Natural sources, extraction methods, anticancer mechanisms, clinical studies, and pharmaceutical formulation are discussed in this review. Studies covered by this review should provide a solid foundation for researchers and physicians to enhance basi

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… RES Nanocores and Nanocapsules Nanocores of RES using polyvinylpyrrolidone 17 PF (PVP K17) as the stabilizer and poloxamer 188 (F188) as the surfactant were developed by Hao and co-workers [ 483 ].RES nanocapsules containing RES nanocores coated with multilayered polyelectrolyte shells showed enhanced …

An Overview of Polymeric Nanoparticles-Based Drug Delivery System in Cancer Treatment.

Cancer is recognized as one of the world's deadliest diseases, with more than 10 million new cases each year. Over the past 2 decades, several studies have been performed on cancer to pursue solutions for effective treatment. One of the vital benefits of utilizing nanoparticles (NPs) in cancer treatment is their high adaptability for modification and amalgamation of different physicochemical properties to boost their anti-cancer activity. Various nanomaterials have been designed as nanocarriers attributing nontoxic and biocompatible drug delivery systems with improved bioactivity. The present

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… In addition, poloxamer-type block copolymer can be used to modify nanocarriers’ surfaces. One of the products available in the market is a micellar formulation Genexol-PM comprised of PEG-based block copolymer. 18 Active targeting Strategies for passive targeting have several drawbacks. … 407; P123, Poloxamer P123; Tf, Transferrin. …

Curcumin and Its Derivatives as Anticancer Agents in Head and Neck Cancer: Molecular Mechanisms and Preclinical Evidence

Head and neck cancer (HNC), particularly oral squamous cell carcinoma (OSCC), remains a major clinical challenge due to its aggressive behavior, high recurrence rates, and frequent resistance to conventional therapies. Natural compounds, especially curcumin and its derivatives, have gained increasing attention as potential anticancer agents due to their ability to target multiple molecular pathways involved in tumor progression. This review critically evaluates the current preclinical and translational evidence supporting curcumin and its derivatives as monotherapeutic agents in HNC, with part

Biopharmaceutical and pharmacokinetic attributes to drive nanoformulations of small molecule tyrosine kinase inhibitors.

Buoyed by the discovery of small-molecule tyrosine kinase inhibitors (smTKIs), significant impact has been made in cancer chemotherapeutics. However, some of these agents still encounter off-target toxicities and suboptimal efficacies due to their inferior biopharmaceutical and/or pharmacokinetic properties. Almost all of these molecules exhibit significant inter- and intra-patient variations in plasma concentration-time profiles. Thus, therapeutic drug monitoring, dose adjustments and precision medicine are being contemplated by clinicians. Complex formulations or nanoformulation-based drug d

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… . | [86] Apatinib (APA) | NPs: APA loaded in Poloxamer 407 and PLGA NPs | Tumor volume reduction by more than two-fold was achieved. | [87] Liposome: Lecithin, cholesterol and PEG-DSPE polymer were used to develop an APA-containing PEG-modified liposome. | The quantity of tumor nodules and tumor weight … APA was encapsulated in PLGA and Poloxamer 407 NPs (APA/p NPs) by Zhang et al. [87] to enhance the effectiveness in treating melanoma. B16 cells were employed to investigate in vitro efficacy. On tumor B16 cells, APA/p NPs had a greater level of cytotoxicity than the free drug solution. …

How to Treat Melanoma? The Current Status of Innovative Nanotechnological Strategies and the Role of Minimally Invasive Approaches like PTT and PDT.

Melanoma is the most aggressive type of skin cancer, the incidence and mortality of which are increasing worldwide. Its extensive degree of heterogeneity has limited its response to existing therapies. For many years the therapeutic strategies were limited to surgery, radiotherapy, and chemotherapy. Fortunately, advances in knowledge have allowed the development of new therapeutic strategies. Despite the undoubted progress, alternative therapies are still under research. In this context, nanotechnology is also positioned as a strong and promising tool to develop nanosystems that act as drug ca

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… . | [ 113 ] Compritol 888, poloxamer 188 and tween 80 | Curcumin and resveratrol | In vitro: murine B16F10 and human SK-MEL-28 cell lines | Cell viability assay: MTT (0.1 to 60 μg/mL of curcumin and 0.03 to 20 μg/mL of resveratrol) Cell proliferation assays: IncuCyte (same concentrations of MTT) and … Zhang et al. [ 152 ] developed a formulation of polymeric NPs composed of PLGA and poloxamer 407 for the controlled release of apatinib (Apa-PLGA NPs). …

Involvement of Resveratrol against Brain Cancer: A Combination Strategy with a Pharmaceutical Approach.

A brain tumor (BT) is a condition in which there is growth or uncontrolled development of the brain cells, which usually goes unrecognized or is diagnosed at the later stages. Since the mechanism behind BT is not clear, and the various physiological conditions are difficult to diagnose, the success rate of BT is not very high. This is the central issue faced during drug development and clinical trials with almost all types of neurodegenerative disorders. In the first part of this review, we focus on the concept of brain tumors, their barriers, and the types of delivery possible to target the b

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… Polysorbate-coated particles were shown to boost CNS pharmacological effects, but Poloxamer coatings were ineffective. Brain-targeted, Poloxamer stabilized stearic acid camptothecin-loaded SLNs were tested in mice following both oral and intravenous injection. …

Reactive oxygen species (ROS) in cancer: from mechanism to therapeutic implications.

Reactive oxygen species (ROS) act as critical secondary messengers in various intracellular signaling pathways that regulate cellular proliferation, differentiation, and survival under normal physiological conditions. However, dysregulation of redox signaling-driven by genetic mutations, epigenetic alterations, and posttranscriptional or posttranslational modifications-plays a central role in malignant transformation and cancer progression. Cancer cells typically exhibit elevated basal ROS levels due to increased metabolic activity, mitochondrial dysfunction, and oncogene activation. This mode